Compounds and uses thereof for decreasing activity of hormone-sensitive lipase

[0001] The present invention relates to compounds, compositions containing them, and their use for treating medical disorders where it is desirable to modulate the activity of hormone-sensitive lipase.

[0002] The overall energy homeostasis of a mammalian system requires a high degree of regulation to ensure the availability of the appropriate substrate at the appropriate time. Plasma glucose levels rise during the post-prandial state, to return to pre-prandial levels within 2-3 hours. During these 2-3 hours, insulin promotes glucose uptake by skeletal muscle and adipose tissue and decreases the release of free fatty acids (FFA) from adipocytes, to ensure that the two substrates do not compete with each other. When plasma glucose levels fall, an elevation in plasma FFA is necessary to switch from glucose to fat utilization by the various tissues.

[0003] In individuals with insulin resistance, FFA levels do not fall in response to insulin, as they do in normal individuals, preventing the normal utilization of glucose by skeletal muscle, adipose and liver. Furthermore, there is a negative correlation between insulin sensitivity and plasma FFA levels.

[0004] Hormone-sensitive lipase (HSL) is an enzyme, expressed primarily in adipocytes, that catalyses the conversion of triglycerides to glycerol and fatty acids. It is through the regulation of this enzyme that the levels of circulating FFA are modulated. Insulin leads to the inactivation of HSL with a subsequent fall in plasma FFA levels during the post-prandial state, followed by the activation of the enzyme when the insulin concentration falls and catecholamines rise during the post-absorptive period. The activation of HSL leads to an increase in plasma FFA, as they become the main source of energy during fasting.

[0005] The activation-inactivation of HSL is primarily mediated through the cAMP-protein kinase A and AMP-dependent kinase pathways. There are compounds like nicotinic acid and its derivatives, that decrease the activation of HSL via these pathways and cause a decrease in lipolysis that leads to a reduction in the FFA levels. These drugs have a beneficial effect in the utilization of glucose and in the normalization of the excess triglyceride synthesis seen in patients with elevated FFA. However, since these pathways are used by other processes in the body, these drugs have severe side effects.

[0006] We have found compounds that specifically inhibit the lipolytic activity of HSL and lead to a decrease in plasma FFA levels. These compounds can be used to treat disorders where a decreased level of plasma FFA is desired, such as insulin resistance, syndrome X, dyslipidemia, abnormalities of lipoprotein metabolism.

[0007] One object of the present invention is to provide compounds and pharmaceutical compositions that inhibit the lipolytic activity of HSL. A further object is to provide compounds which have good pharmaceutical properties such as solubility, bioavailability etc.

[0008] Definitions

[0009] The following is a detailed definition of the terms used to describe the compounds of the invention.

[0010] Halogen designates an atom selected from the group consisting of F, Cl, Br and I.

[0011] The term C_1-6-alkyl in the present context designates a saturated, branched or straight hydrocarbon group having from 1 to 6 carbon atoms. Representative examples include, but are not limited to, methyl, ethyl, n-propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, n-hexyl, isohexyl and the like.

[0012] The term C_2-6-alkyl in the present context designates a saturated, branched or straight hydrocarbon group having from 2 to 6 carbon atoms. Representative examples include, but are not limited to, ethyl, n-propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, neopentyl, tert-pentyl, n-hexyl, isohexyl and the like.

[0013] The term C_1-6alkoxy in the present context designates a group OC_1-6-alkyl wherein C_1-6-alkyl is as defined above. Representative examples include, but are not limited to, methoxy, ethoxy, n-propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, isopentoxy, neopentdxy, tert-pentoxy, n-hexoxy, isohexoxy and the like.

[0014] The term C_3-8-alkoxy in the present context designates a group OC_1-6alkyl wherein C_3-8-alkyl is a saturated, branched or straight hydrocarbon group having from 3-6 carbon atoms. Representative examples of C_3-6-alkoxy include, but are not limited to, n-propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentoxy, isopentoxy, neopentoxy, tert-pentoxy, n-hexoxy, isohexoxy and the like.

[0015] The term C_2-6-alkenyl as used herein, represent an olefinically unsaturated branched or straight hydrocarbon group having from 2 to 6 carbon atoms and at least one double bond. Examples of such groups include, but are not limited to, vinyl, 1-propenyl, 2-propenyl, allyl, iso-propenyl, 1,3-butadienyl, 1-butenyl, hexenyl, pentenyl and the like.

[0016] The term C_3-10-cycloalkyl as used herein represents a saturated mono-, bi-, tri- or spirocarbocyclic group having from 3 to 10 carbon atoms. Representative examples are cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, cyclononyl, cyclodecyl, bicyclo3.2.1octyl, spiro4.5decyl, norpinyl, norbonyl, norcaryl, adamantyl and the like.

[0017] The term C_3-8-heterocyclyl as used herein represents a saturated 3 to 8 membered ring containing one or more heteroatoms selected from nitrogen, oxygen and sulfur. Representative examples are pyrrolidyl, piperidyl, piperazinyl, morpholinyl, thiomorpholinyl, aziridinyl, tetrahydrofuranyl and the like.

[0018] The term aryl as used herein represents a carbocyclic aromatic ring system being either monocyclic, bicyclic, or polycyclic, such as phenyl, biphenyl, naphthyl, anthracenyl, phenanthrenyl, fluorenyl, indenyl, pentalenyl, azulenyl, biphenylenyl and the like. Aryl is also intended to include the partially hydrogenated derivatives of the carbocyclic aromatic systems enumerated above. Non-limiting examples of such partially hydrogenated derivatives are 1,2,3,4-tetrahydronaphthyl, 1,4-dihydronaphthyl and the like.

[0019] The term aryloxy as used herein represents an aryl which is linked via an oxygen atom, e.g. phenoxy, 1-naphthyloxy, 2-naphthyloxy and the like.

[0020] The term heteroaryl as used herein represents a heterocyclic aromatic ring system containing one or more heteroatoms selected from nitrogen, oxygen and sulfur such as furyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, pyranyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, 1,2,3-triazinyl, 1,2,4-triazinyl, 1,3,5-triazinyl, 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,3-thiadiazolyl, 1,2,4-thiadiazolyl, 1,2,5-thiadiazolyl, 1,3,4-thiadiazolyl, tetrazolyl, thiadiazinyl, indolyl, isoindolyl, benzofuranyl, benzothiophenyl (thianaphthenyl), indazolyl, benzimidazolyl, benzthiazolyl, benzisothiazolyl, benzoxazolyl, benzisoxazolyl, purinyl, quinazolinyl, quinolizinyl, quinolinyl, isoquinolinyl, quinoxalinyl, naphthyridinyl, pteridinyl, carbazolyl, azepinyl, diazepinyl, acridinyl and the like. Heteroaryl is also intended to include the partially hydrogenated derivatives of the heterocyclic systems enumerated above. Non-limiting examples of such partially hydrogenated derivatives are 2,3-dihydrobenzofuranyl, 3,4-dihydroisoquinolinyl, pyrrolinyl, pyrazolinyl, indolinyl, oxazolidinyl, oxazolinyl, oxazepinyl and the like.

[0021] The term perhalomethyl as used herein designates a methyl moiety substituted with three halogen atoms. Non-limiting examples of perhalomethyl are CF₃, CCl₃, and CF₂Cl.

[0022] The term perhalomethoxy as used herein designates a perhalomethyl linked via an oxygen atom, e.g. OCF₃, OCCl₃, and OCF₂Cl

[0023] The term ring system as used herein includes aromatic as well as non-aromatic ring moieties, which may be monocyclic, bicyclic or polycyclic, and they encompass moieties with zero, one or more hetereatoms selected from nitrogen, oxygen and sulphur. Non-limiting examples of such ring systems are aryl, C_3-8-heterocyclyl and heteroaryl.

[0024] The term heterocyclic system as used herein includes aromatic as well as non-aromatic ring moieties, which may be monocyclic, bicyclic or polycyclic, and containing in their ring structure one or more heteroatoms selected from nitrogen, oxygen and sulfur. Non-limiting examples of such heterocyclic systems are C_3-8-heterocyclyl and heteroaryl.

[0025] Certain of the above defined terms may occur more than once in the structural formulae, and upon such occurrence each term shall be defined independently of the other.

[0026] The term optionally substituted as used herein means that the groups in question are either unsubstituted or substituted with one or more of the substituents specified. When the groups in question are substituted with more than one substituent the substituents may be the same or different.

[0027] The term optionally covalently bound as used herein means that the substituents in question are either not covalently bound to each other or the substituents are directly connected to each other by a covalent bond. A non-limiting example of such optionally covalently bound substituents is NR¹R² wherein R¹ is ethyl and R² is propyl which provided that the substituents, ethyl and propyl, are optionally covalently bound may be ethyl-propyl-amino, 1-piperidyl, 3-methyl-1-pyrrolidyl or 2,3-dimethyl-1-azetidyl.

[0028] The term hydrolysable group as used herein means a group which can be hydrolysed at certain chemical conditions, i.e. an internal covalent bond in the group can be cleaved to give two compounds. A hydrolysable group does not have to be hydrolysed during carrying out the present invention. For instance, the hydrolysable group C(X)-L can be hydrolysed to give the products C(X)OH and HL, which means that the covalent bond between C(X) and L is cleaved. Examples of hydrolysable groups are carbamates, esters and amides.

[0029] The terms disease, condition and disorder as used herein are used interchangeably to specifiy a state of a patient which is not the normal physiological state of man.

[0030] The term treatment as used herein means the management and care of a patient having developed a disease, condition or disorder, as well as the management and care of an individual at risk of developing the disease, condition or disorder prior to the clinical onset of said disease, condition or disorder. The purpose of treatment is to combat the disease, condition or disorder, as well as to to combat the development of the disease, condition or disorder. Treatment includes the administration of the active compounds to prevent or delay the onset of the symptoms or complications and to eliminate or control the disease, condition or disorder as well as to alleviate the symptoms or complications associated with the disease, condition or disorder.

[0031] The term effective amount as used herein means a dosage which is sufficient in order for the treatment of the patient to be effective compared with no treatment.

[0032] The term modulate as used herein means to influence, i.e. to modulate a parameter means to influence that parameter in a desired way. Examples are to modulate insulin secretion from beta cells and to modulate the plasma level of free fatty acids.

[0033] The term medicament as used herein means a pharmaceutical composition suitable for administration of the pharmaceutically active compound to a patient.

[0034] The term pharmaceutically acceptable as used herein means suited for normal pharmaceutical applications, i.e. giving rise to no adverse events in patients etc.

[0035] The present invention relates to compounds of the general formula II

[0036] wherein R¹ is selected from C_1-6-alkyl, C_2-6-alkenyl and C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano and nitro; and

[0037] R² is selected from C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0038] wherein R² is optionally covalently bound to R¹ by an ether, thioether, CC or CN bond, to form a ring system with the N-atom to which R¹ and R² are bound; and

[0039] R³ is selected from hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_3-10-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C₃-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0040] X is O or S; or

[0041] a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or any tautomeric forms, stereoisomers, mixture of stereoisomers including a racemic mixture, or polymorphs.

[0042] In an aspect of the invention, compounds are of the general formula III

[0043] wherein R^1a and R^2a are independently selected from C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano and nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, perhalomethyl and perhalomethoxy; and

[0044] wherein R^1a is optionally covalently bound to R^2a by an ether, thioether, CC or CN bond, to form a ring system with the N-atom to which R^1a and R^2a are bound; and

[0045] R^4a, R^5a, R^6a and R^7a are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which is optionally substituted by one or more substituents selected from hydroxy, sulfanyl, sulfo, oxo, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, perhalomethyl and perhalomethoxy; and

[0046] A^1a is N or CR^8a; A^2a is N or CR^9a; A^3a, is N or CR^10a; A^4a is N or CR^11a; and A^5a is N or CR^12a; and

[0047] wherein R^8a, R^9a, R^10a, R^11a and R^12a are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, perhalomethyl and perhalomethoxy.

[0048] In one embodiment, the invention is concerned with compounds of formula (III), wherein R^2a is phenyl, optionally substituted by halogen or methyl.

[0049] In another embodiment, the invention in concerned with compounds of formula (III), wherein R^1a is selected from methyl and ethyl, optionally substituted by one or more halogen.

[0050] In another embodiment, the invention in concerned with compounds of formula (III), wherein R^1a and R^2a are covalently bound so as to form a ring system with the N-atom to which they are bound, wherein said ring system is a piperidine, piperazine, morpholine, or thiomorpholine.

[0051] In another embodiment, the invention in concerned with compounds of formula (III), wherein R^4a, R^5a, R^6a and R^7a are independently selected from hydrogen, F, Cl, C_1-6alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0052] In another embodiment, the invention in concerned with compounds of formula (III), wherein A^1a, A^2a, A^3a, A^4a and A^5a are independently selected from N, CH, CF, CCl and CCF₃.

[0053] In an aspect of the invention, compounds are of the general formula IV

[0054] wherein R^1b and R^2b are independently selected from C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy;

[0055] wherein R^1b is optionally covalently bound to R^2b by an ether, thioether, CC or CN bond, to form a ring system with the N-atom to which R^1b and R^2b are bound;

[0056] R^5b and R^6b are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, perhalomethyl and perhalomethoxy;

[0057] R^4b and R^7b are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, perhalomethyl and perhalomethoxy; and

[0058] A^1b is N or CR^8b; A^2b is N or CR^9b; A^3b is N or CR^10b; A^4b is N or CR^11b; and A^5b is N or CR^12b; and

[0059] wherein R^8b, R^9b, R^10b, R^11b and R^12b are selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, perhalomethyl and perhalomethoxy;

[0060] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4b, R^5b, R^6b, R^7b, R^8b, R^9b, R^10b, R^11b and R^12b.

[0061] In one embodiment, the invention is concerned with compounds of formula IV, wherein R^2b is phenyl, optionally substituted by halogen.

[0062] In another embodiment, the invention is concerned with compounds of the general formula IV, wherein R^1b is selected from methyl and ethyl, optionally substituted by one or more halogen.

[0063] In another embodiment, the invention is concerned with compounds of the general formula IV, wherein R^1b and R^2b are covalently bound so as to form a ring system with the N-atom to which they are bound, wherein the ring system is a piperidine, piperazine, morpholine, or thiomorpholine.

[0064] In another embodiment, the invention is concerned with compounds of the general formula IV, wherein R^4b, R^5b, R^6b and R^7b are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0065] In another embodiment, the invention is concerned with compounds of the general formula IV, wherein A^1b, A^2b, A^3b, A^4b and A^5b are independently selected from N, CH and CF.

[0066] In an aspect of the invention, compounds are of the general formula V

[0067] wherein R^4c, R^5c, R^6c, R^7c and R^8c are independently selected from hydrogen, hydroxy, sulfanyl, amino, halogen, cyano, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0068] R^9c, R^10c, R^11c, R^12c and R^13c are independently selected from hydrogen, sulfanyl, amino, halogen, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6 alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0069] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4c, R^5c, R^6c, R^7c and R^8c; and

[0070] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9c, R^10c, R^11c, R^12c and R^13c; and

[0071] at least one of R^4c, R^5c, R^6c, R^7c, R^8c, R^9c, R^10c, R^11c, R^12c and R^13c are different from hydrogen.

[0072] In one embodiment, the invention is concerned with compounds of formula V, wherein R^9c, R^10c, R^11c, R^12c and R^13c are selected from H and F.

[0073] In another embodiment, the invention is concerned with compounds of the general formula V, wherein R^4c, R^5c, R^6c, R^7c and R^8c are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0074] In another embodiment, the invention is concerned with compounds of the general formula V, where there are no covalent bonds between any of the substituents R^9c, R^10c, R^11c, R^12c and R^13c.

[0075] In another embodiment, the invention is concerned with compounds of the general formula V, where there are no covalent bonds between any of the substituents R^4c, R^5c, R^6c, R^7c and R^8c.

[0076] In an aspect of the invention, compounds are of the general formula VI

[0077] wherein R^4d and R^5d are independently selected from hydrogen, hydroxy, sulfanyl, amino, C_2-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, C_2-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0078] R^6d, R^7d, R^8d, R^9d, R^10d, R^11d, R^12d, R^13d and R^14d are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6 alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy:

[0079] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group-consisting of R^4d, R^5d, R^6d, R^7d, R^8d and R^9d; and

[0080] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^10d, R^11d, R^12d, R^13d and R^14d.

[0081] In one embodiment, the invention is concerned with compounds of the general formula VI, wherein R^4d and R^5d are H.

[0082] In another embodiment, the invention is concerned with compounds of the general formula VI, wherein R^6d, R^7d, R^8d and R^9d are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0083] In another embodiment, the invention is concerned with compounds of the general formula VI, wherein R^10d, R^11d, R^12d, R^13d and R^14d are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0084] In another embodiment, the invention is concerned with compounds of the general formula VI, wherein there are no covalent bonds between any of the substituents R^4d, R^5d, R^6d, R^7d, R^8d and R^9d.

[0085] In another embodiment, the invention is concerned with compounds of the general formula VI, wherein there are no covalent bonds between any of the substituents R^10d, R^11d, R^12d, R^13d and R^14d.

[0086] In an aspect of the invention, compounds are of the general formula VII

[0087] wherein R^4e is selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, C_2-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0088] R^5e is selected from hydrogen, F, cyano, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy;

[0089] wherein R^4e and R^5e may be covalently bound to each other by a CO bond.

[0090] In one embodiment, the invention is concerned with compounds of the general formula VII, wherein R^4e or R^5e is selected from the group consisting of

[0091] wherein R^6e, R^7e, R^8e, R^9e and R^10e are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl.

[0092] In another embodiment, the invention is concerned with compounds of the general formula VII, wherein R^4e or R^5e is selected from the group consisting of

[0093] wherein R^6e, R^7e, R^8e, R^9e and R^10e are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy and C_2-6-alkenyl.

[0094] In another embodiment, the invention is concerned with compounds of the general formula VII, wherein at least one of the substituents R^6e, R^7e, R^8e, R^9e and R^10e are selected from the group consisting of F and perhalomethyl.

[0095] In another embodiment, the invention is concerned with compounds of the general formula VII, wherein R^4e and R^5e are connected by a CO bond to form the compound

[0096] wherein R^11e is selected from hydrogen, hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0097] R^12e is selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0098] In an aspect of the invention, compounds are of the general formula VIII

[0099] wherein R^4f, R^5f, R^6f, R^7f, R^9f and R^10f are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: with the proviso that R^4f and R^5f are not both methoxy; and

[0100] R^8f is selected from hydrogen, sulfo, C_1-6-alkyl, C_1-1-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-5-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy;

[0101] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4f, R^5f, R^6f, R^7f and R^8f; and

[0102] wherein there may optionally be a covalent bond between R^9f and R^10f.

[0103] In one embodiment, the invention is concerned with compounds of the general formula VIII, wherein R^9f and R^10f are covalently bound so as to form a ring system with the C-atom to which they are bound.

[0104] In another embodiment, the invention is concerned with compounds of the general formula VIII, wherein said ring system is a cycloalkyl, phenyl, heteroaryl, piperidine, piperazine, morpholine, or thiomorpholine.

[0105] In another embodiment, the invention is concerned with compounds of the general formula VIII, wherein R^4f and R^8f are connected by a CO bond to form the compound

[0106] wherein R^11f is selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0107] R^17f is selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl; and

[0108] wherein there may optionally be a covalent bond between R^9f and R^10f.

[0109] In an aspect of the invention, compounds are of the general formula IX

[0110] wherein R^4g, R^5g, R^6g, R^7g, R^8g, R^9g, R^10g and R^11g are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0111] R^12g is selected from the group consisting of C(O), C(O)NH, CH₂, CH₂CH₂, CHR^15g, CH₂CHR^15g, CHR^15gCH₂, NH, NR^15g, NHC(O), NR^15gC(O), O, S, S(O), S(O)₂;

[0112] wherein R^15g is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0113] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4g, R^5g, R^6g, R^7g and R^15g; and

[0114] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^8g, R^9g, R^10g, R^11g and R^15g; and

[0115] R^13g is selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0116] R^14g is selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, C_2-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0117] wherein R^13g and R^14g may optionally be covalently bound to each other.

[0118] In one embodiment, the invention is concerned with compounds of the general formula IX, wherein R^13g and R^14g are covalently bound so as to form a ring system with the N-atom to which they are bound.

[0119] In another embodiment, the invention is concerned with compounds of the general formula IX, wherein said ring system is a piperidine, piperazine, morpholine, or thiomorpholine.

[0120] In another embodiment, the invention is concerned with compounds of the general formula IX, wherein there are no covalent bonds between any of the substituents R^4g, R^5g, R^6g, R^7g and R^15g.

[0121] In another embodiment, the invention is concerned with compounds of the general formula IX, wherein there are no covalent bonds between any of the substituents R^8g, R^9g, R^10g, R^11g and R^15g.

[0122] In another embodiment, the invention is concerned with compounds of the general formula IX, wherein R^4g, R^5g, R^6g, R^7g, R^8g, R^9g, R^10g, R^11g are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0123] In an aspect of the invention, compounds are of the general formula X

[0124] wherein R^4h and R^5h are independently selected from cyano, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0125] R^6h, R^7h, R^8h, R^9h, R^10h, R^12h, R^14h and R^15h are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0126] R^11h and R^13h are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, perhalomethyl, perhalomethoxy, C_2-6-alkyl, methoxy, C_3-8-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfanyl, amino, C_2-6-alkyl, C_3-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C₂alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0127] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4h, R^5h, R^6h, R^7h, R^8h, R^9h; and

[0128] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^10h, R^11h, R^12h, R^13h, R^14h and R^15h.

[0129] In one embodiment, the invention is concerned with compounds of the general formula X, wherein R^6h, R^7h, R^8h, R^9h, R^10h, R^12h and R^14h are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0130] In another embodiment, the invention is concerned with compounds of the general formula X, wherein there are no covalent bonds between R^4h, R^5h, R^6h, R^7h, R^8h and R^9h.

[0131] In another embodiment, the invention is concerned with compounds of the general formula X, wherein there are no covalent bonds between R^10h, R^11h, R^12h, R^13h, R^14h and R^15h.

[0132] In another embodiment, the invention is concerned with compounds of the general formula X, wherein R^15h is hydrogen.

[0133] In another embodiment, the invention is concerned with compounds of the general formula X, wherein R^11h and R^13h are selected from the group consisting of hydrogen, F, Cl, C_2-6-alkyl, methoxy, C_3-6-alkoxy, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0134] In an aspect of the invention, compounds are of the general formula XI

[0135] R⁵ⁱ is selected from hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0136] R⁶ⁱ, R⁷ⁱ, R⁸ⁱ, R⁹ⁱ, R¹⁰ⁱ, R¹⁴ⁱ and R¹⁵ⁱ are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0137] R¹¹ⁱ and R¹³ⁱ are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, methoxy, C_3-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfanyl, sulfo, C_1-6-alkyl, C_3-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6 alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0138] R¹²ⁱ is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy.

[0139] In one embodiment, the invention is concerned with compounds of the general formula XI, wherein R⁶ⁱ, R⁷ⁱ, R⁸ⁱ and R⁹ⁱ are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0140] In another embodiment, the invention is concerned with compounds of the general formula XI, wherein R¹⁰ⁱ, R¹¹ⁱ, R¹²ⁱ, R¹³ⁱ and R¹⁴ⁱ are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0141] In another embodiment, the invention is concerned with compounds of the general formula XI, wherein R¹⁵ⁱ is hydrogen.

[0142] In another embodiment, the invention is concerned with compounds of the general formula XI, wherein R¹⁰ⁱ, R¹¹ⁱ, R¹²ⁱ, R¹³ⁱ, R¹⁴ⁱ and R¹⁵ⁱ are selected from the group consisting of H, F and methyl.

[0143] In an aspect of the invention, compounds are of the general formula XII

[0144] wherein R^4j, R^5j, R^6j, R^7j, R^8j, R^9j and R^10j are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0145] wherein there may optionally be a covalent bond between the substituents R^6j and R^7j; and

[0146] wherein there may optionally be a covalent bond between R^5j and R^8j; and

[0147] R^11j and R^12j are independently selected from cyano, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, Cl-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one-or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0148] with the proviso that R^9j and R^10j are both hydrogen, there may optionally be a covalent bond connecting R^11j and R^12j.

[0149] In one embodiment, the invention is concerned with compounds of the general formula XII, wherein R^4j, R^5j, R^6j and R^7j are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C, r-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0150] In another embodiment, the invention is concerned with compounds of the general formula XII, wherein at least one of the substituents R^4j, R^5j, R^6j and R^7j are different from hydrogen. In another embodiment, the invention is concerned with compounds of the general formula XII, wherein R^8j is covalently bound to R^5j.

[0151] In an aspect of the invention, compounds are of the general formula XIII

[0152] wherein R^4k is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0153] R^5k is selected from hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: with the proviso that when R^4k is hydrogen, then R^5k is not C(O)N(Me)₂; and

[0154] R^6k, R^7k, R^8k, R^9k, R^10k, R^11k, R^12k, R^13k and R^14k are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0155] R^12k is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0156] wherein there may optionally be a covalent bond between any of the substituents selected from the group consisting of R^4k, R^5k, R^7k and R^8k; and

[0157] wherein there may optionally be a covalent bond between R^5k and any one of the substituents R^7k and R^8k; and

[0158] wherein there may optionally be one or more covalent bonds between R^10k, R^11k, R^12k, R^13k and R^14k.

[0159] In one embodiment, the invention is concerned with compounds of the general formula XIII, wherein the substituents R^4k and R^5k are connected by a covalent bond.

[0160] In another embodiment, the invention is concerned with compounds of the general formula XIII, wherein the substituents R^5k and R^8k are connected by a covalent bond.

[0161] In another embodiment, the invention is concerned with compounds of the general formula XIII, wherein the substituents R^10k and R^11k are connected by a covalent bond.

[0162] In another embodiment, the invention is concerned with compounds of the general formula XIII, wherein the substituents R^12k and R^13k are connected by a covalent bond.

[0163] In another embodiment, the invention is concerned with compounds of the general formula XIII, wherein R^6k, R^7k, R^8k and R^9k are selected from the group consisting of hydrogen, F, Cl, hydroxy, amino, methyl, methoxy, ethoxy and perhalomethyl.

[0164] In another embodiment, the invention is concerned with compounds of the general formula XIII, wherein R^10k, R^11k, R^12k, R^13k and R^14k are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0165] In an aspect of the invention, compounds are of the general formula XIV

[0166] wherein R¹ is C_1-6-alkyl, C_2-6-alkenyl or C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano and nitro; and

[0167] R² is C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, or C_3-10-cycloalkyl, each of which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, perhalomethyl and perhalomethoxy; with the proviso that when R¹ and R² are identical they are not methyl or benzyl; and

[0168] R² is optionally covalently bound to R¹ by an ether, thioether or CC bond, to form a ring system with the N-atom to which R¹ and R² are bound; and

[0169] R^5l, R^6l, R^8l, R^9l, R^10l and R^11l are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl; sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0170] R^4l and R^7l are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, methoxy, C_3-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfanyl, sulfo, amino, C_1-6-alkyl, C_3-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6 alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0171] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4l, R^5l, R^6l, R^7l, R^8l, R^9l, R^10l and R^11l.

[0172] In one embodiment, the invention is concerned with compounds of the general formula XIV, wherein R¹ and R² are covalently bound so as to form a ring system with the N-atom to which they are bound.

[0173] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein said ring system is a piperidine, piperazine, morpholine, or thiomorpholine.

[0174] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein there are no covalent bonds between R¹ and R².

[0175] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein there are no covalent bonds between R^8l and any of the substituents selected from the group consisiting of R^9l, R^10l, R^11l.

[0176] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein there are no covalent bonds between R^8l and any of the substituents selected from the group consisting of R^4l, R^5l, R^6l and R^7l.

[0177] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein there are no covalent bonds between any of the substituents R^4l, R^5l, R^6l, R^7l, R^8l, R^9l, R^10l and R^11l.

[0178] In another embodiment, the invention is concerned with compounds of the general formula XIV, wherein R^4l, R^5l, R^6l and R^7l are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0179] In an aspect of the invention, compounds are of the general formula XV

[0180] wherein R^4m is selected from hydrogen, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0181] R^5m, R^6m, R^7m, R^8m, R^9m, R^10m, R^11m, R^12m, R^13m, R^14m, R^15m and R^16m are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0182] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4m, R^5m, R^6m, R^7m and R^8m; and

[0183] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9m, R^10m, R^11m, R^12m, R^13m, R^14m, R^15m and R^16m.

[0184] In one embodiment, the invention is concerned with-compounds of the general formula XV, wherein there are no covalent bonds between any of the substituents selected from the group consisting of R^5m, R^6m, R^7m and R^8m.

[0185] In another embodiment, the invention is concerned with compounds of the general formula XV, wherein there are no covalent bonds between any of the substituents R^9m, R^10m, R^11m, R^12m and R^13m.

[0186] In another embodiment, the invention is concerned with compounds of the general formula XV, wherein there are no covalent bonds between any of the substituents R^14m, R^15m and R^16m,

[0187] In another embodiment, the invention is concerned with compounds of the general formula XV, wherein R^4m is covalently bound to R^6m.

[0188] In another embodiment, the invention is concerned with compounds of the general formula XV, wherein R^5m, R^6m, R^7m, R^8m, R^9m, R^10m, R^11m, R^12m, R^13m and R^14m are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0189] In another embodiment, the invention is concerned with compounds of the general formula XV, wherein R^14m, R^15m and R^16m are selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0190] In an aspect of the invention, compounds are of the general formula XVI

[0191] wherein R⁴ⁿ is selected from hydrogen, sulfo, C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_2-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0192] Z is selected from S, S(O) and S(O)₂; and

[0193] R⁵ⁿ, R⁶ⁿ, R⁷ⁿ, R⁸ⁿ, R⁹ⁿ, R¹⁰ⁿ, R¹¹ⁿ, R¹²ⁿ, R¹³ⁿ and R¹⁴ⁿ are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0194] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R⁴ⁿ, R⁵ⁿ, R⁶ⁿ, R⁷ⁿ and R⁸ⁿ; and

[0195] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R¹⁰ⁿ, R¹¹ⁿ, R¹²ⁿ and R¹⁴ⁿ; and

[0196] at least one of the substituents R⁵ⁿ, R⁶ⁿ, R⁷ⁿ, R⁸ⁿ, R⁹ⁿ, R¹⁰ⁿ, R¹¹ⁿ, R¹²ⁿ, R¹³ⁿ and R¹⁴ⁿ are different from hydrogen.

[0197] In one embodiment, the invention is concerned with compounds of the general formula XVI, wherein there are no covalent bonds between any of the substituents R⁵ⁿ, R⁶ⁿ, R⁷ⁿ and R⁸ⁿ.

[0198] In another embodiment, the invention is concerned with compounds of the general formula XVI, wherein there are no covalent bonds between any of the substituents R¹⁰ⁿ, R¹¹ⁿ, R¹²ⁿ.

[0199] In another embodiment, the invention is concerned with compounds of the general formula XVI, wherein R¹⁴ⁿ is not covalently bound to any other substituent selected from the group consisting of R⁴ⁿ, R⁵ⁿ, R⁶ⁿ, R⁷ⁿ, R⁸ⁿ, R¹⁰ⁿ, R¹¹ⁿ, R¹²ⁿ.

[0200] In another embodiment, the invention is concerned with compounds of the general formula XVI, wherein R⁴ⁿ is covalently bound to R⁶ⁿ.

[0201] In another embodiment, the invention is concerned with compounds of the general formula XVI, wherein R⁵ⁿ, R⁶ⁿ, R⁷ⁿ and R⁸ⁿ are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0202] In another embodiment, the invention is concerned with compounds of the general formula XVI, wherein R¹⁴ⁿ is selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0203] In an aspect of the invention, compounds are of the general formula XVII

[0204] wherein R^2o, is selected from sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^2o, is not methyl; and

[0205] R^4o, R^5o, R^6o and R^7o are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0206] A^1o is N or CR^8o; A^2o is N or CR^9o; A^3o is N or CR^10o; A^4o is N or CR^11o; and A^5o is N or CR^12o; and

[0207] wherein R^8o, R^9o, R^10o, R^11o and R^12o are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano,-nitro-, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, perhalomethyl and perhalomethoxy; with the proviso that

[0208] when A^1o, A^2o, A^3o, A^4o and A^5o are all CH, and R^4o, R^5o, R^6o and R^7o are all hydrogen, then R^2o is not phenyl; and

[0209] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4o, R^5o, R^6o, R^7o, R^8o, R^9o, R^10o, R^11o and R^12o

[0210] In one embodiment, the invention is concerned with compounds of the general formula XVII, wherein there are no covalent bonds between any of the substituents R^4o, R^5o, R^6o and R^7o. In another embodiment, the invention is concerned with compounds of the general formula XVII, wherein there are no covalent bonds between any of the substituents A^1o, A^2o, A^3o, A^4o and A^5o.

[0211] In another embodiment, the invention is concerned with compounds of the general formula XVII, wherein R^2o is selected from the group consisting of cycloalkyl, phenyl, piperidine, piperazine, morpholine, thiomorpholine and heteroaryl.

[0212] In another embodiment, the invention is concerned with compounds of the general formula XVII, wherein R^4o, R^5o, R^6o and R^7o are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0213] In an aspect of the invention, compounds are of the general formula XVIII

[0214] wherein R^4p is selected from hydrogen, sulfo, C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0215] R^5p, R^6p, R^7p and R^8p are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, F, amino, cyano, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0216] R^9p, R^10p, R^11p, R^12p, R^13p, R^14p, R^15p and R^16p are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0217] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^5p, R^6p and R^7p; and

[0218] wherein there may optionally be a covalent bond between R^4p and R^5p so as to form a chromen ring system; and

[0219] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9p, R^10p, R^11p, R^12p, R^13p, R^14p, R^15p and R^16p; and

[0220] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^17p and CR^17pR^18p; and

[0221] wherein R^17p and R^18p are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy.

[0222] In one embodiment, the invention is concerned with compounds of the general formula XVIII, wherein E is selected from the group consisting of O and CR^17pR^18p.

[0223] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^4p and R^5p are connected by a covalent bond so as to form said chromen ring system.

[0224] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^4p and R^5p are connected by a covalent bond so as to form the chromen ring system

[0225] wherein R^19p is selected from the group consisting of hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy.

[0226] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^4p is selected from the group consisting of

[0227] wherein R^20p, R^21p, R^22p, R^23p and R^24p are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, perhalomethyl and perhalomethoxy.

[0228] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein there are no covalent bonds between any of the substituents R^4p, R^5p, R^6p, R^7p and R^8p.

[0229] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein there are no covalent bonds between any of the substituents R^9p, R^10p, R^11p, R^12p, R^13p, R^14p, R^15p and R^16p.

[0230] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^10p and R^11p are connected by a covalent bond.

[0231] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^9p, R^10p, R^11p, R^12p, R^13p, R^14p, R^15p and R^16p are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0232] In another embodiment, the invention is concerned with compounds of the general formula XVIII, wherein R^5p, R^6p, R^7p and R^8p are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0233] In an aspect of the invention, compounds are of the general formula XIX

[0234] wherein R^4q, R^6q, R^7q, R^9q, R^10q, R^11q, R^12q, R^13q, R^14q, R^15q, R^16q, R^17q and R^18q are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy,-sulfanyl, amino, sulfo, C_1-4-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0235] R^5q and R^8q are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, F, Br, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents-independently-selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0236] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4q, R^5q, R^6q, R^7q and R^8q; and

[0237] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9q, R^10q, R^11q, R^12q, R^13q, R^14q, R^15q, R^16q, R^17q and R^18q.

[0238] In one embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^4q and R^6q are connected by a covalent bond.

[0239] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^4q is selected from the group consisting of substituted heteroaryl and substituted C_3-8-heterocyclyl.

[0240] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^4q is selected from the group consisting of

[0241] wherein R^19q, R^20q, R^21q, R^22q and R^23q are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy.

[0242] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein there are no covalent bonds between any of the substituents R^4q, R^5q, R^6q, R^7q and R^8q.

[0243] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein there are no covalent bonds between any of the substituents R^9q, R^10q, R^11q, R^12q, R^13q, R^14q, R^15q, R^16q, R^17q and R^18q.

[0244] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^10p and R^11p are connected by a covalent bond.

[0245] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^10p and R^13p are connected by a covalent bond.

[0246] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^9q, R^10q, R^11q, R^12q, R^13q, R^14q, R^15q, R^16q, R^17q and R^18q are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0247] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^9q, R^10q, R^11q, R^12q, R^14q, R^15q, R^16q, R^17q and R^18q are all hydrogen or F.

[0248] In another embodiment, the invention is concerned with compounds of the general formula XIX, wherein R^5q, R^6q, R^7q and R^8q are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0249] In an aspect of the invention, compounds are of the general formula XX

[0250] wherein R^4r is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: provided that R^4r is not methyl or phenyl; and

[0251] R^5r, R^6r, R^7r, R^8r, R^9r, R^10r, R^11r, R^12r, R^13r, R^14r, R^15r, R^16r, R^17r and R^18r are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, F, amino, cyano, nitro, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6 alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6 alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0252] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^5r, R^6r, R^7r and R^8r; and

[0253] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9r, R^10r, R^11r, R^12r, R^13r, R^14r, R^15r, R^16r, R^17r and R^18r.

[0254] In one embodiment, the invention is concerned with compounds of the general formula XX, wherein R^4r and R^5r are connected by a covalent bond.

[0255] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^4r is selected from the group consisting of substituted heteroaryl and substituted C_3-8-heterocyclyl.

[0256] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^4r is selected from the group consisting of

[0257] wherein R^19r, R^20r, R^21r, R^22r and R^23r are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy.

[0258] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein there are no covalent bonds between any of the substituents R^5r, R^6r, R^7r and R^8r.

[0259] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein there are no covalent bonds between any of the substituents R^9r, R^10r, R^11r, R^12r, R^13r, R^14r, R^15r and R^16r.

[0260] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^10r and R^11r are connected by a covalent bond.

[0261] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^11r and R^13r are connected by a covalent bond.

[0262] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^9r, R^10r, R^11r, R^12r, R^13r, R^14r, R^15r, R^16r, R^17r and R^18r are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0263] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^9r, R^10r, R^11r, R^12r, R^14r, R^15r, R^16r, R^17r and R^18r are all hydrogen or F.

[0264] In another embodiment, the invention is concerned with compounds of the general formula XX, wherein R^5r, R^6r, R^7r and R^8r are independently selected from hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0265] In an aspect of the invention, compounds are of the general formula XXI

[0266] wherein A^1s is N or CR^17s; A^2s is N or CR^18s; A^3s is N or CR^19s; A^4s is N or CR^20s; and A^5s is N or CR^21s; and

[0267] wherein R¹⁷, R^18s, R^19s, R^20s and R^21s are independently selected from hydrogen, hydroxy, sulfanyl, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0268] R^5s, R^6s, R^7s and R^8s are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, F, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6 alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0269] R^9s, R^10s, R^11s, R^12s, R^13s, R^14s, R^15s and R^16s are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, F, amino, cyano, nitro, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl,-wherein-each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8 heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0270] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^22s and CR^22sR^23s; and

[0271] wherein R^22s and R^23s are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0272] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^5s, R^6s, R^7s and R^8s; and

[0273] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9s, R^10s, R^11s, R^12s, R^13s, R^14s, R^15s, R^16s, R^18s, R^19s, R^20s, R^21s, R^22s and R^23s.

[0274] In one embodiment, the invention is concerned with compounds of the general formula XXI, wherein E is selected from the group consisting of O and CR²² R^23s.

[0275] In another embodiment, the invention is concerned with compounds of the general formula XXI, wherein there are no covalent bonds between any of the substituents R^5s, R^6s, R^7s and R^8s.

[0276] In another embodiment, the invention is concerned with compounds of the general formula XXI, wherein R^5s, R^6s, R^7s and R^8s are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0277] In another embodiment, the invention is concerned with compounds of the general formula XXI, wherein there is a covalent bond between R^10s and R^11s.

[0278] In another embodiment, the invention is concerned with compounds of the general formula XXI, wherein there is a covalent bond between R^3s and R^22s.

[0279] In another embodiment, the invention is concerned with compounds of the general formula XXI, wherein R^9s, R^10s, R^11s, R^12s, R^13s, R^14s, R^15s and R^16s are all hydrogen or F.

[0280] In an aspect of the invention, compounds are of the general formula XXII

[0281] wherein E is selected from the group consisting of O, S, S(O), S(O)₂, NR^18t and CR^18tR^19t; and

[0282] R^4t, R^5t, R^6t, R^7t, R^8t, R^9t, R^10t, R^11t, R^12t, R^13t, R^14t, R^15t, R^16t, R^17t, R^18t and R^19t are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, nitro, C_1-6alkyl, C_1-4-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy,-sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^4t and R^5t are not both methyl; and

[0283] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9t, R^10t, R^11t, R^12t, R^13t, R^14t, R^15t, R^16t, R^17t, R^18t and R^19t.

[0284] In one embodiment, the invention is concerned with compounds of the general formula XXII, wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and CR^18tR^19t. In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein R^18t is hydrogen or F.

[0285] In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein R^10t, R^12t, R^14t and R^16t are all hydrogen

[0286] In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein R^6t, R^7t, R^8t and R^9t are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0287] In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein there is a covalent bond between R^11t and R^13t.

[0288] In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein there is a covalent bond between R^13t and R^19t.

[0289] In another embodiment, the invention is concerned with compounds of the general formula XXII, wherein R^10t, R^11t, R^12t, R^13t, R^14t, R^15t, R^16t and R^17t are all hydrogen or F.

[0290] In an aspect of the invention, compounds are of the general formula XXIII

[0291] wherein R^4u, R^5u, R^6u, R^7u, R^8u, R^9u, R^10u, R^11u, R^12u, R^13u, R^14u and R^15u are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: with the proviso that R^4u, R^5u and R^6u are not all hydrogen; and

[0292] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^16u and CR^16uR^17u;

[0293] wherein R^16u and R^17u are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8--heterocyclyl and C_3-10-cycloalkyl; wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0294] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4u, R^5u and R^6u; and

[0295] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^8u, R^9u, R^10u and R^11u; and

[0296] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^2u; R^13u, R^14u, R^15u, R^16u and R^17u.

[0297] In one embodiment, the invention is concerned with compounds of the general formula XXIII, wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and CR^16uR^17u. In another embodiment, the invention is concerned with compounds of the general formula XXIII, wherein R^17u is hydrogen or F.

[0298] In another embodiment, the invention is concerned with compounds of the general formula XXIII, wherein there are no covalent bonds between any of the substituents R^8u, R^9u, R^10u and R^11u.

[0299] In another embodiment, the invention is concerned with compounds of the general formula XXIII, wherein R^8u, R^9u, R^10u and R^11u are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0300] In another embodiment, the invention is concerned with compounds of the general formula XXIII, wherein there is a covalent bond between R^12u and R^13u.

[0301] In another embodiment, the invention is concerned with compounds of the general formula XXIII, wherein R^12u, R^13u, R^14u and R^15u are all selected from the group consisting of hydrogen, F, methyl and C_1-6-alkyl.

[0302] In an aspect of the invention, compounds are of the general formula XXIVa-b

[0303] wherein R^4v, R^5v, R^6v, R^7v, R^8v, R^9v, R^10v, R^11v, R^12v, R^13v, R^14v, R^15v, R^16v, R^17v and R^18v are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that none of the substituents R^4v, R^5v and R^6v are benzothiazolyl or benzooxazolyl; and

[0304] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^19v and CR^19vR^20v; and

[0305] wherein R^19v and R^20v are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0306] wherein there may optionally be a covalent bond between the substituents R^7v and R^8v or between the substituents R^9v and R^10v; and

[0307] wherein there may optionally be a covalent bond between R^6v and a substituent selected from R^8v and R^9v; and

[0308] wherein there may be a covalent bond between any of the substituents selected from the group consisting of R^4v, R^5v and R^6v; and

[0309] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^11v, R^12v, R^13v, R^14v, R^15v, R^16v, R^17v R^18v, R^19v and R²⁰.

[0310] In one embodiment, the invention is concerned with compounds of the general formula XXIV, wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and CR^19vR^20v.

[0311] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein R^20v is hydrogen or F.

[0312] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein there are no covalent bonds between any of the substituents R^4v, R^5v and R^6v.

[0313] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein there are no covalent bonds between any of the substituents R^7v, R^8v, R^9v and R^10v.

[0314] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein there are no covalent bonds between a substituent selected from the group consisting of R^4v, R^5v and R^6v and a substituent selected from the group consisting of R^7v, R^8v, R^9v and R^10v.

[0315] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein R^7v, R^8v, R^9v and R^10v are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0316] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein there is a covalent bond between R^12v and R^13v.

[0317] In another embodiment, the invention is concerned with compounds of the general formula XXIV, wherein R^11v, R^12v, R^13v, R^14v, R^15v, R^16v, R^17v and R^18v are all hydrogen or F.

[0318] In an aspect of the invention, compounds are of the general formula XXV

[0319] wherein R^4w is selected from hydrogen, hydroxy, amino, sulfo, C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, amino, sulfo, C_2-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-8-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, -and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: with the proviso that R^4w is not methyl, morpholine or a 2-chromen derivative; and

[0320] Z is selected from S, S(O) and S(O)₂; and

[0321] R^5w, R^6w, R^7w, R^8w, R^9w, R^10w, R^11w, R^12w, R^13w, R^14w, R^15w and R^16w are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-4-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8 heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy: and

[0322] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^17w and CR^17wR^18w; and

[0323] wherein R^17w and R^18w are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0324] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^4w, R^5w, R^6w, R^7w and R^8w; and

[0325] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9w, R^10w, R^11w, R^12w, R^13w, R^14w, R^15w, R^16w, R^17w and R^18w.

[0326] In one embodiment, the invention is concerned with compounds of the general formula XXV, wherein the only substituents which are covalently bound are R^4w and R^5w.

[0327] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein there are no covalent bonds between any of the substituents R^5w, R^6w, R^7w and R^8w.

[0328] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein there are no covalent bonds between any of the substituents R^9w, R^10w, R^11w, R^12w, R^13w, R^14w, R^15w and R^16w.

[0329] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and CR^17wR^18w.

[0330] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein R^18w is hydrogen or F.

[0331] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein R^5w, R^6w, R^7w and R^8w are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0332] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein there is a covalent bond between R^10w and R^11w.

[0333] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein there is a covalent bond between R^13w and R^17w.

[0334] In another embodiment, the invention is concerned with compounds of the general formula XXV, wherein R^9w, R^10w, R^11w, R^12w, R^13w, R^14w, R^15w and R^16w are all hydrogen or F.

[0335] In an aspect of the invention, compounds are of the general formula XXVI

[0336] wherein R^4x is selected from imino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of imino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0337] R^5x, R^6x, R^7x, R^8x, R^9x, R^10x, R^11x, R^12x and R^13x are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0338] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^14x and CR^15xR^16x;

[0339] wherein R^14x is selected from hydrogen, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0340] R^15x and R^16x are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8 heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0341] wherein there may optionally be a covalent bond between the substituents R^4x and R^5x; and

[0342] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^6x, R^7x, R^8x and R^9x; and

[0343] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^10x, R^11x, R^12x, R^13x, R^14x, R^15x and R^16x.

[0344] In one embodiment, the invention is concerned with compounds of the general formula XXVI, wherein R^6x, R^7x, R^8x and R^9x are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0345] In another embodiment, the invention is concerned with compounds of the general formula XXVI, wherein R^10x, R^11x, R^12x and R^13x are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0346] In another embodiment, the invention is concerned with compounds of the general formula XXVI, wherein there is a covalent bond between the substituents R^6x and R^7x.

[0347] In another embodiment, the invention is concerned with compounds of the general formula XXVI, wherein there is a covalent bond between the substituents R^10x and R^11x.

[0348] In another embodiment, the invention is concerned with compounds of the general formula XXVI, wherein there is a covalent bond between R^10x and a substituent selected from R^14x and R^15x.

[0349] In an aspect of the invention, compounds are of the general formula XXVII

[0350] wherein R^4y and R^11y are independently selected from imino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of imino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0351] R^5y, R^6y, R^7y, R^8y, R^9y and R^10y are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0352] wherein there may optionally be a covalent bond between the substituents R^4y and R^5y; and

[0353] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^6y, R^7Y, R^8y and R^9y; and

[0354] wherein there may optionally be a covalent bond between the substituents R^10y and R^11y.

[0355] In one embodiment, the invention is concerned with compounds of the general formula XXVII, wherein R^6y, R^7y, R^8y and R^9y are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0356] In another embodiment, the invention is concerned with compounds of the general formula XXVII, wherein there are no covalent bonds between any of the substituents R^6y, R^7y, R^8y and R^9y.

[0357] In another embodiment, the invention is concerned with compounds of the general formula XXVII, wherein there is a covalent bond between the substituents R^4y and R^5y.

[0358] In another embodiment, the invention is concerned with compounds of the general formula XXVII, wherein there is a covalent bond between the substituents R^10y and R^11y.

[0359] In an aspect of the invention, compounds are of the general formula XXVIII

[0360] wherein R^4z, R^8z, R^9z, R^10z, R^11z, R^12z, R^13z, R^14z, R^15z, R^16z and R^17z are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0361] R^5z is a carbon bound substituent selected from C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0362] R^6z and R^7z are independently selected from hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0363] E is selected from the group consisting of O, S, S(O), S(O)₂, NR^18z and CR^19zR^20z;

[0364] wherein R^18z is selected from hydrogen, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0365] R^19z and R^20z are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0366] wherein there may optionally be a covalent bond between the substituents R^4z and R^5z; and

[0367] wherein there may optionally be a covalent bond between any of the substituents R^7z, R^8z, and R^9z; and

[0368] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^10z, R^11z, R^12z, R^13z, R^14z, R^15z, R^16z, R^17z, R^18z, R^19z, and R^20z.

[0369] In one embodiment, the invention is concerned with compounds of the general formula XXVIII, wherein there is a covalent bond between the substituents R^4z and R^5z.

[0370] In another embodiment, the invention is concerned with compounds of the general formula XXVIII, wherein R^6z, R^7z, R^8z and R^9z are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0371] In another embodiment, the invention is concerned with compounds of the general formula XXVIII, wherein there is a covalent bond between R^13z and a substituent selected from R^18z and R^19z.

[0372] In an aspect of the invention, compounds are of the general formula XXIX

[0373] wherein R^4aa is selected from hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0374] R^5aa, R^6aa, R^7aa, R^8aa, R^9aa, R^10aa, R^11aa, R^12aa and R^13aa are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0375] wherein there may optionally be a covalent bond between the substituents R^5aa and R^6aa or between the substituent R^7aa and R^8aa; and

[0376] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9aa, R^10aa, R^11aa and R^12aa; and

[0377] E is selected from the group consisting of O, S, S(O) and S(O)₂.

[0378] In one embodiment, the invention is concerned with compounds of the general formula XXIX, wherein there is a covalent bond between the substituents R^9aa and R^10aa.

[0379] In another embodiment, the invention is concerned with compounds of the general formula XXIX, wherein R^5aa, R^6aa, R^7aa and R^8aa are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0380] In another embodiment, the invention is concerned with compounds of the general formula XXIX, wherein at least one of the substituents R^5aa, R^6aa, R^7aa and R^8aa are different from hydrogen.

[0381] In an aspect of the invention, compounds are of the general formula XXX

[0382] wherein R^4ab is selected from sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0383] E is selected from the group consisting of NR^13ab and CR^14abR^15ab; and

[0384] R^5ab, R^6ab, R^7ab, R^8ab, R^9ab, R^10ab, R^11ab, R^12ab, R^13ab, R^14ab and R^15ab are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-4-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0385] wherein there may optionally be a covalent bond between the substituents R^5ab and R^6ab or between the substituent R^7ab and R^8ab; and

[0386] wherein there may optionally be one or more covalent bonds between any of the substituents selected from the group consisting of R^9ab, R^10ab, R^11ab, R^12ab, R^13ab, R^14ab and R^15ab.

[0387] In one embodiment, the invention is concerned with compounds of the general formula XXX, wherein there is a covalent bond between the substituents R^9ab and R^10ab.

[0388] In another embodiment, the invention is concerned with compounds of the general formula XXX, wherein there is a covalent bond between R^10ab and a substituent selected from R^13ab and R^14ab.

[0389] In another embodiment, the invention is concerned with compounds of the general formula XXX, wherein R^5ab, R^6ab, R^7ab and R^8ab are independently selected from the group consisting of hydrogen, F, Cl, C_1-6alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0390] In another embodiment, the invention is concerned with compounds of the general formula XXX, wherein at least one of the substituents R^5ab, R^6ab, R^7ab and R^8ab are different from hydrogen.

[0391] In another embodiment, the invention is concerned with compounds of the general formula XXX, wherein at least one of the substituents R^9ab, R^10ab, R^11ab, R^12ab, R^13ab, R^14ab and R^15ab are different from hydrogen.

[0392] In an aspect of the invention, compounds are of the general formula XXXI

[0393] wherein R^4ac is a carbon bound substituent selected from C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-4-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0394] A^1ac is N or CR^9ac; A^3ac is N or CR^10ac; and A^5ac is N or CR^11ac; and

[0395] R^5ac, R^6ac, R^7ac, R^8ac, R^9ac, R^10ac and R^11ac are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that A^3ac is not CC(OH)(CF₃)₂; and

[0396] A^2ac is N or CR^12ac; and A^4ac is N or CR^13ac; wherein

[0397] R^12ac and R^13ac are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0398] wherein there may optionally be a covalent bond between R^4ac and a substituent selected from the group consisting of R^5ac and R^6ac; with the proviso that A^1ac, A^2ac, A^3ac, A^4ac and A^5ac are not all CH; and

[0399] wherein there may optionally be a covalent bond between any of the substituents R^6ac, R^7ac and R^8ac; and

[0400] wherein there may optionally be one or more covalent bonds between any of the substituents in A^1ac, A^2ac, A^3ac, A^4ac and A^5ac.

[0401] In one embodiment, the invention is concerned with compounds of the general formula XXXI, wherein there is a covalent bond between the substituents R^4ac and R^6ac.

[0402] In another embodiment, the invention is concerned with compounds of the general formula XXXI, wherein there is a covalent bond between A^3ac and A^4ac.

[0403] In another embodiment, the invention is concerned with compounds of the general formula XXXI, wherein there is a covalent bond between A^3ac and A^2ac.

[0404] In another embodiment, the invention is concerned with compounds of the general formula XXXI, wherein R^5ac, R^6ac, R^7ac and R^8ac are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0405] In another embodiment, the invention is concerned with compounds of the general formula XXXI, wherein at least one of the substituents A^1ac, A^2ac, A^3ac, A^4ac and A^5ac are different from CH.

[0406] In an aspect of the invention, compounds are of the general formula XXXIIa-b

[0407] wherein R^4ad is selected from hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, F, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0408] R^5ad, R^6ad, R^7ad, R^8ad and R^9ad are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8 heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0409] R^10ad are selected from imino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, each of which may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_1-6-alkoxy, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and wherein there may optionally be a covalent bond between R^4ad and a substituent selected from R^6ad and R^7ad; and

[0410] wherein there may optionally be a covalent bond between the substituents R^9ad and R^10ad so as to form a 5-membered ring system.

[0411] In one embodiment, the invention is concerned with compounds of the general formula XXXIIa-b, wherein the substituents R^9ad and R^10ad are covalently bound so as to form a 5-membered ring system.

[0412] In another embodiment, the invention is concerned with compounds of the general formula XXXIIa-b, wherein said 5-membered ring system comprises at least one nitrogen atom in the ring.

[0413] In another embodiment, the invention is concerned with compounds of the general formula XXXIIa-b, wherein said 5-membered ring system contains 5 carbons in the ring.

[0414] In another embodiment, the invention is concerned with compounds of the general formula XXXIIa-b, wherein there is a covalent bond between the substituents R^4ad and R^7ad.

[0415] In another embodiment, the invention is concerned with compounds of the general formula XXXIIa-b, wherein R^5ad, R^6ad, R^7ad and R^8ad are independently selected from the group consisting of hydrogen, F, Cl, C_1-6-alkyl, C_1-6alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0416] In another aspect of the invention, compounds are of the general formula XXXIIIa-b

[0417] wherein E is selected from the group consisting of O, S, S(O), S(O)₂, NR^16ae and CR^17aeR^18ae; and

[0418] R^4ae, R^5ae, R^6ae, R^7ae, R^8ae, R^9ae, R^10ae, R^11ae, R^12ae, R^13ae, R^14ae, R^15ae, R^16ae, R^17ae and R^18ae are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0419] wherein there may optionally be a covalent bond between any of the substituents selected from R^4ae, R^5ae, R^6ae and R^7ae; with the proviso that when R^5ae and R^6ae are covalently bound they do not form a isoquinolin-3-yl or a substituted isoquinolin-3-yl together with the pyridine which they are both bound to; and

[0420] wherein there may optionally be a covalent bond between any of the substituents selected from R^8ae, R^9ae, R^10ae, R^11ae, R^12ae, R^13ae, R^14ae, R^15ae, R^16ae, R^17ae and R^18ae.

[0421] In one embodiment, the invention is concerned with compounds of the general formula XXXIIIa-b, wherein there is a covalent bond between R^6ae and R^7ae.

[0422] In another embodiment, the invention is concerned with compounds of the general formula XXXIIIa-b, wherein there is a covalent bond between R^5ae and R^7ae.

[0423] In another embodiment, the invention is concerned with compounds of the general formula XXXIIIa-b, wherein at least one of R^8ae, R^9ae, R^10ae, R^11ae, R^12ae, R^13ae, R^14ae and R^15ae is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0424] In another aspect of the invention, compounds are of the general formula XXXIV

[0425] wherein R^4af, R^5af, R^6af, R^7af, R^8af, R^9af, R^10af, R^11af, R^12af, R^13af, R^14af and R^15af are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0426] wherein there may optionally be a covalent bond between R^6af and any of the substituents selected from R^5af and R^7af; and

[0427] wherein there may optionally be a covalent bond between the substituents R^9af and R^10af; and

[0428] R^16af is selected from hydrogen, hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, C_3-8 heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C₁-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^16af is not methyl; and

[0429] wherein there may optionally be a covalent bond between the substituents R^12af and R^15af.

[0430] In one embodiment, the invention is concerned with compounds of the general formula XXXIV, wherein there is a covalent bond between the substituents R^5af and R^6af.

[0431] In another embodiment, the invention is concerned with compounds of the general formula XXXIV, wherein there is a covalent bond between the substituents R^9af and R^10af.

[0432] In another embodiment, the invention is concerned with compounds of the general formula XXXIV, wherein at least one of R^8af, R^9af, R^10af, R^11af, R^12af, R^13af, R^14af and R^15af is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0433] In another aspect of the invention, compounds are of the general formula XXXV

[0434] wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and CR^16agR^17ag; and

[0435] R^4ag, R^5ag, R^6ag, R^10ag, R^11ag, R^12ag, R^13ag, R^16ag and R^17ag are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl-and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^4ag is not CH₂N(CH₃)₂; and

[0436] wherein there may optionally be a covalent bond between the substituents R^5ag and R^6ag; and

[0437] R^7ag is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6 alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy;

[0438] R^8ag, R^9ag, R^14ag and R^15ag are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-1-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0439] wherein there may optionally be a covalent bond between the substituents R^9ag and R^10ag; and

[0440] wherein there may optionally be a covalent bond between the substituents R^12ag and R^16ag.

[0441] In one embodiment, the invention is concerned with compounds of the general formula XXXV, wherein there is a covalent bond between the substituents R^5ag and R^6ag.

[0442] In another embodiment, the invention is concerned with compounds of the general formula XXXV, wherein there is a covalent bond between the substituents R^9ag and R^10ag.

[0443] In another embodiment, the invention is concerned with compounds of the general formula XXXV, wherein at least one of R^8ag, R^9ag, R^10ag, R^11ag, R^12ag, R^13ag, R^14ag and R^15ag are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0444] In another aspect of the invention, compounds are of the general formula XXXVIa-b

[0445] wherein R^4ah, R^5ah, R^6ah, R^7ah, R^8ah and R^9ah are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^5ah and R^6ah are not both CF₃; and

[0446] wherein there may optionally be a covalent bond between any of the substituents selected from R^4ah, R^5ah, R^6ah and R^7ah; and

[0447] wherein there may optionally be a covalent bond between the substituents R^8ah and R^9ah; with the proviso that when R^8ah and R^9ah together with the carbon to which they are bound forms phenyl then R^5ah, R^6ah, R^7ah and R^8ah are not all hydrogen.

[0448] In one embodiment, the invention is concerned with compounds of the general formula XXXVIa-b, wherein there is a covalent bond between R^8ah and R⁹ h.

[0449] In another embodiment, the invention is concerned with compounds of the general formula XXXVIa-b, wherein there is a covalent bond between R^6ah and R^7ah.

[0450] In another embodiment, the invention is concerned with compounds of the general formula XXXVIa-b, wherein there is a covalent bond between R^5ah and R^6ah.

[0451] In another embodiment, the invention is concerned with compounds of the general formula XXXVIa-b, wherein at least one of R^5ah, R^6ah, R^7ah and R^8ah are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0452] In another aspect of the invention, compounds are of the general formula XXXVII

[0453] R^4ai, R^5ai, R^6ai, R^7ai, R^8ai and R^9ai are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^4ai is not CH₂N(Me)₂; and

[0454] wherein there may optionally be a covalent bond between any of the substituents selected from R^4ai, R^5ai, R^6ai and R^7ai; and

[0455] wherein there may optionally be a covalent bond between the substituents R^8ai and R^9ai; with the proviso that R^8ai and R^9ai together with the carbon to which they are bound do not form 4-methoxy-phenyl, 4-chloro-phenyl or 4-nitro-phenyl.

[0456] In one embodiment, the invention is concerned with compounds of the general formula XXXVII, wherein there is a covalent bond between R^8ai and R^9ai.

[0457] In another embodiment, the invention is concerned with compounds of the general formula XXXVII, wherein there is a covalent bond between R^6ai and R^7ai.

[0458] In another embodiment, the invention is concerned with compounds of the general formula XXXVII, wherein there is a covalent bond between R^5ai and R^6ai.

[0459] In another embodiment, the invention is concerned with compounds of the general formula XXXVII, wherein at least one of R^5ai, R^6ai, R^7ai and R^8ai are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0460] In another aspect of the invention, compounds are of the general formula XXXVIII

[0461] wherein R^4aj, R^5aj, R^6aj and R^7aj are independently selected from amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0462] wherein there may optionally be a covalent bond between the substituents R^4aj and R^5aj; and

[0463] wherein there may optionally be a covalent bond between the substituents R^6aj and R^7aj.

[0464] In one embodiment, the invention is concerned with compounds of the general formula XXXVIII, wherein there is a covalent bond between R^6aj and R^7aj.

[0465] In another embodiment, the invention is concerned with compounds of the general formula XXXVIII, wherein R^6aj, R^7aj and said covalent bond are selected so as to form a ring system selected from an optionally substituted piperedine, piperazine, morpholine and thiomorpholine.

[0466] In another embodiment, the invention is concerned with compounds of the general formula XXXVIII, wherein said ring system is selected from piperedine, piperazine, morpholine and thiomorpholine

[0467] In another embodiment, the invention is concerned with compounds of the general formula XXXVIII, wherein there is a covalent bond between R^4aj and R^5aj.

[0468] In another aspect of the invention, compounds are of the general formula XXXIX

[0469] wherein R^4ak, R^5ak, R^6ak and R^7ak are independently selected from amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that none of R^4ak and R^5ak are C(O)O isopropyl; and

[0470] wherein there may optionally be a covalent bond between the substituents R^4ak and R^5ak; with the proviso that R^4ak, R^5ak and the nitrogen to which they are bound do not form a substituted tetrazolyl moiety; and

[0471] wherein there may optionally be a covalent bond between the substituents R^6ak and R^7ak;

[0472] In one embodiment, the invention is concerned with compounds of the general formula XXXIX, wherein there is a covalent bond between R^6ak and R^7ak.

[0473] In another embodiment, the invention is concerned with compounds of the general formula XXXIX, wherein R^6ak, R^7ak and said covalent bond are selected so as to form a ring system selected from an optionally substituted piperedine, piperazine, morpholine and thiomorpholine.

[0474] In another embodiment, the invention is concerned with compounds of the general formula XXXIX, wherein said ring system is selected from piperedine, piperazine, morpholine and thiomorpholine

[0475] In another embodiment, the invention is concerned with compounds of the general formula XXXIX, wherein there is a covalent bond between R^4ak and R^5ak.

[0476] In another aspect of the invention, compounds are of the general formula XXXX

[0477] wherein R^4al and R^5al are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-0-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0478] wherein there may optionally be a covalent bond between R^4al and R^5al; with the proviso that R^4al and R^5al together with the nitrogen to which they are bound do not form 2,5-pyrrolidinedione or an annealed ring system comprising 3 or more rings; and

[0479] wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and NR^14al, CR^15alR^6al; and

[0480] R^6al, R^7al, R^8al, R^9al, R^10al, R^11al, R^12al, R^13al, R^14al, R^15al and R^16al are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; and

[0481] wherein there may optionally be a covalent bond between the substituents R^7al and R^8al; and

[0482] wherein there may optionally be a covalent bond between the substituents R^10al and a substituent selected from R^14al and R^5al.

[0483] In one embodiment, the invention is concerned with compounds of the general formula XXXX, wherein there is a covalent bond between the substituents R^4al and R^5al.

[0484] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein there is a covalent bond between the substituents R^7al and R^8al.

[0485] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein there is a covalent bond between R^10al and a substituent selected from R^14al or R^15al.

[0486] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein E is NR^14al.

[0487] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein R^14al is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0488] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein E is CR^15alR^16al.

[0489] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein R^16al is selected from F, Cl, C_1-6-alkyl, C_1-6alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0490] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein R^15al is hydrogen.

[0491] In another embodiment, the invention is concerned with compounds of the general formula XXXX, wherein at least one of R^6al, R^7al, R^8al, R^9al, R^10al, R^11al, R^12al and R^13al are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0492] In another aspect of the invention, compounds are of the general formula XXXXI

[0493] wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and NR^14am, CR^15amR^16am; and

[0494] wherein A^1am is N or CR^17am; A^2am is N or CR^18am; A^3am is N or CR^19am; A^4am is N or CR^20am; and

[0495] R^6am, R^7am, R^8am, R^9am, R^10am, R^11am, R^12am, R^13am, R^14am, R^15am, R^16am, R^17am, R^18am, R^19am and R^20am are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6 alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^17am and R^20am are not both hydroxy; and

[0496] wherein there may optionally be a covalent bond between R^18am and a substituent selected from R^17am and R^19am; and

[0497] wherein there may optionally be a covalent bond between the substituents R^10am and a substituent selected from R^14am and R^15am; and

[0498] wherein there may optionally be a covalent bond between the substituents R^7am and R^8am.

[0499] In one embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein there is a covalent bond between R^18am and a substituents selected from R^17am and R^19am.

[0500] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein there is a covalent bond between R^10am and a substituent selected from R^14am or R^15am.

[0501] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein E is NR^14am.

[0502] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein R^14am is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0503] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein E is CR^15amR^16am.

[0504] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein R^16am is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0505] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein R^15am is hydrogen.

[0506] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein there is a covalent bond between R^15am and R^16am.

[0507] In another embodiment, the invention is concerned with compounds of the general formula XXXXI, wherein at least one of R^6am, R^7am, R^8am, R^9am, R^10am, R^11am, R^12am and R^13am are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0508] In another aspect of the invention, compounds are of the general formula XXXXII

[0509] wherein E is selected from the group consisting of O, S, S(O), S(O)₂ and NR^17an, CR^18anR^19an; and

[0510] R^4an, R^5an, R^6an, R^7an, R^8an, R^9an, R^10an, R^11an, R^12an, R^13an, R^14an, R^15an, R^16an, R^17an, R^18an and R^19an are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl,-heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of the hydroxy, sulfanyl, amino, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, oxo, halogen, amino, cyano, nitro, sulfo, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, C_3-10-cycloalkyl, perhalomethyl and perhalomethoxy; with the proviso that R^4an is not methyl or phenyl; and

[0511] wherein there may optionally be a covalent bond between R^13an and a substituent selected from R^17an and R^18an; and

[0512] wherein there may optionally be a covalent bond between the substituents R^7an and R^8an.

[0513] In one embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein R^4an is a substituted heteroaryl.

[0514] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein said substituted heteroaryl is a substituted pyridine.

[0515] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein there is a covalent bond between the substituents R^7an and R^8an.

[0516] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein there is a covalent bond between R^13an and a substituents selected from R^17an and R^18an.

[0517] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein E is NR^17an.

[0518] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein E is CR^18anR^19an.

[0519] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein R^19an is selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0520] In another embodiment, the invention is concerned with compounds of the general formula XXXXII, wherein R^18an is hydrogen.

[0521] In another embodiment, the invention-is concerned with compounds of the general formula XXXXII, wherein at least one of R^5an, R^6an, R^7an, R^8an, R^9an, R^10an, R^11an, R^12an, R^13an, R^14an, R^15an and R^16an are selected from F, Cl, C_1-6-alkyl, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, hydroxy, amino and perhalomethyl.

[0522] In another aspect of the invention, compounds are of the general formula XXXXIII

[0523] wherein R^4ao is selected from hydrogen, hydroxy, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0524] wherein R^5ao, R^6ao, R^7ao, R^8ao, R^9ao, R^10ao, R^11ao and R^12ao are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy;

[0525] with the proviso that any one of R^6ao and R^8ao is not methyl; and with the further proviso that R^4ao, R^5ao, R^6ao, R^7ao and R^8ao are not all hydrogen; and

[0526] wherein there may optionally be a covalent bond beween R^4ao and R^6ao; and

[0527] wherein there may optionally be a covalent bond between R^7ao and R^8ao; and

[0528] wherein there may optionally be a covalent bond between R^9ao and R^10ao.

[0529] In one embodiment the invention is concerned with compounds of the general formula XXXXIII, wherein R^5ao, R^6ao, R^7ao and R^8ao are independently selected from hydrogen and fluor.

[0530] In another embodiment the invention is concerned with compounds of the general formula XXXXIII, wherein R^9ao, R^10ao, R^11ao and R^12ao are independently selected from hydrogen and fluor.

[0531] In another aspect of the invention, compounds are of the general formulae XXXXIVa-b

[0532] wherein R^1ap and R^2ap are independently selected from C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; with the proviso that if R^1ap and R^2ap are identical then they are not methyl or ethyl; and

[0533] wherein there may optionally be a covalent bond between the substituents R^1a and R^2ap; and

[0534] wherein R^5ap, R^6ap and R^7ap are independently selected from hydrogen and F; and

[0535] wherein R^4ap is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6 alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; with the proviso that R^4ap is not methyl.

[0536] In one embodiment the invention is concerned with compounds of the general formulae XXXXIVa-b, wherein R^1ap and R^2ap are not identical.

[0537] In another aspect of the invention, compounds are of the general formulae XXXXVa-b

[0538] wherein R^1aq and R^2aq are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; with the proviso that R^1aq and R^2aq are not both methyl; and

[0539] wherein there may optionally be a covalent bond between R^1aq and R^2aq; and

[0540] wherein R^3aq, R^4aq, R^5aq, R^6aq, R^7aq, R^8aq, R^9aq, R^10aq and R^11ao are indenpendently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0541] wherein there may optionally be a covalent bond between R^4aq and R^5aq; and

[0542] wherein R^3aq is selected from the group consisting of C(O), C(O)NH, CH₂, CH₂CH₂, CHF, CH₂CHF, CHFCH₂, NH, S(O)₂NH, NHS(O)₂, NHC(O), O, S, S(O), S(O)₂; and

[0543] wherein there may optionally be a covalent bond between two substituents selected from R^8aq, R^9aq, R^10aq and R^11ao.

[0544] In one embodiment the invention is concerned with compounds of the general formulae XXXXVa-b, wherein there is one covalent bond between the substituents R^1aq and R^2aq.

[0545] In another embodiment the invention is concerned with compounds of the general formulae XXXXVa-b, wherein R^4aq, R^5aq, R^6aq and R^7aq are independently selected from hydrogen and fluor.

[0546] In another embodiment the invention is concerned with compounds of the general formula XXXXVa-b, wherein R^3aq is selected from O, S, CH₂, CH₂CH₂, NH, NHC(O), C(O)NH, S(O)₂NH and NHS(O)₂.

[0547] In another aspect of the invention, compounds are of the general formula XXXXVI

[0548] wherein A^1ar is N or CR^10ar; and A^2ar is N or C-R^11ar; and A^3ar is N or CR^12ar; and

[0549] wherein R^1ar, R^2ar, R^3ar, R^4ar, R^5ar, R^6ar, R^7ar, R^8ar, R^9ar, R^10ar, R^11ar and R^12ar are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; with the proviso that if R^1ar and R^2ar are identical then they are not methyl or ethyl; and

[0550] wherein there may optionally be a covalent bond between R^1ar and R^2ar.

[0551] In one embodiment the invention is concerned with compounds of the general formula XXXXVI, wherein R^9ar is S(O)₂R^13ar or C(O)R^13ar; and wherein R^13ar is selected from hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-0-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy

[0552] In another embodiment the invention is concerned with compounds of the general formula XXXXVI, wherein R^1ar and R^2ar are not identical.

[0553] In another embodiment the invention is concerned with compounds of the general formula XXXXVI, wherein there is a covalent bond between the substituents R^1ar and R^2ar.

[0554] In another aspect of the invention, compounds are of the general formula XXXXVII

[0555] wherein R^1as, R^2as, R^3as, R^4as, R^5as, R^6as, R^7as R^8as and R^9as are independetly selected from hydrogen and fluor; and

[0556] wherein R^10as is selected from aryl and heteroaryl, which is optionally substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0557] wherein R^12as is selected from hydrogen, hydroxy, sulfanyl, sulfo, amino, cyano, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0558] wherein R^13as, R^14as, R^15as and R^16as are independently selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8 heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; with the proviso that R^12as, R^13as, R^14as, R^15as and R^16as are not all hydrogen; and

[0559] wherein there may optionally be a covalent bond between the substituents R^13as and R^14as.

[0560] In one embodiment the invention is concerned with compounds of the general formula XXXXVII, wherein R^13as, R^14as, R^15as and R^16as are independently selected from hydrogen and fluor.

[0561] In another aspect of the invention, compounds are of the general formula XXXXVIII

[0562] wherein R^5at, R^6at, R^7at, R^8at, R^9at, R^10at, R^11at, R^12at, R^13at, R^14at, R^15at, R^16at, R^17at and R^18at are independently selected from hydrogen and fluor; and

[0563] wherein R^4at is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6alkyl, C_2-6-alkenyl, perhalomethyl and perhalomethoxy; and

[0564] wherein R^19at is selected from hydrogen, hydroxy, sulfanyl, sulfo, halogen, amino, cyano, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl, and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, halogen, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl, wherein each of hydroxy, sulfanyl, sulfo, amino, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl may optionally be substituted with one or more substituents independently selected from hydroxy, sulfanyl, sulfo, oxo, fluor, iodine, amino, cyano, nitro, C_1-6-alkyl, C_2-6-alkenyl, aryl, heteroaryl, C_3-8-heterocyclyl and C_3-10-cycloalkyl; with the proviso that R^19at is not methoxy.

[0565] In one embodiment the invention is concerned with compounds of the general formula XXXXVIII, wherein R^5at, R^6at, R^7at R^8at, R^9at, R^10at R^11at, R^12at, R^13at R^14at, R^15at, R^16at, R^17at and R^18at are all hydrogen.

[0566] In another embodiment the invention is concerned with compounds of the general formula XXXXVIII, wherein R^4at is an optionally substituted aryl or heteroaryl.

[0567] In another embodiment, the invention is concerned with compounds of the general formulae I-XXXXVIII, wherein said compound comprises only one F.

[0568] In another embodiment, the invention is concerned with compounds of the general formulae I-XXXXVIII, wherein said compound comprises two F and preferably three F.

[0569] In another embodiment; the invention is concerned with compounds of the general formulae I-XXXXVIII, wherein said compound comprises a CF₃ moiety.

[0570] In another embodiment, the invention is concerned with compounds of the general formulae I-XXXXVIII, wherein said compound comprises a hydrophilic substituent selected from the group consisting of hydroxy, amino, C_1-6-alkoxy, C(O)NH₂, NHC(O)OH, S(O)₂NH₂, NHS(O)₂OH, NHC(O)R^1am, NHS(O)₂R^1am, N(R^1am)C(O)R^2am, N(R^1am)S(O)₂R^2am, wherein R^1am and R^2am are independently selected from C_1-6-alkyl.

[0571] In another embodiment, the invention is concerned with compounds of the general formulae I-XXXXVIII, wherein said compound comprises a moiety selected from the group consisting of

[0572] Examples of specific compounds of the invention are:

[0573] Methyl-phenyl-carbamic acid 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl ester,

[0574] Methyl-phenyl-carbamic acid 3-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl ester,

[0575] Methyl-phenyl-carbamic acid 4-(3,5-dichloro-pyridin-2-yloxy)-phenyl ester,

[0576] Methyl-phenyl-carbamic acid 4-(5-trifluoromethyl-pyridin-2-ylamino)-phenyl ester,

[0577] Methyl-phenyl-carbamic acid 4-(3,5-dichloro-pyridin-4-yloxy)-phenyl ester,

[0578] Methyl-phenyl-carbamic acid 4-(4-trifluoromethyl-phenoxy)-phenyl ester,

[0579] Methyl-phenyl-carbamic acid 4-(2-cyano-5-trifluoromethyl-pyridine-3-yloxy)-phenyl ester,

[0580] Methyl-phenyl-carbamic acid 2-benzenesulfonyl-4-(3-chloro-5-trifluoromethyl-pyridine-2-yloxy)-phenyl ester,Methyl-phenyl-carbamic acid 4-tert-butoxy-phenyl ester,Methyl-phenylcarbamic acid 3-(4-fluorobenzyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0581] Methyl-phenyl-carbamic acid 4-phenoxy-phenyl ester,

[0582] Methyl-phenyl-carbamic acid 4-(4-chlorobenzoyl)-phenyl ester,

[0583] Methyl-phenyl-carbamic acid 4-(3-chloro-5-trifluoromethyl)-pyridine-2-yloxy)-phenyl ester,

[0584] Methyl-phenyl-carbamic acid 4-4-(4-chloro-phenyl)-thiazol-2-yl-phenyl ester,

[0585] Methyl-phenyl-carbamic acid 4-pyrrol-1-yl-phenyl ester,

[0586] Methyl-phenyl-carbamic acid 4-imidazol-1-yl-phenyl ester,

[0587] Methyl-phenyl-carbamic acid 4-(3-chloro-5-trifluoromethyl)-pyridine-2-ylmethyl)-phenyl ester,

[0588] Methyl-phenyl-carbamic acid 4-trifluoromethylsulfanyl-phenyl ester,

[0589] Methyl-phenyl-carbamic acid 4-pentafluoroethyloxy-phenyl ester,

[0590] Methyl-phenyl-carbamic acid 4-benzyloxy-phenyl ester,

[0591] Methyl-phenyl-carbamic acid 4-benzyl-phenyl ester,

[0592] Methyl-phenyl-carbamic acid 4-cyano-biphenyl-4-yl-ester,

[0593] Methyl-phenyl-carbamic acid 4-bromo-biphenyl-4-yl-ester,

[0594] Methyl-phenyl-carbamic acid biphenyl-4-yl-ester,

[0595] Methyl-phenyl-carbamic acid 4-3-(4-chlorophenyl)-ureido-phenyl ester,

[0596] Methyl-phenyl-carbamic acid 4-(4-nitro-phenoxy)-phenyl ester,

[0597] Methyl-phenyl-carbamic acid 4-heptylsulfanyl-phenyl ester,

[0598] Methyl-phenyl-carbamic acid 4-butoxy-phenyl ester,

[0599] Methyl-phenyl-carbamic acid 4-(4-chloro-benzenesulfonyl)-phenyl ester,

[0600] Methyl-phenyl-carbamic acid 4-(4-chloromethyl-thiazol-2-yl)-phenyl ester,

[0601] Methyl-phenyl-carbamic acid 4-(4,4-dimethyl-2,6-dioxo-piperidin-1-yl)-phenyl ester, cis-Methyl-phenyl-carbamic Acid 4-(1,3-dioxo-octahydro-isoindol-2-yl)-phenyl ester,

[0602] Methyl-phenyl-carbamic acid 4-(cyclohexanecarbonyl-amino)-phenyl ester,

[0603] Methyl-phenyl-carbamic acid 4-(2-cyclohexyl-acetylamino)-phenyl ester, cis/trans-Methyl-phenyl-carbamic Acid 4-(4-tert-butyl-cyclohexanecarbonyl)-amino-phenyl ester, cis-Methyl-phenyl-carbamic Acid 4-(4-tert-butyl-cyclohexanecarbonyl)-amino-phenyl ester, trans-Methyl-phenyl-carbamic Acid 4-(4-tert-butyl-cyclohexanecarbonyl)-amino-phenyl ester,

[0604] Methyl-phenyl-carbamic acid 4-(3,3-dimethyl-butyrylamino)-phenyl ester,

[0605] Methyl-phenyl-carbamic acid 3-benzyl-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0606] Methyl-phenyl-carbamic acid 3-(3,4-dichloro-benzyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0607] Methyl-phenyl-carbamic acid 3-(2-chloro-6-fluoro-benzyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0608] Methyl-phenyl-carbamic acid 3-(2,6-dichloro-benzyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0609] Methyl-phenyl-carbamic acid 3-(2,6-dichloro-benzyl)-6-chloro-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0610] Methyl-phenyl-carbamic acid 6-chloro-3-(2-chloro-6-fluoro-benzyl)-4-n-propy-2-oxo-2H-chromen-7-yl ester,

[0611] Methyl-phenyl-carbamic acid 3-(4-methoxy-phenyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0612] Methyl-phenyl-carbamic acid 4-methyl-2-oxo-3-phenyl-2H-chromen-7-yl ester,

[0613] Methyl-phenyl-carbamic acid 3-(2,5-dimethoxy-phenyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0614] Methyl-phenyl-carbamic acid 3-(3,4-dimethoxy-phenyl)-4-methyl-2-oxo-2H-chromen-7-yl ester,

[0615] Methyl-phenyl-carbamic acid 4-pyrrolidine-1-yl-phenyl ester,

[0616] Methyl-phenyl-carbamic acid 4-piperidine-1-yl-phenyl ester,

[0617] Methyl-phenyl-carbamic acid 4-morpholine-1-yl-phenyl ester,

[0618] Methyl-phenyl-carbamic acid 4-(6-chloro-pyridine-3-carbonyl)-amino-phenyl ester,

[0619] Methyl-phenyl-carbamic acid 4-(6-chloro-pyridine-3-carbonyl)-amino-phenyl ester,

[0620] Methyl-phenyl-carbamic acid 4-(pyridine-2-carbonyl)-amino-phenyl ester,

[0621] 4-Chlor-phenyl-methyl-carbamic acid 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl ester,

[0622] 4-Chlor-phenyl-methyl-carbamic acid 4-(3,5-dichloro-pyridin-2-yloxy)-phenyl ester,

[0623] (4-Chloro-phenyl)-methyl-carbamic acid 4-(2-cyano-5-trifluoromethyl-pyridin-3-yloxy)-phenyl ester,

[0624] Ethyl-phenyl-carbamic acid 4-(5-trifluoromethyl-pyridin-2-yloxy)-phenyl ester,

[0625] Ethyl-phenyl-carbamic acid 4-(4-trifluoromethyl-phenoxy)-phenyl ester,

[0626] Methyl-phenyl-carbamic acid pyrazol-1-yl ester,

[0627] Methyl-phenyl-carbamic acid 4-bromo-pyrazol-1-yl ester,

[0628] Methyl-phenyl-carbamic acid 3,4,5-tribromo-pyrazol-1-yl ester,

[0629] Methyl-phenyl-carbamic acid 3-(4-methoxy-phenyl)-pyrazol-1-yl ester,

[0630] Methyl-phenyl-carbamic acid imidazol-1-yl ester,

[0631] Methyl-phenyl-carbamic acid 1,2,3triazol-1-yl ester,

[0632] Methyl-phenyl-carbamic acid 3-bromo-pyrazol-1-yl ester,

[0633] Methyl-phenyl-carbamic acid 5-bromo-pyrazol-1-yl ester,

[0634] Methyl-phenyl-carbamic acid 3-chloro-pyrazol-1-yl ester,

[0635] Methyl-phenyl-carbamic acid 4-chloro-pyrazol-1-yl ester,

[0636] Methyl-phenyl-carbamic acid 5-chloro-pyrazol-1-yl ester,

[0637] Methyl-phenyl-carbamic acid 4-iodo-pyrazol-1-yl ester,

[0638] Methyl-phenyl-carbamic acid 5-iodo-pyrazol-1-yl ester,

[0639] Methyl-phenyl-carbamic acid 3-methyl-pyrazol-1-yl ester,

[0640] Methyl-phenyl-carbamic acid 4-methyl-pyrazol-1-yl ester,

[0641] Methyl-phenyl-carbamic acid 5-methyl-pyrazol-1-yl ester,

[0642] Methyl-phenyl-carbamic acid 4-(4-methoxy-phenyl)-pyrazol-1-yl ester,

[0643] Methyl-phenyl-carbamic acid 5-(4-methoxy-phenyl)-pyrazol-1-yl ester,

[0644] Methyl-phenyl-carbamic acid 3-(2-methoxy-phenyl)-pyrazol-1-yl ester,

[0645] Methyl-phenyl-carbamic acid 3-(4-nitro-phenyl)-pyrazol-1-yl ester,

[0646] Methyl-phenyl-carbamic acid 3-(2-nitro-phenyl)-pyrazol-1-yl ester,

[0647] Methyl-phenyl-carbamic acid 3-pyridin-2-yl-pyrazol-1-yl ester,

[0648] Methyl-phenyl-carbamic acid 4-pyridin-2-yl-pyrazol-1-yl ester,

[0649] Methyl-phenyl-carbamic acid 3-(2-fluoro-phenyl)-pyrazol-1-yl ester,

[0650] Methyl-phenyl-carbamic acid 4-(2-fluoro-phenyl)-pyrazol-1-yl ester,

[0651] Methyl-phenyl-carbamic acid 5-(2-fluoro-phenyl)-pyrazol-1-yl ester,

[0652] Methyl-phenyl-carbamic acid 3-phenylsulfanyl-pyrazol-1-yl ester,

[0653] Methyl-phenyl-carbamic acid 4-phenylsulfanyl-pyrazol-1-yl ester,

[0654] Methyl-phenyl-carbamic acid 5-phenylsulfanyl-pyrazol-1-yl ester,

[0655] Methyl-phenyl-carbamic acid 4-thiophen-3-yl-pyrazol-1-yl ester,

[0656] Methyl-phenyl-carbamic acid 3-thiophen-2-yl-pyrazol-1-yl ester,

[0657] Methyl-phenyl-carbamic acid 4-thiophen-2-yl-pyrazol-1-yl ester,

[0658] Methyl-phenyl-carbamic acid 5-thiophen-2-yl-pyrazol-1-yl ester,

[0659] Methyl-phenyl-carbamic acid 2-chloro-imidazol-1-yl ester,

[0660] Methyl-phenyl-carbamic acid 2-bromo-imidazol-1-yl ester,

[0661] Methyl-phenyl-carbamic acid 2-iodo-imidazol-1-yl ester,

[0662] Methyl-phenyl-carbamic acid 2-methyl-imidazol-1-yl ester,

[0663] Methyl-phenyl-carbamic acid 2-phenylsulfanyl-imidazol-1-yl ester,

[0664] Methyl-phenyl-carbamic acid 2-(4-methoxy-phenyl)-imidazol-1-yl ester,

[0665] Methyl-phenyl-carbamic acid 2-(4-fluoro-phenyl)-imidazol-1-yl ester,

[0666] Methyl-phenyl-carbamic acid 2-thiophen-2-yl-imidazol-1-yl ester,

[0667] Methyl-phenyl-carbamic acid 2-pyridin-2-yl-imidazol-1-yl ester,

[0668] Methyl-phenyl-carbamic acid 2,5-dichloro-imidazol-1-yl ester,

[0669] Methyl-phenyl-carbamic acid 4-bromo-2,5-dichloro-imidazol-1-yl ester,

[0670] 4-(Methyl-phenyl-carbamoyloxy)-benzoic acid 2,5-dioxo-pyrrolidin-1-yl ester,

[0671] Methyl-phenyl-carbamic acid 4-(1,3,5-trimethyl-1H-pyrazol-4-ylmethyl)-phenyl ester,

[0672] Methyl-phenyl-carbamic acid 4-(2-cyano-ethyl)-phenyl ester,

[0673] Methyl-phenyl-carbamic acid 4-(1,2,3,4thiatriazol-5-ylamino)-phenyl ester,

[0674] Methyl-phenyl-carbamic acid 4-pentyl-phenyl ester,

[0675] Methyl-phenyl-carbamic acid 4-(2-methoxy-ethyl)-phenyl ester,

[0676] Methyl-phenyl-carbamic acid 4-acetyl-phenyl ester,

[0677] Methyl-phenyl-carbamic acid pyridin-4-yl ester,

[0678] Methyl-phenyl-carbamic acid pyridin-3-yl ester,

[0679] Methyl-phenyl-carbamic acid 6-methyl-pyridin-3-yl ester,

[0680] Methyl-phenyl-carbamic acid isoquinolin-1-yl ester,

[0681] Methyl-phenyl-carbamic acid 3-phenoxy-phenyl ester,

[0682] Methyl-phenyl-carbamic acid 3-acetyl-phenyl ester,

[0683] Methyl-phenyl-carbamic acid 4-acetyl-2-carbamoyl-phenyl ester,

[0684] Methyl-phenyl-carbamic acid 4-acetyl-3-methyl-phenyl ester,

[0685] Methyl-phenyl-carbamic acid 1-oxo-indan-4-yl ester,

[0686] Methyl-phenyl-carbamic acid benzothiazol-2-yl ester,

[0687] Methyl-phenyl-carbamic acid 5-oxo-5,6,7,8-tetrahydro-naphthalen-2-yl ester,

[0688] Methyl-phenyl-carbamic acid benzodisoxazol-3-yl ester,

[0689] Methyl-phenyl-carbamic acid pyridin-2-yl ester,

[0690] Methyl-phenyl-carbamic acid 1-(methyl-phenyl-carbamoyl)-1H-benzimidazol-2-yl ester,

[0691] Methyl-phenyl-carbamic acid 4-(pyridine-3-carbonyl)-amino-phenyl ester,

[0692] Methyl-phenyl-carbamic acid 4-(3-pyridin-3-yl-acryloyl)-phenyl ester,

[0693] Methyl-phenyl-carbamic acid 4-3-(3,4,5-trimethoxy-phenyl)-acryloyl-phenyl ester,

[0694] Methyl-phenyl-carbamic acid 4-diethylcarbamoyl-2-methoxy-phenyl ester,

[0695] Methyl-phenyl-carbamic acid 3-phenylcarbamoyl-phenyl ester,

[0696] Methyl-phenyl-carbamic acid quinolin-7-yl ester,

[0697] Methyl-phenyl-carbamic acid 4-(4-methyl-piperazine-1-carbonyl)-phenyl ester,

[0698] Methyl-phenyl-carbamic acid 3-acetylamino-phenyl ester,

[0699] Methyl-phenyl-carbamic acid 4-benzoyl-phenyl ester,

[0700] Methyl-phenyl-carbamic acid biphenyl-3-yl ester,

[0701] Methyl-phenyl-carbamic acid 1H-indol-4-yl ester,

[0702] Methyl-phenyl-carbamic acid 5,6,7,8-tetrahydro-naphthalen-1-yl ester,

[0703] Methyl-phenyl-carbamic acid 5-oxo-5,6,7,8-tetrahydro-naphthalen-1-yl ester,

[0704] Methyl-phenyl-carbamic acid 1,3-dioxo-1,3-dihydro-isobenzofuran-4-yl ester,

[0705] Methyl-phenyl-carbamic acid 4-(5-chloro-pyridin-2-yloxy)-phenyl ester,

[0706] Methyl-phenyl-carbamic acid 4-morpholin-4-yl-phenyl ester,

[0707] Methyl-phenyl-carbamic acid 4-(5,6-dichloro-1,3-dioxo-1,3-dihydro-isoindol-2-yl)-phenyl ester, Methyl-phenyl-carbamic acid 4-(2-phenoxy-acetylamino)-phenyl ester,

[0708] Methyl-phenyl-carbamic acid 4-2-(4-chloro-phenyl)-ethyl-phenyl ester,

[0709] Methyl-phenyl-carbamic acid 4-(pyridine-2-carbonyl)-amino-phenyl ester,

[0710] Methyl-phenyl-carbamic acid 4-methyl-(thiophene-2-carbonyl)-amino-phenyl ester,

[0711] Methyl-phenyl-carbamic acid 4-butyrylamino-phenyl ester,

[0712] Methyl-phenyl-carbamic acid 4-(4,6-dimethyl-pyrimidin-2-ylsulfanyl)-phenyl ester,

[0713] Methyl-phenyl-carbamic acid 4-methanesulfonyl-phenyl ester,

[0714] Methyl-phenyl-carbamic acid 4-2-(3-oxo-1-, 2, 3, 4-tetrahydro-quinoxalin-2-yl)-acetylamino-phenyl ester,

[0715] Methyl-phenyl-carbamic acid 4-phenylacetyl-phenyl ester,

[0716] Methyl-phenyl-carbamic acid 4-4-(methyl-phenyl-carbamoyloxy)-2-oxo-1,2-dihydro-quinoline-3-carbonyl-amino-phenyl ester,

[0717] Methyl-phenyl-carbamic acid 4-(4-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carbonyl)-amino-phenyl ester,

[0718] Methyl-phenyl-carbamic acid 4-(4-hydroxy-benzyl)-phenyl ester Methyl-phenyl-carbamic acid 4-(4-trifluoromethyl-benzylcarbamoyl)-phenyl ester,

[0719] Methyl-phenyl-carbamic acid 4-(butyl-methyl-carbamoyl)-phenyl ester,

[0720] Methyl-phenyl-carbamic acid 4-(methyl-phenethyl-carbamoyl)-phenyl ester,

[0721] Methyl-phenyl-carbamic acid 4-(pyridin-2-ylmethyl)-carbamoyl-phenyl ester,

[0722] Methyl-phenyl-carbamic acid 4-(2-pyridin-2-yl-ethylcarbamoyl)-phenyl ester,

[0723] Methyl-phenyl-carbamic acid 4-(2-phenylamino-ethylcarbamoyl)-phenyl ester,

[0724] Methyl-phenyl-carbamic acid 4-(3-methyl-butylcarbamoyl)-phenyl ester,

[0725] Methyl-phenyl-carbamic acid 4-(3,3-dimethyl-butylcarbamoyl)-phenyl ester,

[0726] Methyl-phenyl-carbamic acid 4-(tetrahydro-furan-2-ylmethyl)-carbamoyl-phenyl ester,

[0727] Methyl-phenyl-carbamic acid 4-cyclohexylcarbamoyl-phenyl ester,

[0728] Methyl-phenyl-carbamic acid 4-cyclopropylcarbamoyl-phenyl ester,

[0729] Methyl-phenyl-carbamic acid 4-(cyclohexylmethyl-carbamoyl)-phenyl ester,

[0730] Methyl-phenyl-carbamic acid 5-nitro-pyridin-2-yl ester,

[0731] Methyl-phenyl-carbamic acid pyrimidin-2-yl ester,

[0732] Methyl-phenyl-carbamic acid 7-chloro-quinolin-4-yl ester,

[0733] Methyl-phenyl-carbamic acid quinolin-4-yl ester,

[0734] Methyl-phenyl-carbamic acid 5-methyl-isoxazol-3-yl ester,

[0735] Methyl-phenyl-carbamic acid quinoxalin-2-yl ester,

[0736] Methyl-phenyl-carbamic acid 4-methyl-quinolin-2-yl ester,

[0737] Methyl-phenyl-carbamic acid 3-methyl-quinoxalin-2-yl ester,

[0738] Methyl-phenyl-carbamic acid 4,6-dimethyl-pyrimidin-2-yl ester,

[0739] Methyl-phenyl-carbamic acid isoquinolin-6-yl ester,

[0740] Methyl-phenyl-carbamic acid quinolin-2-yl ester,

[0741] Methyl-phenyl-carbamic acid isoquinolin-3-yl ester,

[0742] Methyl-phenyl-carbamic acid 4-trifluoromethyl-pyrimidin-2-yl ester,

[0743] Methyl-phenyl-carbamic acid 3-nitro-pyridin-2-yl ester,

[0744] Methyl-phenyl-carbamic acid 5-chloro-pyridin-2-yl ester,

[0745] Methyl-phenyl-carbamic acid 5-(2-nitro-phenyl)-pyrimidin-2-yl ester,

[0746] Methyl-phenyl-carbamic acid 5-trifluoromethyl-pyridin-2-yl ester,

[0747] Methyl-phenyl-carbamic acid 3-chloro-5-trifluoromethyl-pyridin-2-yl ester,

[0748] Methyl-phenyl-carbamic acid 5-nitro-3-trifluoromethyl-pyridin-2-yl ester,

[0749] Methyl-phenyl-carbamic acid 4,5-dichloro-pyridazin-3-yl ester,

[0750] Methyl-phenyl-carbamic acid 5-benzoylamino-pyridin-2-yl ester,

[0751] Methyl-phenyl-carbamic acid 5-(cyclohexanecarbonyl-amino)-pyridin-2-yl ester,

[0752] Methyl-phenyl-carbamic acid 4,4-dimethyl-2,6-dioxo-3,4,5,6-tetrahydro-2H-1,3bipyridinyl-6-yl ester,

[0753] Methyl-phenyl-carbamic acid 5-(2,2-dimethyl-propionylamino)-pyridin-2-yl ester,

[0754] Methyl-phenyl-carbamic acid 5-(2-cyclohexyl-acetylamino)-pyridin-2-yl ester,

[0755] Methyl-phenyl-carbamic acid 5-(4-methoxy-phenoxy)-pyrimidin-2-yl ester,

[0756] Methyl-phenyl-carbamic acid 5-(3,4-dichloro-phenoxy)-pyrimidin-2-yl ester,

[0757] Methyl-phenyl-carbamic acid 6-pyridin-2-ylmethyl-pyridazin-3-yl ester,

[0758] Methyl-phenyl-carbamic acid 6-(4-methoxy-benzyl)-pyridazin-3-yl ester,

[0759] Methyl-phenyl-carbamic acid 6-(2,4-dichloro-benzyl)-pyridazin-3-yl ester,

[0760] Methyl-phenyl-carbamic acid 4-iodo-pyrazol-1-yl ester,

[0761] Methyl-phenyl-carbamic acid benzotriazol-1-yl ester,