Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

CROSS-REFERENCE TO RELATED APPLICATION

REFERENCE TO SEQUENCE LISTING SUBMITTED ELECTRONICALLY

FIELD OF THE INVENTION

BACKGROUND OF THE INVENTION

SUMMARY OF THE INVENTION

[0017]
and include tautomers, isomers, and esters of said compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, tautomers, isomers, and esters, wherein each of R, R¹, X, Y, Z, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁸, R¹⁹ and n are selected independently and wherein:
R is selected from alkyl, aryl, heteroaryl, cycloalkyl, aryl-fused cycloalkyl, heteroaryl-fused cycloalkyl, cycloalkenyl, aryl-fused cycloalkenyl, heteroaryl-fused cycloalkenyl, heterocycloalkyl, aryl-fused heterocycloalkyl, and heteroaryl-fused heterocycloalkyl,

• • [0018] wherein each of said alkyl, said aryl, said heteroaryl, said cycloalkyl, said aryl-fused cycloalkyl, said heteroaryl-fused cycloalkyl, said cycloalkenyl, said aryl-fused cycloalkenyl, said heteroaryl-fused cycloalkenyl, said heterocycloalkyl, said aryl-fused heterocycloalkyl, and said heteroaryl-fused heterocycloalkyl, is unsubstituted or optionally independently substituted with from one to five substituents, which are the same or different, each substituent being independently selected from halo, —OH, —CN, oxo, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, heteroalkyl, heterohaloalkyl, -alkyl-OH, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, heteroarylalkyl-, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, heterocycloalkylalkyl-, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)-cycloalkyl, —C(O)-heterocycloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —C(O)O-haloalkyl, —C(O)O-cycloalkyl, —C(O)O-heterocycloalkyl, —OC(O)-alkyl, —OC(O)-haloalkyl, —OC(O)-cycloalkyl, —OC(O)-heterocycloalkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —OC(O)NH₂, —CO(O)NHR¹⁰, —CO(O)NR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NH₂, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, —S(O)₂R¹⁰, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl;
    X and Y are each independently selected from N and CH, with the proviso that at least one of X or Y is N;
    Z═H, halo, —OH, —SH, —CN, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, heterohaloalkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-heteroaryl, cycloalkyl, aryl, heteroaryl, —NH₂, —NHR¹², and —NR¹²R¹³;
    R¹ is selected from H, halo, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, heteroaryl, —OH, —O-alkyl, —O-aryl, —O-heteroalkyl, —O-heteroaryl, —SH, —S-alkyl, —S-aryl, —S-heteroalkyl, —S-heteroaryl, —NH₂, —NHR¹⁴, —NR¹⁴R¹⁵, —NO₂, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰;
    R² (when R² is not joined with R⁹) is selected from H and alkyl;
    n=0, 1, or 2;
    R³ is selected from H, -alkyl, alkenyl, alkynyl, aryl, heteroaryl, and cycloalkyl,
  • [0019] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, and said cycloalkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁴ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0020] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁵ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0021] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
  • [0022] or, alternatively, R⁴ and R⁵ are taken together with the carbon atom to which they are shown attached to form a 3- to 7-membered, saturated or partially unsaturated, spirocycloalkyl ring containing from 0 to 3 spiro ring heteroatoms selected from O, N, and S;
    R⁶ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0023] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    or, alternatively, R⁵ and R⁶ are taken together to form a double bond;
    R⁷ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0024] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —CO(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
  • [0025] or, alternatively, R⁶ and R⁷ are taken together with the carbon atom to which they are shown attached to form a 3- to 7-membered, saturated or partially unsaturated, spirocycloalkyl ring containing from 0 to 3 spiro ring heteroatoms selected from O, N, and S;
    R⁸ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0026] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —CO(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to five substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-cycloalkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —O(C)O—N(R¹⁰)R¹¹, —O(C)O—NHR¹¹, —O(C)O—NH₂, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, —S(O)₂R¹⁰, —SR¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, —CN, —NH₂, —NHR¹⁶, and —NR¹⁶R¹⁷, —N(R¹⁰)S(O)₂R¹⁰, —NHS(O)₂R¹⁰, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁹ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0027] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to five substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-cycloalkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —O(C)O—N(R¹⁰)R¹¹, —O(C)O—NHR¹¹, —O(C)O—NH₂, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, —S(O)₂R¹⁰, —SR¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, —CN, —NH₂, —NHR¹⁶, and —NR¹⁸R¹⁷, —N(R¹⁰)S(O)₂R¹⁰, —NHS(O)₂R¹⁰, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
  • [0028] or, alternatively, R⁸ and R⁹ are taken together with the carbon atom to which they are shown attached to form a 3- to 7-membered, saturated or partially unsaturated, spirocycloalkyl ring containing from 0 to 3 spiro ring heteroatoms selected from O, N, and S;
    each R¹⁸ (when present) is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0029] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    each R¹⁹ (when present) is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NO₂, —NHR¹⁰, —NR¹⁰R¹¹, —C(O)OH, —C(O)OR¹⁰, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —S(O)NHR¹⁰, —S(O)NR¹⁰R¹¹, —S(O)R¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, and —S(O)₂R¹⁰,
  • [0030] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, haloalkyl, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
  • [0031] or, alternatively, n is 1 and R¹⁸ and R¹⁹ are taken together with the carbon atom to which they are attached to form a 3- to 7-membered, saturated or partially unsaturated, spirocycloalkyl ring containing from 0 to 3 spiro ring heteroatoms selected from O, N, and S;

[0033]

• • [0034] wherein R²⁰ and R²¹ are each independently selected from H, alkyl, and heteroalkyl and wherein R⁵ and R⁶ are defined above, with the proviso that
  • [0035] when R⁴ and R⁷ form a moiety (1C), then R⁵ and R⁶ are not taken together to form a double bond;

[0037]

[0040]

DETAILED DESCRIPTION OF THE INVENTION

[0078]
and includes tautomers, isomers, and esters of such compounds, and pharmaceutically acceptable salts, solvates, and prodrugs of said compounds, tautomers, isomers, and esters, wherein each of R, R¹, X, Y, Z, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁸, R¹⁹ and n are selected independently and wherein:
R, R¹, R², X, Y, Z, and n are as defined in Formula (I);
R³ is selected from H, -alkyl, -alkenyl, alkynyl, aryl, heteroaryl, and cycloalkyl,

• • [0079] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, and said cycloalkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁴ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0080] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁵ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0081] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl,
    R⁶ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0082] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁷ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0083] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
  • [0084] or, alternatively, R⁶ and R⁷ are taken together with the carbon atom to which they are shown attached to form a 3- to 7-membered, saturated or partially unsaturated, spirocycloalkyl ring containing from 0 to 3 spiro ring heteroatoms selected from O, N, and S;
    R⁸ is selected from is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0085] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to five substituents, which can be the same or different, each substituent being independently selected from halo, —OH, —NH₂, —NHR¹⁶, —NR¹⁶R¹⁷, —NHS(O)₂R¹⁰, —N(R¹⁰)S(O)₂R¹⁰, alkyl, —O-alkyl, —S-alkyl, —S(O)₂-alkyl, —S(O)₂NH₂, —S(O)₂NHalkyl, —S(O)₂N(alkyl)₂, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —O(C)O—NHR¹⁰, —O(C)O—N(R¹⁰)R¹¹, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, —S(O)₂R¹⁰, —SR¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, —CN, —NH₂, —NHR¹⁶, and —NR¹⁶R¹⁷, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    R⁹ is selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0086] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to five substituents, which can be the same or different, each substituent being independently selected from halo, —OH, —NH₂, —NHR¹⁶, —NR¹⁶R¹⁷, —NHS(O)₂R¹⁰, —N(R¹⁰)S(O)₂R¹⁰, alkyl, —O-alkyl, —S-alkyl, —S(O)₂-alkyl, —S(O)₂NH₂, —S(O)₂NHalkyl, —S(O)₂N(alkyl)₂, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —O(C)O—NHR¹⁰, —O(C)O—N(R¹⁰)R¹¹, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, —S(O)₂R¹⁰, —SR¹⁰, —S(O)₂NHR¹⁰, —S(O)₂NR¹⁰R¹¹, —CN, —NH₂, —NHR¹⁶, and —NR¹⁶R¹⁷, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    each R¹⁸ (when present) is independently selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0087] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;
    each R¹⁹ (when present) is independently selected from H, —OH, halo, -alkyl, -alkenyl, alkynyl, azido, aryl, heteroaryl, —O-alkyl, —O-alkenyl, —OC(O)-alkyl, —SH, —S-alkyl, —NH₂, —NHalkyl, and —N(alkyl)₂,
  • [0088] wherein each of said -alkyl, said -alkenyl, said alkynyl, said aryl, said heteroaryl, said —O-alkyl, said —O-alkenyl, said —OC(O)-alkyl, and said —S-alkyl, is unsubstituted or optionally independently substituted with from one to three substituents, which can be the same or different, each substituent being independently selected from halo, —OH, alkyl, —O-alkyl, —O-alkenyl, —O-haloalkyl, —O-haloalkenyl, —OC(O)-alkyl, —OC(O)-alkenyl, —OC(O)-haloalkyl, —OC(O)-haloalkenyl, —C(O)O-alkyl, —C(O)O-alkenyl, —C(O)O-haloalkyl, —C(O)O-haloalkenyl, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocycloalkyl, and heterocycloalkenyl;

[0104]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R⁴, R⁵, R⁷, and R⁹ is selected independently and defined in Formula (I).

[0121]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0123]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0125]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0127]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0129]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0131]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0133]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0135]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0137]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0139]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0141]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently defined in Formula (I).

[0143]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0145]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0147]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0149]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently defined in Formula (I).

[0151]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0153]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², n, and R¹⁶ is selected independently defined in Formula (I).

[0155]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and R¹⁶ is selected independently and defined in Formula (I).

[0157]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², n, R¹⁶, and R¹⁷ is selected independently and defined in Formula (I).

[0159]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R¹⁶, and R¹⁷ is selected independently and defined in Formula (I).

[0161]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and is selected independently and defined in Formula (I), and wherein CB is a moiety selected from the group consisting of:

[0162]
wherein each R¹⁰ is independently selected from the group consisting of methyl, ethyl, and cyclopropyl.

[0169]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, and R_d is independently selected from H, halo, —OH, —CN, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl; and

[0172]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R³, R⁴, R⁷, R⁸, R⁹, R¹⁸, R¹⁹, and n is selected independently and defined in Formula (I).

[0174]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and R⁹ is selected independently and defined in Formula (I).

[0178]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0180]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0182]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0184]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0186]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R³, R⁵, R⁶, R⁸, R⁹, R¹⁸, R¹⁹, R²⁰, R²¹, and n is selected independently and defined in Formula (I), with the proviso that R⁵ and R⁶ are not taken together to form a double bond.

[0188]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R⁹, R²⁰, and R²¹ is selected independently and defined in Formula (I).

[0191]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0193]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0195]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², and n is selected independently and defined in Formula (I).

[0197]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently defined in Formula (I).

[0199]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R³, R⁵, R⁶, R⁸, R⁹, R¹⁸, and R¹⁹, and n is selected independently and defined in Formula (I).

[0201]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R⁹, and n is selected independently and defined in Formula (I).

[0205]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0207]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, and R² is selected independently and defined in Formula (I).

[0209]
and includes pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R², R³, R⁵, R⁶, R⁸, R⁹, R¹⁸, and R¹⁹, and n is selected independently and defined in Formula (I).

[0211]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, Z, R³, R⁴, R⁵, R⁶, R⁷, and R⁸ is selected independently and defined in Formula (I).

[0213]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, and Z is selected independently and wherein R, R¹, X, Y, and Z are defined in Formula (I).

[0215]
and include pharmaceutically acceptable salts, esters, prodrugs, or isomers of said compounds, wherein each of R, R¹, X, Y, and Z is selected independently and wherein R, R¹, X, Y, and Z are defined in Formula (I).

[0244]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl.

[0246]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —ON, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl.

[0248]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl.

[0250]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl.

[0252]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —ON, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl.

[0254]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein:
Ra is selected from the group consisting of H, methyl, ethyl, n-propyl, cyclopropyl, and cyclobutyl;
Rb is selected from the group consisting of methyl, ethyl, n-propyl, —O-methyl, and —O-ethyl;
Rc is selected from the group consisting of H, methyl, ethyl, and cyclopropyl; and
Rd is selected from the group consisting of H, methyl, and ethyl.

[0316]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each R_aa is independently selected from haloalkyl (non-limiting examples of which include —CH₂F, —CHF₂, —CF₃, etc.), R_ab is selected from OH, OAc, and —O-alkyl (non-limiting examples of which include —O-Me, —O-Et, —O-n-Pr, —O-i-Pr, —O-n-Bu, —O-i-Bu, and —O-t-Bu), —O-haloalkyl (non-limiting examples of which include —O—CH₂F, —O—CHF₂, and —O—CF₃), —NH₂, —NHalkyl, and —N(alkyl)₂.

[0318]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein R_af is selected from H and acetyl. It shall be understood that positional isomers of the heteroatoms shown in the moieties above are also contemplated. Such positional isomers include semmetric positional isomers such as

[0319]
Additional non-limiting examples of R¹ when R¹ is —NHR¹⁴ include:

[0320]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl, and wherein each R_ad and each R_ae is independently selected from alkyl and haloalkyl.

[0322]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each R_aa is independently selected from haloalkyl (non-limiting examples of which include —CH₂F, —CHF₂, —CF₃, etc.), R_ab is selected from OH, OAc, and —O-alkyl (non-limiting examples of which include —O-Me, —O-Et, —O-n-Pr, —O-i-Pr, —O-n-Bu, —O-i-Bu, and —O-t-Bu), —O-haloalkyl (non-limiting examples of which include —O—CH₂F, —O—CHF₂, and —O—CF₃), —NH₂, —NHalkyl, and —N(alkyl)₂.
Additional non-limiting examples of R¹ when R¹ is —NR¹⁴R¹⁵ include:

[0323]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein R_af is selected from H and acetyl.

[0325]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl, and wherein each R_ad and each R_ae is independently selected from alkyl and haloalkyl.

[0327]
wherein X is selected from O, NH, and NMe.

[0342]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl, and

[0344]
wherein the wavy line represents the point of attachment of R to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl;

[0346]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each R_aa is independently selected from haloalkyl (non-limiting examples of which include —CH₂F, —CHF₂, —CF₃, etc.), R_ab is selected from OH, OAc, and —O-alkyl (non-limiting examples of which include —O-Me, —O-Et, —O-n-Pr, —O-i-Pr, —O-n-Bu, —O-i-Bu, and —O-t-Bu), —O-haloalkyl (non-limiting examples of which include —O—CH₂F, —O—CHF₂, and —O—CF₃), —NH₂, —NHalkyl, and —N(alkyl)₂,

[0347]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein R_af is selected from H and acetyl,

[0348]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, cycloalkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl, and wherein each R_ad is independently selected from alkyl and haloalkyl,

[0349]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each R_aa is independently selected from haloalkyl (non-limiting examples of which include —CH₂F, —CHF₂, —CF₃, etc.), R_ab is selected from OH, OAc, and —O-alkyl (non-limiting examples of which include —O-Me, —O-Et, —O-n-Pr, —O-i-Pr, —O-n-Bu, —O-i-Bu, and —O-t-Bu), —O-haloalkyl (non-limiting examples of which include —O—CH₂F, —O—CHF₂, and —O—CF₃), —NH₂, —NHalkyl, and —N(alkyl)₂,

[0350]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein R_af is selected from H and acetyl,

[0351]
wherein the wavy line represents the point of attachment of R¹ to the rest of the molecule, and wherein each of R_a, R_b, R_c, R_d, and R_e, is independently selected from H, halo, —OH, —CN, alkyl, haloalkyl, -alkyl-OH, heteroalkyl, heterohaloalkyl, —O-alkyl, —O-haloalkyl, —O-alkyl-OH, aryl, —O-aryl, —S-aryl, —O-alkyl-aryl, —S-alkyl-aryl, heteroaryl, —O-heteroaryl, —S-heteroaryl, —O-alkyl-heteroaryl, —S-alkyl-heteroaryl, heterocycloalkyl, —C(O)-alkyl, —C(O)-haloalkyl, —C(O)H, —C(O)OH, —C(O)O-alkyl, —OC(O)-alkyl, —C(O)NH₂, —C(O)NHR¹⁰, —C(O)NR¹⁰R¹¹, —C(O)ONH₂, —C(O)ONHR¹⁰, —C(O)ONR¹⁰R¹¹, —NH₂, —NHR¹⁰, —NR¹⁰R¹¹, —NO₂, substituted aryl, and substituted heteroaryl, wherein each of said substituted aryl and said substituted heteroaryl independently contains from one to three substituents, which may be the same or different, each substituent being independently selected from halo, alkyl, —O-alkyl, and —C(O)Oalkyl, and wherein each R_ad is independently selected from alkyl and haloalkyl, and

[0352]
wherein X is selected from O, NH, and NMe; and

• • [0353] Z is selected from the group consisting of H, halo, —OH, —SH, —CN, alkyl, alkenyl, alkynyl, heteroalkyl, haloalkyl, heterohaloalkyl, —S-alkyl, —O-alkyl, —O-aryl, —O-heteroaryl, cycloalkyl, aryl, heteroaryl, —NH₂, —NHR¹², and —NR¹²R¹³.

DEFINITIONS

[0369]
is para-phenylene.

[0375]

[0379]

[0381]

[0383]

[0388]

[0429]

• • [0430] As used herein, the term “composition” is intended to encompass a product comprising the specified ingredients in the specified amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts.

[0432]
means containing both

[0433]

[0434] The wavy line , as used herein, indicates a point of attachment to the rest of the compound. For example, each wavy line in the following structure:

[0435]
indicates a point of attachment to the core structure, as described herein.

[0437]

• • [0438] indicate that the indicated line (bond) may be attached to any of the substitutable ring carbon atoms.
  • [0439] “Oxo” is defined as a oxygen atom that is double bonded to a ring carbon in a cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, or other ring described herein, e.g.,

[0440]

• • [0441] In this specification, where there are multiple oxygen and/or sulfur atoms in a ring system, there cannot be any adjacent oxygen and/or sulfur present in said ring system.
  • [0442] It is noted that the carbon atoms for compounds of the invention may be replaced with 1 to 3 silicon atoms so long as all valency requirements are satisfied.
  • [0443] As well known in the art, a bond drawn from a particular atom wherein no moiety is depicted at the terminal end of the bond indicates a methyl group bound through that bond to the atom, unless stated otherwise. For example:

[0444]

PREPARATIVE EXAMPLES

[0487]

Example 5

Procedure A-1

Example 5

(1R,2S,3R,5R)-3[(2-amino-6-chloro-5-phenyl-4-pyrimidinyl)amino]-5-hydroxymethyl)-1,2-cyclopentanol

[0495]

Example 9

Procedure A-2

Example 9

[0501]

Example 21

[0505]

Example 101

Procedure A

[0515]

Example 102

Procedure B

[0517]

Example 105

Procedure C

[0519]

Example 108

Procedure D

[0522]

Example 110

Procedure E

[0524]

Example 115

Procedure F

[0528]

Examples 120 and 121

Procedure G

[0532]

Example 124

Procedure H

[0540]

Example 125

Procedure I

[0545]

Example 112

Procedure J

[0547]

Example 403 and 404

Procedure K

[0550]

Example 308

Procedure L

[0556]

[0557]

Example 310

Procedure M

[0565]

Example 312

Procedure N

[0572]

[0573]

Example 418

Procedure O

[0588]

Intermediate 516

Procedure P

[0590]

Example 516

Procedure Q

[0595]

Procedure R

[0598]

Example 321

Procedure S

[0600]

Example 324

Procedure T

[0607]

Example 328 and 329

Procedure U

[0615]

Example 332 and 327

Procedure V

[0622]

Example 335

Procedure W

[0631]

Example 333 and 338

Procedure X

[0635]

Example 524

Procedure Y

[0640]
Step 1:

Example 523

Procedure Z

[0648]
Step 1:

Example 535

Procedure Z1

[0656]
Step 1:

Example 542

Procedure Z2

[0664]
Step 1:

Examples 248 and 252

Procedure Z3

[0668]

Example 1015

Procedure Z10

[0673]

Example 1019

Procedure Z11

[0677]

Example 1057

Procedure Z13

[0682]

Example 1058

Procedure Z14

[0686]

Example 1104

Procedure Z-15

[0688]

Example 1120

Procedure Z16

[0694]

Example 1132

Procedure Z17

[0701]

Example 1133

Procedure Z18

[0715]

Example 1134

Procedure Z19

[0719]

Example 1136

Procedure Z20

[0724]

Example 1211

Procedure Z21

[0731]

Example 1219

Procedure Z21

[0734]

Example 1223

Procedure Z22

[0737]

Example 1227

Procedure Z23

[0739]

Example 1238

Procedure Z24

[0742]

Example 1240

Procedure Z25

[0748]

Example 1244

Procedure Z26

[0751]

Example 1251

Procedure Z27

[0754]

Example 1252

Procedure Z28

[0757]

Example 1301

Procedure Z29

[0762]

Example 1302

Procedure Z30

[0764]

Example 1315

Procedure Z31

[0766]
Step 1:

Example 1318

Procedure Z32

[0770]
Step 1:

Example 1321

Procedure Z33

[0775]
Step 1:

Example 1327

Procedure Z34

[0778]

Example 1328

Procedure Z35

[0783]
Step 1:

Example 1330

Procedure Z36

[0786]
Step 1:

Example 1331

Procedure Z37

[0789]
Step 1:

Example 1343

Procedure Z38

[0792]
Step 1:

Example 1350

Procedure Z39

[0796]
Step 1:

Example 1367

Procedure Z40

[0806]
Step 1:

Example 1366

Procedure Z41

[0817]
Step 1:

Example 1374

Procedure Z42

[0827]
Step 1:

Example 1383

Procedure Z43

[0833]
Step 1:

Example 1396

Procedure Z44

[0841]

Example 1400

Procedure Z45

[0846]
Step 1:

Example 1402

Procedure Z46

[0852]
Step 1:

Example 1398

Procedure Z47

[0855]
Step 1:

Examples 1392 and 1393

Procedure Z48

[0860]
Step 1:

Example 1528

Procedure Z49

[0865]
Step 1:

Example 1538

Procedure Z50

[0872]

Example 1539

Procedure Z51

[0876]
Step 1: Compound 1539c was synthesized from 1539a and 1539b using Procedure Z49.
Step 2:

Example 1610

Procedure Z56

[0881]

Example 1616

Procedure Z57

[0888]

Example 1617

Procedure Z58

[0894]

Example 1628

Procedure Z59

[0900]

Example 1630

Procedure Z60

[0904]

Example 1632

Procedure Z61

[0907]

Example 1637

Procedure Z62

[0911]

Examples 1636 and 1640

Procedure Z63

[0914]

Example 1643

Procedure Z64

[0918]

Example 1653

Procedure Z66

[0922]

Example 1701

Procedure Z67

[0925]
Step 1:

Example 1702

Procedure Z68

[0932]
Step 1:

Example 1703

Procedure Z69

[0934]
Step 1:

Example 1901

Procedure Z70

[0940]

Example 1902

Procedure Z71

[0942]

Example 1905

Procedure Z72

[0944]

Example 1907

Procedure Z73

[0947]

Example 1915

Procedure Z74

[0950]

Example 1916

Procedure Z75

[0953]

Example 1917

Procedure Z76

[0956]

Example 31

Procedure A-3

[0959]

Example 48

Procedure A-4

[0971]

Example 53

Procedure A-5

[0975]

Example 54

[0983]

Example 55

Procedure A-6

[0985]

Example 43

Procedure A-7

[0988]

[0992]

TABLE I
		EC90		LC-
Compd		(μM)		MS
#	Structure	range	NMR data	(M + H)+	Procedure
5		C	(DMSO-d6): δ 0.91 (m, 1H), 1.82 (m, 1H), 2.18 (m, 1H), 3.26 (t, 2H, J = 4.8 Hz), 3.55 (m, 2H), 4.37 (m, 2H), 4.51 (d, 1H, J = 4.0 Hz), 5.37 (d, 1H, J = 7.8 Hz), 6.48 (bs, 2H), 7.21 (d, 2H, J = 8.1), 7.43 (m, 3H).	351.1	A-1
6		—	(DMSO-d6): δ 1.02 (dt, 1H, J = 8.5, 13.0 Hz), 1.77-1.90 (m, 1H), 2.00-2.12 (m, 1H), 3.22-3.39 (m, 2H + H2O), 2.59- 2.72 (m, 2H), 4.30- 4.43 (m, 2H), 4.47- 4.57 (m (app quart), 2H, OHs), 6.61 (d, 1H, J = 7.9 Hz, NH), 6.87 (hr s, 2H, NH2), 7.12 (d, 1H, J = 1.0 Hz), 7.33 (dd, 1H, J = 4.8, 8.3 Hz), 7.99 (dm, 1H, J = 8.3 Hz), 8.51 (dd, 1H, J = 1.3, 4.7 Hz).	392.2 (Cl pattern)	A-2
7		—	(DMSO-d6): δ 1.01 (dt, 1H, J = 8.9, 13.0 Hz), 1.77-1.89 (m, 1H), 2.00-2.12 (m, 1H), 3.22-3.39 (m, 2H), 2.59-2.71 (m, 2H), 4.30-4.43 (m, 2H), 4.46-4.55 (m, 72H, OHs), 6.58 (d, 1H, J = 7.9 Hz, NH), 6.86 (br s, 2H, NH2), 6.99 (s, 1H), 7.35 (dd, 1H, J = 4.8, 7.6 Hz), 8.10 (dd, 1H, J = 1.6, 7.6 Hz), 8.29 (dd, 1H, J = 1.7, 4.8 Hz).	392.1 (Cl pattern)	A-2
8		B	(DMSO-d6) δ 0.96- 1.05 (m, 1H), 1.78- 1.87 (m, 1H), 2.01- 2.11 (m, 1H), 3.27- 3.34 (m, 2H coincident with H2O), 3.59-3.68 (m, 2H), 4.30-4.40 (m, 2H), 4.48-4.53 (m, 2H), 6.56 (d, 1 H, J = 7.8 Hz), 6.87 (s, 2 H), 7.08 (d, 1 H, J = 0.7 Hz), 7.65 (d, 1 H, J = 5.6 Hz).	392.16	A-2
9		A	(DMSO-d6) δ 0.98- 1.08 (m, 1H), 1.75- 1.95 (m, 1H), 2.04- 2.14 (m, 1H), 3.27- 3.35 (m, 2H), 3.62- 3.68 (m, 2H), 4.30- 4.40 (m, 1H), 6.72 (d, 1 H, J = 7.8 Hz), 7.02 (s, 2 H), 7.27 (d, 1 H, J = 20.66 Hz), 7.65 (dd, 1 H, J = 0.4, 5.6 Hz), 8.52 (d, 1 H, J = 25.7 Hz), 9.20 (s, 1 H).	392.20	A-2
10		A	(DMSO-d6) δ 0.98- 1.08 (m. 1H), 1.78- 1.90 (m, 1H), 2.04- 2.14 (m, 1H), 3.26- 3.36 (m, 2H), 3.62- 3.69 (m, 2H), 3.87 (s, 3H), 4.30-4.37 (m, 1H, coincident with H2O), 6.58 (d, 1 H, J = 7.9 Hz, D2O exchangeable), 6.84- 6.94 (br s, 2 H, D2O exchangeable), 6.93 (s, 1 H), 7.01 (s, 1 H), 8.56 (s, 1H).	518.11	A-2
11		A	(DMSO-d6) δ 1.00- 1.07 (m, 1H), 1.78- 1.90 (m, 1H), 2.02- 2.14 (m, 1H), 3.28- 3.50 (m, 2H), 3.63- 3.70 (m, 2H), 3.93 (s, 3H), 4.30-4.37 (m, 1H, coincident with H2O), 6.84 (d, 1 H, J = 7.6 Hz, D2O exchangeable), 7.04 (s, 1 H), 7.16 (s, 1 H), 8.61 (s, 1 H).	422.14	A-2
12		B	(DMSO-d6) δ 1.05- 1.12 (m, 1H), 1.84- 1.93 (m, 1H), 2.14- 2.24 (m, 1H), 2.56 (s, 3H), 3.11 (s, 6H), 3.34-3.38 (m, 2H, coincident with HDO), 3.63-3.76 (m, 2H), 3.85 (s, 3H), 4.24-4.30 (m, 1H), 4.40 (d, 1H, J = 5.2 Hz, D2O exchangeable), 4.49- 4.53 (m, 2H, D2O exchangeable), 6.70 (d, 1 H, J = 7.1 Hz, D2O exchangeable), 6.80 (d, 1 H, J = 0.6 Hz), 6.89 (s, 1 H).	464.22	A-2
13		C	(DMSO-d6) δ 1.06- 1.16 (m, 1H), 1.85- 1.95 (m, 1H), 2.16- 2.26 (m, 1H), 2.64 (s, 3H), 3.12 (s, 6H), 3.31-3.37 (m, 2H), 3.66-3.75 (m, 2H), 3.95 (s, 3H), 4.25- 4.30 (m, 1H), 6.80 (d, 1 H, J = 7.0 Hz, D2O exchangeable), 7.03-7.10 (m, 2H).		A-2
14		A	(DMSO-d6) δ 0.98- 1.09 (m, 1H), 1.80- 1.89 (m, 1H), 2.05- 2.17 (m, 1H), 2.58 (s, 3H), 3.29-3.35 (m, 2H), 3.62-3.70 (m, 2H), 3.87 (s, 3H), 4.29-4.37 (m, 1H), 6.66 (d, 1 H, J = 7.6 H), 6.73-7.07 (br s, 2H), 6.87 (s, 1H), 6.93 (s, 1H).	436.1	A-2
15		A	(DMSO-d6) δ 0.98- 1.15 (m, 1H), 1.82- 1.93 (m, 1H), 2.10- 2.25 (m, 1H), 2.59 (s, 3H), 2.80 (s, 3H), 3.28-3.38 (m, 2H), 3.63-3.76 (m, 2H), 3.88 (s, 3H), 4.27- 4.34 (m, 1H), 6.62- 6.82 (m, 1 H, D2O exchangeable), 6.89 (s, 1H), 6.94 (s, 1H), 7.24-7.46 (br s, 1H, D2O exchangeable).	450.21	A-2
16		B	(CD3OD) δ 1.18-1.27 (m, 1H), 2.01-2.10 (m, 1H), 2.30-2.40 (m, 1H), 2.62 (s, 3H), 3.42- 3.56 (m, 2H), 3.80- 3.89 (m, 2H), 4.38- 4.48 (m, 1H), 6.98 (br s, 1H), 7.20 (d, 1H, J = 8.4 Hz), 7.81 (d, 1H, J = 8.8 Hz).	406.1	A-2
17		A	(DMSO-d6) δ 1.05- 1.12 (m, 1H), 1.82- 1.94 (m, 1H), 2.12 (s, 3H), 2.10-2.28 (m, 1H), 2.56 (s, 3H), 2.80 (d, 3H, J = 4.7 Hz), 3.34-3.39 (m, 2H, coincident with H2O), 3.64-3.72 (m, 2H), 3.84 (s, 3H), 4.24-4.30 (m, 1H), 4.33-4.36 (m, 1H, D2O exchangeable), 4.48-4.52 (m, 1H, D2O exchangeable), 4.55-4.60 (m, 1H, D2O exchangeable), 6.20-6.31 (br s, 1H, D2O exchangeable), 6.76 (s, 1H), 6.77 (s, 1H), 6.75-6.88 (br s, 1H, D2O exchangeable).	430.2	A-2
18		A	(DMSO-d6) δ 1.02- 1.16 (m, 1H), 1.81- 1.93 (m, 1H), 2.09- 2.25 (m, 1H), 2.58 (s, 3H), 3.27 (s, 3H), 3.31-3.45 (m, 2H), 3.40-3.53 (m, 4H), 3.64-3.77 (m, 2H), 3.88 (s, 3H), 4.24- 4.37 (m, 1H), 4.47- 4.9 (br s, H2O under which are the hydroxyls), 6.61-6.85 (m, 1H, D2O exchangeable), 6.88 (s, 1 H), 6.94 (s, 1H), 7.29-7.57 (m, 1H, D2O exchangeable).	494.2	A-2
19		A	(DMSO-d6): δ 1.02- 1.18 (m, 1H), 1.81- 1.95 (m, 1H), 2.03- 2.23 (m, 1H), 2.57 (s, 3H), 3.27-3.42 (m, 2H), 3.61-3.78 (m, 2H), 3.86 (s, 3H), 4.03-4.17 m, 1H), 4.20-4.37 (m, 2H, visible upon D2O exchange), 6.84 (s, 1H), 6.80-6.95 (m, 1H, D2O exchangeable), 6.95 (s, 1H), 7.92-8.13 (m, 1H, D2O exchangeable).	518.2	A-2
20		A	(DMSO-d6) δ 1.02- 1.17 (m, 1H), 1.32 (t, 3H, J = 6.9 Hz), 1.83- 1.94 (m, 1H), 2.07- 2.22 (m, 1H), 2.55 (s, 3H), 3.33-3.4 (m, 2H, visible upon D2O exchange), 3.69-3.83 (m, 2H, 2H visible upon D2O exchange), 4.16-4.15 (m, 1H), 4.20-4.31 (m, 2H), 4.28 (q, 2H, J = 7.0 Hz), 6.80 (s, 1H), 6.83- 6.93 (m, 1H, D2O exchangeable), 6.93 (s, 1H), 7.92-8.12 (m, 1H, D2O exchangeable).	532.2	A-2
21		A	(DMSO-d6) δ 1.02- 1.16 (m, 1H), 1.33 (t, 3H, J = 7.1 Hz), 1.81- 1.93 (m, 1H), 2.09- 2.25 (m, 1H), 2.56 (s, 3H), 3.27 (s, 3H), 3.30-3.37 (m, 2H), 3.39-3.50 (m, 4H), 3.64-3.77 (m, 2H), 3.88 (s, 3H), 4.24- 4.35 (m, 3H), 4.58- 5.6 (hr s, H2O under which are the hydroxyls), 6.60-6.81 (m, 1H, D2O exchangeable), 6.84 (s, 1H), 6.92 (s, 1H), 7.25-7.55 (m, 1H, D2O exchangeable).	508.2	A-2
22		A	(DMSO-d6) δ 1.05- 1.18 (m, 1H), 1.84- 1.98 (m, 1H), 2.12- 2.28 (m, 1H), 3.33- 3.43 (m, 2H), 3.63- 3.80 (m, 2H), 3.88 (s, 3H), 4.02-4.16 (hr s, 1H), 4.20-4.31 (hr s, 2H), 4.34-4.43 (m, 1H, D2O exchangeable), 4.48- 4.56 (m, 2H D2O exchangeable), 6.78- 6.90 (m, 1H, D2O exchangeable), 6.97 (s, 1 H), 7.01 (s, 1 H), 7.90-8.12 (m, 1H, D2O exchangeable), 8.49 (s, 1 H).	504.1	A-2
24		0.02	(DMSO-d6) δ 1.00- 1.15 (m, 1H), 1.19- 1.34 (m, 1H), 1.35 (t, 3H, J = 7.0 Hz), 1.80-1.98 (m, 2H), 2.31 (br s, 3H), 2.61 (s, 3H), 3.17 (s, 1H), 3.25-3.39 (m, 2H), 3.58-3.69 (m, 1H), 3.76 (app t, 1H, J = 5.9 Hz), 4.28-4.40 (m, 2Hz), 7.02 (s, 1H), 7.13 (s, 1H), 7.70 (d, 1H, J = 3.1 Hz), 7.79 (d, 1H, J = 3.1 Hz) 8.09 (app d, 1H, J = 2.9 Hz), 8.60-8.72 (br s, 1H).	527.2	A-2
25		0.8	(DMSO-d6) δ 1.10- 1.26 (m, 1H), 1.84- 1.97 (m, 1H), 2.04- 2.18 (m, 1H), 2.24 (s, 3H), 3.31 (s, 3H), 3.25-3.39 (m, 2H), 3.49-3.58 (m, 2H), 3.56-3.70 (m, 3H), 3.79 (app t, 1H, J = 5.9 Hz), 3.90 (s, 3H), 4.35-4.49 (m, 1H, 7.11 (s, 1H), 7.13 (s, 1H), 7.91-8.04 (m, 2H), 8.59 (s, 1H), 13.43 (br s, 1H).	460.2	A-2
26		0.5	(DMSO-d6) δ 0.89 (t, 3H, J = 7.4 Hz), 1.11-1.26 (m, 2H), 1.36 (t, 3H, J = 7.0 Hz), 1.41 (s, 6H), 1.82 (app q, 2H, J = 7.6 Hz), 1.84-1.97 (m, 1H), 2.08-2.21 (m, 1H), 2.26 (s, 3H), 2.62 (s, 3H), 3.29- 3.40 (m, 2H), 3.69 (app t, 1H, J = 5.0 Hz), 3.81 (app t, 1H, J = 5.6 Hz), 4.28- 4.42 (m, 3H), 7.02 (s, 1H), 7.12 (s, 1H), 7.98 (d, 1H, J = 7.8 Hz), 8.01 (s, 1H), 13.37 (br s, 1H).	500.3	A-2
27		0.35	(DMSO-d6) δ 0.95 (s, 9H), 1.12-1.28 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.86-1.98 (m, 1H), 2.07-2.20 (m, 1H), 2.27 (s, 3H), 2.59 (s, 3H), 3.24- 3.41 (m, 4H), 3.67 (app t, 1H, J = 5.0 Hz), 3.80 (app t, 1H, J = 5.8 Hz), 4.31 (q, 2H, J = 7.0 Hz), 4.30-4.44 (m, 2H), 6.94 (s, 1H), 7.08 (s, 1H), 7.96 (d, 1H, J = 7.3 Hz), 8.18-8.28 (m, 1H), 13.33 (br s, 1H).	500.3	A-2
28		0.45	(DMSO-d6) δ 1.09- 1.27 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.85-1.98 (m, 1H), 2.07-2.20 (m, 1H), 2.27 (s, 3H), 2.60 (s, 3H), 2.97 (d, 3H, J = 4.5 Hz), 3.27-3.41 (m, 2H), 3.67 (app t, 1H, J = 5.0 Hz), 3.80 (app t, 1H, J = 5.8 Hz), 6.96 (s, 1H), 7.08 (s, 1H), 7.78- 7.88 (m, 1H), 7.93- 8.03 (m, 1H), 13.30 (br s, 1H).	444.2	A-2
29		0.1	(DMSO-d6) δ 1.11- 1.28 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), (m, 1H), 2.05-2.20 (m, 1H), 2.31 (s, 3H), 2.60 (s, 3H), 3.27-3.41 (m, 2H), 3.66 (app t, 1H, J = 5.0 Hz), 3.79 (app t, 1H, J = 5.8 Hz), 6.97 (s, 1H), 7.12 (s, 1H), 8.12-8.22 (m, 1H), 8.41-8.54 (m, 1H).	512.2	A-2
30		0.14	(DMSO-d6) δ 0.28- 0.34 (m, 2H), 0.46- 0.55 (m, 2H), 1.08- 1.26 (m, 2H), 1.34 (t, 3H, J = 7.0 Hz), 1.85-1.98 (m, 1H), 2.05-2.20 (m, 1H), 2.27 (s, 3H), 2.59 (s, 3H), 3.27-3.40 (m, 5H), 4.31 (q, 3H, J = 7.0 Hz), 4.35-4.48 (m, 1H), 6.96 (s, 1H), 7.08 (s, 1H), 7.93- 8.02 (m, 1H), 7.96- 8.08 (m, 1H), 13.18 (br s, 1H).	484.3	A-2
31		A	(DMSO-d6) δ 1.10- 1.25 (m, 1H), 1.35 (t, 3H, J = 7.0 Hz), 1.84-1.98 (m, 1H), 2.05-2.18 (m, 1H), 2.27 (br s, 3H), 2.60 (s, 3H), 3.17 (s, 1H), 3.25-3.40 (6H), 3.48- 3.71 (m, 6H), 3.79 (app t, 1H, J = 5.9 Hz), 4.32 (q, 2H, J = 7.0 Hz), 4.37-4.50 (m, 1H), 6.98 (s, 1H), 7.10 (s, 1H), 7.90- 8.07 (m, 2H, D2O exchangeable).	488.2	A-3
32		0.95	(DMSO-d6) δ 1.10- 1.25 (m, 1H), 1.23 (d, 3H, J = 2.3 Hz), 1.26 (d, 3H, J = 2.3 Hz), 1.35 (t, 3H, J = 7.0 Hz), 1.85-1.98 (m, 1H), 2.07-2.21 (m, 1H), 2.26 (s, 3H), 2.60 (s, 3H), 3.27- 3.40 (m, 2H), 3.68 (app t. 1H, J = 4.9 Hz), 3.82 (app t, 1H, J = 6.0 Hz), 4.10- 4.24 (m, 1H), 4.32 (q, 3H, J = 7.0 Hz), 4.32-4.48 (m, 1H), 6.98 (s, 1H), 7.09 (s, 1H), 7.93-8.09 (m, 2H), 13.21 (brs, 1H).	472.3	A-2
33		C	(DMSO-d6) δ 1.13- 1.28 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.86-1.98 (m, 1H), 2.04-2.18 (m, 1H), 2.33 (s, 3H), 2.60 (s, 3H), 3.28-3.40 (m, 2H), 3.69 (app t, 1H, J = 4.9 Hz). 3.82 (app t, 1H, J = 5.9 Hz), 6.96 (s, 1H), 7.13 (s, 1H), 7.19 (t, 1H, J = 7.4 Hz), 7.42 (t, 2H, J = 7.9 Hz), 7.67 (d, 2H, J = 7.6 Hz), 8.21 (app d, 1H, J = 7.6 Hz), 10.52 (s, 1H).	506.3	A-2
34		0.1	(DMSO-d6) δ 0.99 (t, 3H, J = 7.4 Hz), 1.12-1.25 (m, 1H), 1.75 (hex, 2H, J = 7.3 Hz), 1.86-1.99 (m, 1H), 2.07-2.20 (m, 1H), 2.31 (s, 3H), 2.60 (s, 3H), 3.28- 3.40 (m, 2H), 3.67 (app t, 1H, J = 5.0 Hz), 3.79 (app t, 1H, J = 5.9 Hz), 6.99 (s, 1H), 7.12 (s, 1H), 8.12-8.22 (m, 1H), 8.42-8.54 (m, 1H), 13.63 (br s, 1H).	526.2	A-2
35		0.1	(DMSO-d6) δ 0.99) t, 3H, J = 7.4 Hz), 1.12-1.24 (m, 1H), 1.78 (hex, 2H, J = 7.2 Hz), 1.87-1.99 (m, 1H), 2.07-2.30 (m, 1H), 2.28 (s, 3H), 2.60 (s, 3H), 3.31 (s, 3H), 3.28-3.40 (m. 2H), 3.51-3.60 (m, 1H), 3.58-3.66 (m, 1H), 3.68 (app t, 1H, J = 4.8 Hz), 4.24 (app t, 2H, J = 6.4 Hz), 4.38-4.48 (m, 1H), 6.99 (s, 1H), 7.10 (s, 1H), 7.89-8.04 (m, 2H), 13.34 (br s, 1H).	502.3	A-2
36		0.01	(DMSO-d6) δ 1.04- 1.14 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.84-2.01 (m, 1H), 2.28 (s, 3H), 2.59 (s, 3H), 3.31-3.40 (app d. 2H, J = 4.7 Hz), 3.66 (app t, 1H, J = 4.8 Hz), 3.74 (s, 6H), 3.78 (app t, 1H, J = 5.7 Hz), 6.40-6.43 (m, 1H), 6.57 (s, 1H), 6.58 (s, 1H), 6.96 (s, 1H), 7.08 (s, 1H), 7.99 (app d, 1H, J = 7.2 Hz), 8.44-8.53 (m, 1H), 13.39 (br s, 1H).	580.3	A-2
37		0.3	(DMSO-d6) δ 1.08- 1.24 (m, 1H), 1.30 (s, 3H) 1.32 (s, 3H), 1.85-1.96 (m, 1H), 2.06-2.20 (m 1H), 2.28 (s, 3H), 2.60 (s, 3H), 3.28-3.40 (m, 2H), 3.31 (s, 3H), 3.50-3.58 (m, 2H), 3.58-3.65 (m, 2H), 3.67 (app t, 1H, J = 4.8 Hz), 3.80 (app t, 1H, J = 5.7 Hz), 4.35-3.48 (m, 1H), 5.22 (quint, 1H, J = 6.1 Hz), 6.97 (s, 1H), 7.09 (s, 1H), 7.89- 8.04 (m, 2H), 13.35 (br s, 1H).	502.3	A-2
38		0.25	(DMSO-d6) δ 0.28- 0.35 (m, 2H), 0.47- 0.55 (m, 2H), 0.99 (t, 3H, J = 7.4 Hz), 1.06-1.26 (m, 2H), 1.75 (hex, 2H, J = 1.3 Hz), 1.85-1.97 (m, 1H), 2.06-2.20 (m, 1H), 2.27 (s, 3H), 2.60 (s, 3H), 3.28- 3.41 (m, 4H), 3.67 (app t, 1H, J = 4.9 Hz), 3.80 (app t, 1H, J = 5.6 Hz), 4.22 (t, 2H, J = 6.7 Hz), 4.36-4.47 (m, 1H), 6.97 (s, 1H), 7.08 (s, 1H), 7.91-8.01 (m, 1H), 8.03-8.12 (m, 1H), 13.30 (br s, 1H).	498.3	A-2
39		0.1	(DMSO-d6) δ 0.29- 0.36 (m, 2H), 0.48- 0.57 (m, 2H), 1.08- 1.26 (m, 2H), 1.31 (s, 3H), 1.33 (s, 3H), 1.87-1.99 (m, 1H), 2.07-2.20 (m, 1H), 2.28 (s, 3H), 2.61 (s, 3H), 3.28-3.41 (m, 4H), 3.68 (app t, 1H, J = 4.9 Hz), 3.80 (app t, 1H, J = 5.8 Hz), 5.20 (quint, 1H, J = 6.1 Hz), 6.99 (s, 1H), 7.09 (s, 1H), 7.91- 8.01 (m, 1H), 8.04- 8.15 (m, 1H), 13.40 (br s, 1H).	498.3	A-2
40		0.15	(DMSO-d6) δ 0.90- 1.02 (m, 1H), 1.33 (t, 3H, J = 7.0 Hz), 1.50 (d, 3H, J = 6.9 Hz), 1.60-1.74 (m, 1H), 1.81-1.95 (m, 1H), 2.25 (s, 3H), 2.28 (s, 3H), 2.57 (s, 3H), 3.31 (d, 2H, J = 5.3 Hz), 3.65 (app t, 1H, J = 4.8 Hz), 3.76 (app t, 1H, J = 5.7 Hz), 5.01-5.14 (m, 1H), 6.95 (s, 1H), 7.05 (s, 1H), 7.17 (d, 2H, J = 7.9 Hz), 7.31 (d, 2H, J = 8.0 Hz), 7.98 (app d, 1H, J = 7.6 Hz), 8.63-8.72 (m, 1H), 13.24 (br s, 1H).	548.3	A-2
41		0.2	(DMSO-d6) δ 0.23- 0.59 (m, 4H), 0.99- 1.13 (m, 1H), 1.12- 1.28 (m, 1H), 1.29 (d, 3H, J = 6.6 Hz), 1.34 (t, 3H, J = 7.0 Hz), 1.84-1.97 (m, 1H), 2.02-2.18 (m, 1H), 2.26 (s, 3H), 2.60 (s, 3H), 3.28-3.40 (m, 2H), 3.55-3.67 (m, 1H), 3.66 (app t, 1H, J = 4.9 Hz), 3.79 (app t, 1H, J = 5.9 Hz), 6.96 (s, 1H), 7.08 (s, 1H), 7.90-7.99 (m, 1H), 8.06-8.16 (m, 1H), 13.17 (br s, 1H).	499.3	A-2
42		0.3	(DMSO-d6) δ 0.28- 0.39 (m, 4H), 0.47- 0.61 (m, 4H), 1.08- 1.32 (m, 3H), 1.85- 1.98 (m, 1H), 2.05- 2.20 (m, 1H), 2.27 (s, 3H), 2.59 (s, 3H), 3.28-3.40 (m, 4H), 3.67 (app t, 1H, J = 4.9 Hz), 3.79 (app t, 1H, J = 5.8 Hz), 4.12 (d, 2H, J = 7.0 Hz), 6.98 (s, 1H), 7.09 (s, 1H), 7.92-8.01 (m, 1H), 8.03-8.13 (m, 1H), 13.35 (br s, 1H).	510.2	A-2
43		C	(DMSO-d6) δ 0.29- 0.36 (m, 2H), 0.48- 0.56 (m, 2H), 1.08- 1.30 (m, 2H), 1.86- 1.99 (m, 1H), 2.06- 2.21 (m, 1H), 2.30 (s, 3H), 2.71 (s, 3H), 3.28-3.41 (m, 4H), 3.68 (app t, 1H, J = 4.9 Hz), 3.80 (app t, 1H, J = 5.9 Hz), 7.15-7.20 (m, 1H), 7.21 (s, 1H), 7.60 (dd, 1H, J = 0.9, 5.1 Hz), 7.78-7.82 (m, 1H), 7.96-8.05 (m, 1H), 8.03-8.13 (m, 2H), 8.10 (s, 1H), 13.31 (br s, 1H).	522.2	A-7
44		>25	(DMSO-d6) δ 0.29- 0.33 (m, 2H), 0.47- 0.53 (m, 2H), 0.91 (t, 6H, J = 7.4 Hz), 1.08-1.40 (m, 2H), 1.59-1.74 (m, 4H), 1.90-2.00 (m, 1H), 2.08-2.18 (m, 1H), 2.27 (s, 3H), 2.59 (s, 3H), 3.27-3.39 (m, 4H), 3.61-3.72 (m, 1H), 4.37-4.44 (m, 1H), 4.90-4.95 (m, 1H), 6.99 (s, 1H), 7.07 (s, 1H), 7.90- 8.07 (m, 2H, D2O exchangeable).		A-3, A-4
45		>25	(DMSO-d6) δ 0.21- 0.22 (m, 2H), 0.39- 0.41 (m, 2H), 1.00 (s, 9H), 1.86-1.95 (m, 1H), 2.11 (s, 3H), 3.10-3.19 (m, 2H). 3.61-3.72 (m, 2H), 4.27-4.44 (m, 2H), 4.51-4.52 (m, 2H), 6.10-6.29 (bs, 1H), 6.76 (s, 2H), 6.86- 7.04 (m, 3H).		A-3, A-4
46		0.85	(CD3OD) δ 1.03 (s, 9H), 1.22-1.35 (m, 1H), 2.05-2.15 (m, 1H), 2.32 (s, 3H), 2.35-2.46 (m, 1H), 2.65 (s, 3H), 3.40- 3.47 (m, 2H), 3.49- 3.53 (m, 2H), 3.87- 3.89 (m, 2H), 4.56- 4.59 (m, 1H), 6.98 (s, 1H), 7.03 (s, 1H).	555.3	A-3, A-4
47		0.4	(CD3OD) δ 0.35-0.40 (m, 2H), 0.50-0.65 (m, 2H), 1.22-1.35 (m, 1H), 2.05-2.15 (m, 2H), 2.05-2.18 (m, 1H), 2.36 (s, 3H), 2.75 (s, 3H), 3.40- 3.57 (m, 4H), 3.89-3.99 (m, 2H), 4.55-4.65 (m, 1H), 7.21 (s, 1H), 7.80 (s, 1H).	538.2	A-3, A-4
48		>25	(DMSO-d6) δ 0.91 (t, 6H, J = 7.5 Hz), 1.10-1.20 (m, 1H), 1.59-1.74 (m, 4H), 1.87-2.00 (m, 1H), 2.08-2.18 (m, 1H), 2.26 (s, 3H), 2.58 (s, 3H), 3.30 (s, 3H), 3.50-3.79 (m, 4H), 4.90-4.95 (m, 1H), 6.92 (s, 1H), 7.04 (s, 1H), 7.85-7.99 (m, 2H, D2O exchangeable).	530.3	A-3, A-4
49		>25	(DMSO-d6) δ 1.11 (s, 9H), 1.28-1.36 (m, 1H), 1.10-1.20 (m, 1H), 2.05-2.15 (m, 1H), 2.35 (s, 3H), 2.77 (s, 3H), 3.41 (s, 1H), 3.51 (m, 1H), 3.60-3.65 (m, 3H), 3.71-3.80 (m, 1H), 3.90 (m, 2H), 4.55- 4.62 (m, 1H), 7.23 (s, 1H), 7.28 (s, 1H).		A-3, A-4
50		0.05	(DMSO-d6) δ 1.40.- 1.12 (m, 1H), 1.33 (t, 3H, J = 7.0 Hz), 1.90-1.99 (m, 1H), 1.97-2.07 (m, 1H), 2.25 (s, 3H), 3.30- 3.40 (m, 2H), 3.67 (t, 1H, J = 5.1 Hz), 3.81 (app t, 1H, J = 6.4 Hz), 4.31 (q, 2H, J = 7.0 Hz), 4.64-4.72 (m, 1H), 4.78-4.85 (m, 1H), 6.93 (s, 1H), 7.05 (s, 1H). 7.10- 7.19 (m, 2H), 7.40- 7.48 (m, 1H), 8.03 (br d, 1H, J = 7.6 Hz), 8.42 (br s. 1H).	556.3	A-2
51		0.08	(DMSO-d6) δ 1.22.- 1.29 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.90-1.99 (m, 1H), 2.10-2.22 (m, 1H), 2.26 (s, 3H), 2.60 (s, 3H), 2.86 (app t, 2,. J = 7.2 Hz), 3.55-3.67 (m, 2H), 3.70 app (t, 1H, J = 4.9 Hz), 3.79-3.84 (m, 1H, 3.83 (s, 3H), 4.33 (q, 2H, J = 7.0 Hz), 4.46-4.52 (m, 1H), 6.99 (s, 1H), 7.09 (d, 1H, J = 4.5 Hz), 7.10 (d, 1H, J = 3.9 Hz), 7.27 (dd, 1H, J = 2.0 Hz, 8.4 Hz), 7.26-7.38 (m, 1H).	598.2	A-2
52		0.3	0.28- 0.35 (m, 2H), 0.47- 0.55 (m, 2H), 1.07- 1.20 (m, 1H), 1.34 (t, 3H, J = 7.0 Hz), 1.76-1.91 (m, 3H), 2.08-2.21 (m, 1H), 2.27 (s, 3H), 2.59 (s, 3H), 3.28-3.46 (m, 4H), 3.87-3.95 (m, 1H), 4.32 (q, 2H, J = 7.1 Hz), 6.95 (s, 1H), 7.07 (s, 1H), 7.95- 8.04 (m, 1H), 7.99- 8.12 (m, 1H), 13.27 (br s, 1H).	468.2	A-2
53		2.1	(DMSO-d6) δ 0.42- 0.53 (m, 1H), 0.60- 0.68 (m, 1H), 1.38- 1.50 (m. 2H), 1.50- 1.60 (m, 1H), 1.81 (dd, 1H, J = 7.5, 14.5 Hz), 2.58 (s, 3H), 4.28-4.45 (m, 2H), 4.48-4.62 (m, 2H), 7.50-7.68 (m, 2H), 8.09 (d, 1H, J = 7.9 Hz). 8.22 (d, 1H, J = 7.8 Hz), 8.34-8.45 (m, 1H), 10.00 (br s, 1H).	436.1	A-5
54		1.0	(DMSO-d6) δ 1.48- 1.59 (m, 2H), 1.69- 1.77 (m, 1H), 1.83- 2.00 (m, 2H), 2.12- 2.23 (m, 1H), 2.47 (s, 3H), 4.18-4.25 (m, 2H), 4.35 (q, 1H, J = 9.4 Hz), 4.62-4.73 (m, 1H), 7.52-7.66 (m, 2H), 8.13 (d, 1H, J = 8.0 Hz), 8.21 (d, 1H, J = 8.0 Hz).	419.2	A-5
55		3.4	(DMSO-d6, 2 isomers) δ 1.10-1.25 and 1.40-1.50 (m, 1H), 1.66-1.82 and 1.72-1.85 (m, 1H), 2.36-2.50 (m, 1H), 2.45 and 2.62 (s, 3H), 3.42-3.62 (m, 2H), 3.70 and 3.87 (s, 2H), 4.00-4.48 (m, 3H), 4..50-4.66 (m 1H), 4.80-5.04 (m 1H), 5.20 and 5.26 (d, 1H, J = 6.2 Hz), 7.44 (app t, 1H, J = 7.5 Hz), 7.55 (app t, 1H, J = 8.0 Hz), 7.64-7.92 (m, 1H), 7.92 (m, 1H), 8.12 (d, 1H, J = 7.8 Hz), 9.3, 9.7, and 10.0 (3 br s, 1H).	4.97	A-6
56		0.06	(DMSO-d6) δ 0.31- 0.39 (m, 2H), 0.59- 0.63 (m, 2H), 1.10- 1.18 (m, 1H), 1.25- 1.31 (m, 1H), 2.00- 2.09 (m, 1H), 2.18 (s, 3H), 2.25-2.31 (m, 2H), 3.45-3.55 (m, 2H, CH2), 3.75 (s, 6H, 2 × OCH3), 3.78- 3.88 (m, 2H), 4.19 (t, 1H, J = 6.3 Hz), 4.33- 4.41 (m, 1H), 4.49- 4.62 (m, 1H), 6.33 (t, 1H, J = 2.1 Hz), 6.53 (d, 1H, J = 2.4 Hz). 6.78-6.80 (m, 1H), 6.95-6.99 (m, 1H), 8.30 (s, 1H).	592.3	A-3, A-4
57		0.1	(DMSO-d6) δ 1.02 (t, 1H, J = 7.2 Hz), 1.10- 1.18 (m, 1H), 1.78- 1.83 (m, 1H), 2.00- 2.09 (m, 1H), 2.19 (s, 3H), 2.24-2.31 (m, 1H), 3.44-3.51 (m, 2H, CH2), 3.75 (s, 6H, 2 × OCH3), 3.78- 3.88 (m, 2H), 4.07 (d, 1H, J = 6.9 Hz), 4.37 (q, 1H, J = 6 Hz), 4.49-4.62 (m, 1H), 6.34 (t, 1H, J = 2.1 Hz), 6.55 (d, 1H, J = 2.4 Hz), 6.78-6.80 (m, 1H), 6.95-6.99 (m, 1H), 8.32 (s, 1H).	488.2	A-3, A-4
58		1.0	(DMSO-d6) δ 0.50- 0.58 (m, 2H), 0.75- 0.79 (m, 2H), 1.03 (s, 9H), 1.30-1.45 (m, 2H), 2.00-2.09 (m, 1H), 2.36-2.42 (m, 4H), 3.45-3.55 (m, 4H, CH2), 3.87-3.95 (m, 2H), 4.29-4.35 (m, 2H), 4.59 (bs, 1H), 7.35-7.45 (m, 1H), 7.68-7.75 (m, 1H), 8.86 (s, 1H).	512.3	A-3, A-4
59		2.0	(DMSO-d6) δ 0.34- 0.39 (m, 2H), 0.58- 0.62 (m, 2H), 1.20- 1.31 (m, 2H), 2.06- 3.0 (m, 1H), 2.17 (s, 3H), 2.38-2.42 (m, 1H), 3.50-3.56 (m, 2H, CH3), 3.59-3.62 (m, 2H), 4.09-4.11 (m, 2H), 4.37-4.42 (m, 1H), 6.78-6.8 (m, 1H), 6.95-6.99 (m, 1H), 8.32 (s, 1H).	500.02	A-3, A-4
60		C	(DMSO-d6) δ 1.05 (t, 3H, J = 7.2 Hz), 1.20- 1.31 (m, 2H), 2.04- 2.1 (m, 1H), 2.17 (s, 3H), 2.35-2.41 (m, 1H), 3.39 (s, 3H), 3.54-3.56 (m, 4H, CH2), 3.59-3.62 (m, 2H), 4.09-4.11 (m, 2H), 4.37-4.42 (m, 1H), 6.78-6.8 (m, 1H), 6.95-6.99 (m, 1H), 8.32 (s, 1H).	488.2	A-3, A-4
61		>1	(DMSO-d6) δ 1.03 (s, 9H), 1.12 (t, 3H, J = 7.2 Hz), 1.32-1.38 (m, 2H), 1.89-1.98 (m, 1H), 2.08-2.14 (m, 1H), 2.18 (s, 3H), 2.38-2.44 (m, 1H), 3.29-3.34 (m, 2H), 3.5-3.57 (m, 2H), 3.82-3.91 (m, 2H), 4.19 (t, 3H, J = 6.3 Hz), 4.39-4.42 (m, 1H), 6.78-6.8 (m, 1H), 6.95-6.99 (s, 1H), 8.32 (s, 1H).	500.2	A-3, A-4
62		0.7	(DMSO-d6) δ 0.29- 0.30 (m, 2H), 0.48- 0.52 (m, 2H), 1.05 (t, 3H, J = 7.2 Hz), 1.20- 1.35 (m, 2H), 1.89- 1.96 (m, 1H), 2.06- 2.10 (m, 1H), 2.32- 2.41 (m + s, 4H), 3.41- 3.47 (m, 2H, CH2), 3.49-3.56 (m, 2H), 4.87-4.92 (m, 2H), 4.38 (t, 3H, J = 6.3 Hz), 4.59 (bs, 1H), 7.34 (s, 1H), 7.61 (s, 1H), 8.79 (s, 1H).	484.5	A-3, A-4
63		0.45	(DMSO-d6) δ 1.10 1.19 (m, 1H), 2.16- 2.20 (m, 1H), 2.37- 2.42 (m, 1H), 2.55 (s, 3H), 3.23-3.32 (m, 4H), 3.39-3.48 (m, 4H), 3.73-3.79 (m, 1H), 3.79-3.89 (m, 1H), 3.9-4.08 (m. 1H), 4.19-4.31 (m, 2H), 4.70-4.81 (bs, 2H), 7.40-7.50 (m, 1H), 7.52-7.60 (m, 1H), 7.90-8.05 (m, 1H), 8.12 (t, 3H, J = 7.8 Hz), 9.68 (bs, 1H).	583.2	Similar to procedure Z59 with modifi- cations
64		0.8	(DMSO-d6) δ 1.30- 1.39 (m, 1H), 1.65- 1.78 (m, 4H), 2.30- 2.40 (m, 1H), 2.50- 2.60 (m, 1H), 2.60 (s, 3H), 3.22-3.34 (m, 4H), 3.95-3.98 (m, 2H), 4.13-4.17 (m, 4H), 4.31 (bs, 1H), 4.42-4.41 (m, 1H), 7.41 (t, 1H, J = 5.7 Hz), 7.52 (t, 1H, J = 5.7 Hz), 7.97 (t, 1H, J = 5.1 Hz), 8.12 (t, 3H, J = 7.8 Hz), 9.68 (bs, 1H).	567.2	Similar to procedure Z59 with modifi- cations
65		1.0	(DMSO-d6) δ 1.0- 1.06 (m, 6H), 1.27- 1.33 (m, 1H), 2.30- 2.38 (m, 1H), 2.50- 2.54 (m, 1H), 2.57 (s, 3H), 3.15-3.24 (m, 4H), 3.89-3.95 (m, 2H), 4.09-4.19 (m, 2H), 4.28 (bs, 1H), 4.38-4.45 (m, 1H), 7.35-7.39 (m, 1H), 7.45-7.49 (m, 1H), 7.92-7.95 (m, 2H).	569.2	Similar to procedure Z59 with modifi- cations
66		0.85	(DMSO-d6) δ 1.25- 1.35 (m, 1H), 2.24- 2.35 (m, 1H), 2.40- 2.50 (m, 1H), 2.63- 2.68 (m, 6H), 3.84- 3.88 (m, 1H), 3.96- 4.0 (m, 1H), 4.02- 4.12 (m, 2H), 4.23- 4.27 (m, 1H), 4.58- 4.64 (m, 1H), 7.52- 7.58 (m, 1H), 7.60- 7.65 (m, 1H), 8.09- 8.16 (m, 2H).	527.2	Similar to procedure Z59 with modifi- cations
101		C	—	443.2	A
102		C	—	407.2	B
103		C	—	443.2	B
104		C	—	358.2	C
105		A	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.38-1.45 (m, 1H), 2.14-2.20 (m, 1H), 2.47-2.55 (m, 1H), 3.62-3.70 (m, 2H), 3.92-3.96 (m, 2H), 4.44-4.51 (m, 1H), 7.43 (t, 1H, J = 8.1 Hz), 7.52 (t, 1H, J = 8.5 Hz), 8.00 (t, 2H, J = 8.5 Hz), 10.66 (d, 1H, J = 5.5 Hz).	408.2	C
106		C	—	342.2	C
107		C	—	375.2	C
108		C	1H NMR (CD3OD) δ 1.17-1.24 (m, 1H), 2.01-2.09 (m, 1H), 2.3l-2.39 (m, 1H), 3.49-3.51 (m, 2H), 3.80 (t, 1H, J = 5.2 Hz), 3.85 (t, 1H, J = 5.1 Hz), 4.37-4.42 (m, 1H), 7.05 (s, 1H), 7.60 (d, 1H, J = 8.9 Hz), 7.68 (d, 1H, J = 8.7 Hz), 7.98 (s, 1H).	—	C
109		A	1H NMR (CD3OD) δ 1.34-1.41 (m, 1H), 2.11-2.20 (m, 1H), 2.44-2.52 (m, 1H), 3.61-3.69 (m, 2H), 3.89-3.94 (m, 2H), 4.43-4.50 (m, 1H), 7.35-7.40 (m, 2H), 7.60-7.64 (m, 1H), 7.68-7.72 (m, 1H), 9.45 (d, 1H, J = 6.4 Hz).	—	C
110		B	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.37-1.4 (m, 1H), 2.12-2.19 (m, 1H), 2.46-2.54 (m, 1H), 3.62-3.68 (br. s, 2H), 3.92-3.96 (br. s, 2H), 4.30-4.50 (m, 1H), 7.27-731 (m, 1H), 7.75-7.79 (m, 1H), 7.98-8.02 (m, 1H), 10.52-10.54 (m, 1H).	426.2	E
111		A	—	476.3	Prepared via hydro- genation of 105 (H2, 20% Pd(OH)2, MeOH/ AcOH, 50 psi).
112		B	—	476.3	J
113		B	—	358.2	Prepared via hydro- genation of 4 (H2, 10% Pd/C, MeOH/ THF).
114		—	1H NMR(CDCl3) δ 1.34 (s, 3H), 1.51 (s, 3H), 1.71-1.75 (m, 1H), 2.41-2.45 (m, 1H), 2.53-2.60 (m, 1H), 3.04 (s, 6H), 3.78-3.82 (m, 2H), 4.51-4.56 (m, 1H), 4.58-4.62 (m, 2H), 5.12 (s, 2H), 6.95 (dd, 1H, J = 9.6, 2.5 Hz), 7.09 (d, 1H, J = 2.1 Hz), 7.79 (d, 1H, J = 8.7 Hz), 10.44 (d, 1H, J = 6.4 Hz).	491.3	F
115		C	—	451.2	F
116		B	1H NMR (DMSO- d6) δ 1.21-1.32 (m, 1H), 1.96-2.01 (m, 1H), 2.32-2.39 (m, 1H), 3.40-3.48 (m, 2H), 3.66-3.84 (m, 10H), 4.30-4.35 (m, 1H), 4.51 (d, 1H, J = 5.1 Hz), 4.66 (t, 1H, J = 5.1 Hz), 4.73 (d, 1H, J = 6.0 Hz), 7.43 (t, 1H, J = 7.4 Hz), 7.53 (t, 1H, J = 7.7 Hz), 8.02 (d, 1H, J = 8.0 Hz), 8.10 (d, 1H, J = 8.1 Hz), 10.51 (d, 1H, J = 6.6 Hz).	478.3	H
117		B		420.2	C
118		C		393.2	H (Step 4)
119		A		388.2	I
120		C	1H NMR(CDC3) δ 1.31 (s, 3H), 1.52 (s, 3H), 1.71-1.77 (m, 1H), 2.45-2.51 (m, 1H), 2.52-2.59 (m, 1H), 3.23 (s, 6H), 3.29 (s, 3H), 3.51 (d, 2H, J = 5.7 Hz), 4.49- 4.55 (m, 2H), 4.63- 4.65 (m, 1H), 7.34 (t, 1H, J = 8.2 Hz), 7.45 (t, 1H, J = 7.7 Hz), 7.86 (d, 1H, J = 7.4 Hz), 7.92 (d, 1H, J = 8.1), 10.61 (d, 1H, J = 6.1 Hz).	490.3	G
121		A	—	450.2	G (Step 7) (Obtained from 120)
122		—	1H NMR (CDCl3) δ 1.30 (s, 3H), 1.52 (s, 3H), 1.66-1.73 (m, 1H), 2.42-2.47 (m, 1H), 2.50-2.58 (m, 1H), 2.69 (s, 3H), 3.24 (s, 9H), 3.48 (d, 2H, J = 6.6 Hz), 4.50- 4.55 (m, 2H), 4.63- 4.65 (m, 1H), 7.33 (t, 1H, J = 7.7 Hz), 7.45 (t, 1H, J = 7.7 Hz), 7.85 (d, 1H, J = 8.2 Hz), 7.94 (d, 1H, J = 8.1 Hz), 9.62 (d, 1H, J = 6.0 Hz).	470.12	I
123		C	—	430.2	G (Step 7) (Obtained from 122)
124		A	1H NMR (DMSO- d6) δ 1.20-1.29 (m, 1H), 1.93-2.01 (m, 1H), 2.31-2.39 (m, 1H), 3.39-3.48 (m, 2H), 3.75 (q, 1H, J = 10.2, 5.1 Hz), 3.79-3.83 (m, 1H), 4.05-4.16 (m, 1H), 4.23-4.40 (m, 2H), 4.53 (d, 1H, J = 5.2 Hz), 4.64 (t, 1H, J = 5.1 Hz), 4.69 (d, 1H, J = 5.2 Hz), 7.45 (t, 1H, J = 7.3 Hz), 7.54 (t, 1H, J = 7.3 Hz), 8.03 (d, 1H, J = 8.1 Hz), 8.11 (d, 1H, J = 8.0 Hz), 8.28- 8.32 (m, 1H), 10.53 (d, 1H, J = 5.8 Hz).	490.3	H
125		A	1H NMR (DMSO- d6) δ 1.13-1.25 (m, 1H), 1.93-2.01 (m, 1H), 2.28-2.37 (m, 1H), 2.55 (s, 3H), 3.37-3.49 (m, 2H), 3.71-3.79 (m, 2H), 4.06-4.17 (m, 1H), 4.19-4.32 (m, 2H), 4.42-4.50 (m, 1H), 4.58-4.61 (m, 2H), 7.43 (t, 1H, J = 7.2 Hz), 7.54 (t, 1H, J = 7.7 Hz), 7.61 and 7.62-7.79 (br. s and m, 1H) 8.02 (d, 1H, J = 8.1 Hz), 8.11 (d, 1H, J = 7.8 Hz), 9.33 and 9.59-9.65 (br. s and m, 1H)	470.3	I
126		A	1H NMR (DMSO- d6) δ 1.12-1.29 (m, 1H), 1.89-2.01 (m, 3H), 2.31-2.42 (m, 1H), 3.36-3.50 (m, 4H), 3.76-3.82 (m, 2H), 4.27-4.33 (m, 1H), 4.45-4.51 (m, 2H), 4.56-4.68 (m, 3H), REDO this proton, 7.52 (t, 1H, J = 7.5 Hz), 7.80-7.86 (br. s, 1H), 7.99 (d, 1H, J = 8.3 Hz), 8.08 (d, 1H, J = 7.2 Hz), 10.59 (d, 1H, J = 5.7 Hz).	468.3	H
127		0.7	1H NMR (DMSO- d6) δ 1.14-1.25 (m, 1H), 1.88-1.98 (m, 3H), 2.30-2.38 (m, 1H), 2.55 (s, 3H), 3.38-3.46 (m, 4H), 3.71-3.78 (m, 2H), 4.27-4.33 (m, 1H), 4.45-4.65 (m, 5H), 7.26-7.30 (br. s, 1H), 7.39 (t, 1H, J = 7.5 Hz), 7.50 (t, 1H, J = 7.7 Hz), 7.97 (d, 1H, J = 8.0 Hz), 8.07 (d, 1H, J = 8.3 Hz), 9.78-9.80 (br. s, 1H).	448.2	I
151		C		395.2	A
152		C		341.2	B
153		C		357.2	B
154		C		399.2	B
155		C		385.2	B
156		C		369.2	B
157		C		352.2	C
158		C		437.2	C
159		C		353.2	C
160		C		NA	C
161		C		358.2	C
162		C		395.2	C
163		C		358.2	C
164		C		409.2	D
165		C		425.2	D
166		B		462.3	D
167		C		409.2	D
168		C		462.3	D
169		C		427.2	D
170		C		427.2	D
171		C		416.2	D
172		C		448.2	D
173		C		434.2	D
174		C		467.3	D
175		C		504.3	D
176		C		461.99	D
177		C		NA	D
178		C		433.95	D
179		C		504.3	D
180		C		508.3	D
181		A		438.2	E
182		A		452.2	E
183		B	1H NMR (CD3OD) δ 1.10-1.20 (,, 31H), 2.01-2.09 (m, 1H), 2.22-2.34 (m, 1H), 3.47-3.60 (m, 2H), 3.69-3.77 (m, 2H), 3.85 (s, 2H), 4.20- 4.29 (m, 1H), 6.63- 6.67 (m, 1H), 6.70- 6.73 (m, 1H), 6.75- 6.79 (m, 1H).	442.2	E
184		A	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.33 (s, 3H), 1.50 (s, 3H) 1.67- 1.77 (m, 1H), 2.31- 2.42 (m, 1H), 2.48- 2.58 (m, 1H), 2.61- 2.64 (m, 1H), 3.68- 3.73 (m, 2H), 4.46- 4.54 (m, 1H), 4.60- 4.64 (m, 2H), 7.41 (t, 1 H, J = 7.7 Hz), 7.51 (t, 1 H, J = 7.3 Hz), 7.97 (d, 1 H, J = 8.0 Hz), 10.57 (d, 1 H, J = 5.9 Hz).	448.2	Prepared from 105 using Pro- cedure F, Step 1.
185		C		619.3	F
186		B		484.6	F
187		C	1H NMR (CDCl3) δ 1.33 (s, 3H), l.54 (s, 3H), 1.70- 1.78 (m, 1H), 2.40- 2.47 (m, 1H), 2.52- 2.64 (m, 1H), 3.78- 3.83 (m, 1H), 4.51- 4.64 (m, 2H), 5.19- 5.25 (m, 1H), 7.40- 7.45 (m, 1H), 7.83- 7.91 (m, 2H), 10.55- 10.62 (m, 1H).	615.3	F
188		C	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.40-1.53 (m, 1H), 2.17-2.25 (m, 1H), 2.48-2.61 (m, 1H), 3.51-3.56 (m, 2H), 3.65-3.73 (m, 2H), 3.96-4.03 (m, 1H), 4.49-4.57 (m, 1H), 7.43 (t, 1 H, J = 8.1 Hz), 7.56- 7.63 (m, 1 H), 8.05- 8.09 (m, 1H), 8.14- 8.16 (m, 1H).	442.2	F
189		B	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.28-1.41 (m, 1H), 2.11-2.22 (m, 1H), 2.45-2.57 (m, 1H), 3.55-3.69 (m, 2H), 3.87-3.96 (m, 2H), 4.45-4.53 (m, 1H), 7.23-7.31 (m, 1 H), 7.68-7.74 (m, 1 H).	444.2	F
190		C		446.2	F
191		B	1H NMR (CD3OD + DMS0-d6, 3 drops) 51.43-1.51 (m, 1H), 2.17-2.54 (m, 1H), 2.48-2.61 (m, 4H), 3.67-3.70 (m, 2H), 3.96-4.06 (m, 2H), 4.52-4.61 (m, 1H), 7.33-7.39 (m, 1 H), 7.59-7.66 (m, 1 H), 7.70-7.76 (m, 1H).	406.2	F
192		C		446.2	F
193		C	1H NMR (CD3OD) δ 1.29-1.37 (m, 1H), 2.04-2.13 (m, 1H), 2.36-2.46 (m, 4H), 3.51-3.58 (m, 2H), 3.81-3.93 (m, 2H), 4.39-4.66 (m, 2H), 7.18-7.24 (mm 1H), 7.46-7.55 (mm 1H).	406.2	F
194		A	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.41-1.51 (m, 1H), 2.15-2.24 (m, 1H), 2.49-2.58 (m, 1H), 3.18 (s, 3H), 3.65-3.71 (m, 2H), 3.94-4.01 (m, 2H), 4.47-4.55 (m, 1H), 7.54-7.61 (m, 1H), 7.65-7.71 (m, 1 H), 8.17-8.19 (m, 1 H), 8.24 (d, 1H, J = 9.0 Hz).	437.2	F
195		A		492.3	E
196		A	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.37-1.48 (m, 1H), 2.11-2.20 (m, 1H), 2.44-2.54 (m, 1H), 3.09-3.16 (m, 3H), 3.52-3.74 (m, 4H), 3.89-4.11 (m, 2H), 4.42-4.51 (m, 1H), 7.47-7.52 (m, 1H), 7.98-8.03 (m, 1 H), 8.10-8.15 (m, 1 H).	437.2	F
197		A	1H NMR(CDCl3) δ 1.07 (t, 3H, J = 7.3 Hz), 1.25 (s, 1H), 1.32 (s, 3H), 1.53 (s, 1H), 1.69- 1.78 (m, 1H), 1.81- 1.90 (m, 2H), 2.38- 2.48 (m, 1H), 2.51- 2.61 (m, 1H), 3.75- 3.86 (m, 1H), 3.99 (t, 1H, J = 6.6 Hz), 4.50-4.55 (m, 1H), 4.58-4.64 (m, 1H), 5.22 (s, 1H), 7.04- 7.10 (m, 1H), 7.31- 7.34 (m, 1 H), 7.84 (d, 1H, J = 8.9 Hz), 10.50 (d, 1H, J = 6.4 Hz).	466.3	F
198		C	1H NMR (CDCl3) δ 1.32 (s, 3H), 1.52 (s, 3H), 1.69- 1.80 (m, 1H), 2.38- 2.48 (m, 1H), 2.51- 2.61 (m, 1H), 3.76- 3.84 (m, 1H), 4.52- 4.56 (m, 1H), 4.58- 4.65 (m, 1H), 5.14- 5.19 (m, 2H), 7.12- 7.17 (m, 1H), 7.35- 7.39 (m, 1 H), 7.39- 7.50 (m, 1H), 7.83- 7.89 (m, 1H), 10.49- 10.54 (m, 1H).	554.3	F
199		C		514.3	F
200		A		451.2	F (from starting material 403a)
201		A		466.3	H
202		B		480.3	H
203		C	1.36-1.50 (m, 4H), 2.13-2.24 (m, 1H), 2.52-2.63 (m, 1H), 3.23 (s, 3H), 3.61-3.72 (m, 2H), 3.92-4.01 (m, 2H), 4.11-4.19 (m, 2H), 4.37-4.12 (m, 1H), 4.43-4.52 (m, 1H), 7.09-7.15 (m, 1H), 7.15-7.53 (m, 1 H), 7.52 (t, 1 H, J = 8.5 Hz), 7.90 (6, 1 H, J = 8.8 Hz), 10.57 (d, 1 H, J = 6.8 Hz).	480.3	E
204		C	1H NMR (CD3OD + DMSO-d6, 3 drops) δ 1.38-1.47 (m, 1H), 2.18-2.33 (m, 1H), 2.55-2.61 (m, 1H), 3.064 (s, 1H) 3.65-3.71 (m, 2H), 3.92-3.99 (m, 2H), 4.37 (s, 1H) 4.44-4.53 (m, 1H), 7.02-7.05 (m, 1H), 7.33 (d, 1 H, J = 2.0 Hz), 7.56 (d, 1 H, J = 8.8 Hz), 10.77 (d, 1 H, J = 5.5 Hz).	479.3	E (Steps 2 and 3)
205		A		446.2	I
206		A	1H NMR (DMSO) δ 1.17-1.28 (m, 1H), 1.91-2.02 (m, 1H), 2.27-2.41 (m, 1H), 3.39-3.52 (m, 4H) 3.72-3.84 (m, 2H), 4.26-4.34 (rn, 1H) 4.52-4.53 (m, 1H), 4.61-4.67 (rn, 1H), 4.68-4.74 (m, 1H), 7.38-7.46 (m, 1H), 7.48-7.56 (m, 1 H). 7.70-7.77 (m, 1 H), 7.99 (d, 1H, J = 8.0 Hz), 8.07 (d, 1H, J = 8.2 Hz) 10.58- 10.59 (m, 1 H).	480.3	H
207		C		460.3	I
208		A		460.3	I
209		A	1H NMR (DMSO)- d6) δ 1.21-1.29 (m, 1H), 1.90-1.98 (m, 1H), 2.00 (s, 3H), 2.29-2.41 (m, 1H), 3.32 (s, 3H), 3.40- 3.47 (m, 2H) 3.52- 3.57 (m, 2H), 3.74- 3.74 (m, 1H), 3.79- 3.83 (m, 1H) 4.13- 4.17 (m, 1H), 4.25- 4.30 (m, 1H), 4.52 (d, 1H J = 5.1 Hz), 4.65 (t, 1H J = 4.8 Hz), 4.70 (d, 1H, J = 5.1 Hz), 7.38-7.46 (m, 1H), 7.52 (t, 1H, J = 7.3 Hz), 7.83-7.89 (m, 1H), 7.99-8.03 (m, 1H), 8.06-8.11 (m, 1H), 10.58 (d, 1H, J = 5.9 Hz)	494.3	H
210		A		432.2	I
211		A	1H NMR (DMSO)- D6) δ 1.08-1.30 (m, 1H), 1.88-1.99 (m, 1H), 2.00 (s, 3H), 2.28-2.40 (m, 1H), 2.54 (s, 3H), 3.38- 3.48 (m, 2H) 3.50- 3.56 (m, 3H), 3.69- 3.79 (m, 1H), 4.10- 4.18 (m, 1H), 4.22- 4.37 (m, 1H), 4.57- 4.68 (m, 1H), 7.39 (t, 1H, J = 7.0 Hz), 7.50 (t, 1H, J = 7.8 Hz), 7.97 (d, 1H, J = 7.3 Hz), 8.07 (d, 1H, J = 8.3 Hz)	474.3	I
212		A	1H NMR (DMSO)- d6) δ 1.20-1.30 (m, 1H), 1.91-2.03 (m, 1H), 2.28-2.44 (m, 1H), 3.36-3.56 (m, 4H). 3.72-3.84 (m, 2H) 4.25-4.37 (m, 1H), 4.50-4.51 (m, 1H), 4.62-4.74 (m, 3H), 7.39-7.46 (m, 1H), 7.47-7.49 (m, 1H), 7.59-7.65 (m, 1H), 7.98 (d, 1H, J = 8.3 Hz), 8.07 (d, 1H, J = 7.1 Hz), 10.58 (d, 1H, J = 5.9 Hz).	452.2	Prepared via treatment of 209 with aqueous potassium carbonate and dioxane.
213		A	1H NMR (DMSO)- d6) δ 1.22-1.32 (m, 1H), 1.92-2.03 (m, 1H), 2.29-2.40 (m, 1H), 3.39-3.49 (m, 2H), 3.54-3.67 (m, 2H) 3.74-3.82 (m, 2H), 4.24-4.35 (m, 1H), 4.44-4.55 (m, 1H), 4.60-4.72 (m, 1H), 7.39-7.46 (m, 1H), 7.50-7.55 (m, 1H), 7.91-7.95 (m, 1H), 8.08-8.11 (m, 1H), 10.53-10.60 (m, 1H)	454.2	H
214		A	1H NMR (DMSO)- d6) δ 1.22-1.32 (m, 1H), 1.92-2.04 (m, 1H), 2.29-2.39 (m, 1H), 3.40-3.51 (m, 2H), 3.64-3.83 (m, 4H) 4.25-4.37 (m, 1H), 4.43-4.55 (m, 1H), 4.57-4.72 (m, 2H), 4.63-4.72 (m, 2H) 6.03-6.31 (m, 1H), 7.41-7.47 (m, 1H), 7.51-7.56 (m, 1H), 7.84-7.89 (m, 1H), 8.04-8.10 (m, 1H), 8.09 (d, 1H J = 8.3 Hz), 10.54 (d, 1H J = 5.2 Hz)	472.3	H
215		A	1H NMR (DMSO)- d6) δ 1.08-1.31 (m, 1H), 1.91-2.05 (m, 1H), 2.25-2.39 (m, 1H) 2.53 (s, 3H), 3.37-3.53 (m, 3H), 3.63-3.81 (m, 4H) 4.23-4.36 (m, 1H), 4.41-4.52 (m, 1H), 4.57-4.72 (m, 2H) 6.00-6.29 (m, 1H), 7.34-7.44 (m, 1H), 7.45-7.56 (m, 1H), 7.99 (d, 1H, J = 1H, Hz), 8.10 (d, 1H, J = 7.8 Hz), 9.52-9.65 (m, 1H)	452.2	I
216		B		434.2	I
217		A	1H NMR (DMSO) δ 1.12-1.33 (m, 1H), 1.91-2.05 (m, 1H), 2.29-2.43 (m, 1H), 2.54-3.39 (m, 2H), 3.38-3.63 (m, 4H) 3.71-3.88 (m, 2H), 4.23-4.39 (m, 1H) 4.47-4.57 (m, 1H), 4.62-4.76 (m, 1H), 7.39-7.61 (m, 2H), 7.86-7.95 (m, 1 H), 8.01-8.15 (m, 2H), 10.54-10.67 (m, 1 H).	504.3	H
218		A		484.3	I
219		A	1H NMR (DMSO) δ 1.08 (d, 6H J = 5.9), 1.16-1.29 (m, 1H), 1.90-2.02 (m, 1H), 2.28-2.42 (m, 1H), 3.24-3.62 (m, 4H) 3.72-3.85 (m, 2H), 3.99-4.16 (m, 1H), 4.25-4.36 (m, 1H), 4.43-4.74 (m, 3H), 7.38-7.46 (m, 1H), 7.51 (t, 1 H J = ), 8.01- 8.15 (m, 2H), 10.54- 10.67 (m, 1 H).	494.3	H
220		A	—	474.3	I
222		A	—	480.3	H
223		A	—	460.3	I
224		A		518.3	H
225		A	—	498.3	I
226		A	—	494.3	H
227		A	—	474.3	I
228		A		480.3	H
229		A		460.3	I
302		B	1H NMR (DMSO)- d6) δ 0.98-1.06 (m, 1H), 1.78-1.87 (m, 1H), 2.04-2.12 (m, 1H), 3.24-3.35 (m, 2H), 3.60-3.67 (m, 2H), 4.31-4.38 (m, 2H), 4.48-4.53 (m, 2H), 6.69 (d, 1 H, J = 6.69 Hz), 6.96 (br. s, 2 H), 7.22 (s, 1 H), 8.97 (d, 1 H, J = 2.6 Hz) and 9.19 (d, 1 H, J = 2.6 Hz). 13C NMR(DMSO- d6) δ 29.90, 44.92, 55.67, 62.50, 71.81, 75.29, 93.69, 109.30, 121.30, 126.11, 140.13, 141.65, 153.08, 158.59, 161.80, 162.35 and 163.63	437.2	A-2
303		B	1H NMR (CD3OD) δ 0.80-1.00 (m, 1H), 1.99-2.08 (m, 1H), 2.22-2.40 (m, 1H), 3.41-3.55 (m, 2H), 3.72-3.80 (m, 2H), 4.35-4.49 (m, 1H), 7.18 (s, 1H), 8.28 (br. s, 1 H) and 8.75 (br. s, 1 H).	410.2	L
304		C	1H NMR (CD3OD) δ 1.18-1.26 (m, 1H), 2.00-2.09 (m, 1H), 2.30-2.39 (m, 1H), 2.55 (s, 3H), 3.48- 3.54 (m, 2H), 3.78- 3.83 (m, 1H), 3.83- 3.88 (m, 1H), 4.38- 4.45 (m, 1H), 7.10 (s, 1 H), 8.16 (br. s, 1H) and 8.64 (br. s, 1 H), 13C NMR (CD3OD) 815.71, 30.79, 46.28, 57.45. 63.81, 74.20, 78.12, 97.03, 107.90. 128.12, 131.59, 137.19, 142.35, 153.12, 154.67, 160.05, 163.32 and 163.69.	406.2	L
306		A	1H NMR (CD3OD) δ 1.17-1.23 (m, 1H), 2.00-2.09 (m, 1H), 2.31-2.39 (m, 1H), 2.60 (s, 3H), 3.48- 3.54 (m, 2H), 3.78- 3.83 (m, 1H), 3.83- 3.88 (m, 1H), 4.38- 4.43 (m, 1H), 6.96 (d, 1 H,), 7.52 (br. s, 1H) and 8.66 (br. s, 1 H). 13C NMR (CD3OD) δ23.45, 30.82, 46.25, 57.44, 63.74, 74.22, 78.14, 97.01, 108.84, 116.24, 132.67, 138.23, 151.71, 152.14, 155.44, 159.97, 163.22 and 163.66.	406.2	L
305		A	1H NMR (CD3OD) δ 1.18-1.23 (m, 1H), 2.00-2.10 (m, 1H), 2.31-2.40 (m, 1H), 2.72 (s, 3H), 3.46- 3.53 (m, 2H), 3.78- 3.83 (m, 1H), 3.83- 3.88 (m, 1H), 4.38- 4.44 (m, 1H), 7.02 (s, 1 H,), 7.52 (d, 1H, J = 5.6 Hz) and 8.19 (d, 1 H, J = 5.6 Hz). 13C NMR (CD3OD) δ 17.99, 30.87, 46.25, 57.41. 63.78, 74.26, 78.22, 97.05, 109.42, 115.64, 136.64, 141.99, 143.51, 152.00, 154.59, 159.97, 163.28 and 163.69.	406.2	L
307		C	1H NMR (CD3OD) δ 1.23-1.38 (m, 1H), 2.00-2.11 (m, 1H), 2.27-2.38 (m, 1H), 3.42-3.56 (m, 2H), 3.80-3.92 (m, 2H), 4.48-4.59 (m, 1H), 7.03 (s, 1 H,) and 8.43 (s, 1 H).	409.0	L
308		A	1H NMR (DMSO- d6) δ 0.99-1.08 (m, 1H), 1.46 (t, 3H, J = 7.4 Hz), 1.82-1.90 (m, 1H), 2.10-2.19 (m, 1H), 3.22-3.34 (m, 4H), 3.62-3.72 (m, 2H), 4.31-4.41 (m, 1H), 6.92 (d, NH, J = 7.6 Hz), 7.12 (br. s, NH2) 7.43 (s, 1 H), 8.08 (d, 1H, J@ 5 Hz) and 8.50 (br. s, 1H). 13C NMR (DMSO- d6) δ 12.37, 21.97, 29.86, 44.79, 55.67, 62.34, 71.80, 75.38, 93.10, 108.88, 116.13, 133.84, 140.83, 142.82, 148.80, 158.27, 159.95, 161.13 and 162.07.	420.2	L
309		A	1H NMR (CD3OD) δ 1.20-1.26 (m, 1H), 1.32 (t, 3H, J = 7.6 Hz), 2.01-2.09 (m, 1H), 2.32-2.40 (m, 1H), 2.71 (s, 3H), 2.86 (q, 2H, J = 7.6 Hz), 3.47-3.53 (m, 2H), 3.77-3.81 (m, 1H), 3.83-3.87 (m, 1H), 4.38-4.43 (m, 1H), 6.94 (s, 1 H,) and 7.36 (s, 1 H). 13C NMR (CD3OD) δ 15.40, 17.78, 30.88, 31.49, 46.24, 57.40, 63.77, 74.26, 78.24, 97.23, 109.28, 112.97, 137.51, 142.37, 150.62, 154.64, 156.84, 159.87, 163.25 and 163.61.	434.2	N
403		A	1H NMR (DMSO- d6) 1.13-1.30 (m, 1H), 1.11-2.04 (m, 1H), 2.28-2.47 (m, 1H), 2.78-2.92 (m, NHCH3), 3.39-3.52 (m, 2H), 3.72-3.80 (m, 1H), 3.80-3.87 (m, 1H), 4.27-4.40 (m, 1H), 4.43-4.52 (m, OH), 4.60-4.69 (m, OH), 4.69-4.76 (m, OH), 7.37-7.47 (m, 1H), 7.47-7.55 (m, 1H), @7.50, 7.64 and 7.77 (br. s., NHCH3), 7.96- 8.02 (m, 1H), 8.03- 8.12 (m, 1H) and 10.30, 10.47 and 10.56 (d, 1 H, all J = 6.2).	422.2	K
310		A		436.1	Combi- nation of M and N
311		A	1H NMR (DMSO- d6 + CD3OD) δ 1.04- 1.10 (m, 1H), 1.83- 1.92 (m, 1H), 2.12- 2.20 (m, 1H), 2.86 (s, 3H) 3.30-3.35 (m, 2H), 3.43 (s, 3H), 3.66-3.70 (m, 2H), 4.33-4.40 (m, 1H), 4.73 (s, 2H), 7.38 (s, 1H) and 8.02 (s, 1H).	450.16	Combi- nation of M and N
408		A	1H NMR (DMSO- d6) δ 1.22-1.30 (m, 1H), 1.97-2.05 (m, 1H), 2.36-2.46 (m, 1H), 3.17 (s, 6H, 2xNCH3) 3.42-3.52 (m, 2H), 3.75-3.79 (m, 1H), 3.82-3.86 (m, 1H), 4.28-4.35 (m, 1H), 4.51 (d, 1 OH, J = 5.2 Hz), 4.65 (t, 1 OH, J = 5.2 Hz), 4.71 (d, 1 OH, J = 5.4 Hz), 7.42-7.60 (m, 1 H), 7.51-7.60 (m, 1 H), 8.02 (d, 1 H, J = 8.0 Hz), 8.10 (d, 1H, J = 7.8 Hz) and 10.51 (d, 1H, J = 6.5 Hz). 13C NMR (DMSO- d6) δ 30.36, 36.36 (2xC), 44.85, 56.03, 62.44, 72.50, 76.56, 96.81, 121.16, 121.56, 124.99, 126.31, 132.80, 150.27, 157.76, 158.09, 159.83 and 162.96.	436.05	C
312		A	1H NMR (DMSO- d6) δ 0.93 (t, CH3CH2, J = 7.4 Hz), 0.97-1.14 (m, 1H), 1.67-1.75 (m, 2H), 1.81-1.92 (m, 1H), 2.06-2.23 (m, 1H), 2.65 (s, CH3), 2.72-2.80 (m, 2H), 2.83 (br.s, NHCH3), 3.27-3.41 (m, 2H), 3.61-3.78 (m, 2H), 4.27-4.36 (m, 1H), 4.44 (br. s, OH), 4.55 (br. s, 2x OH), 6.61 and 6.76 (br. s, NH), 6.99 (s, 1H), 7.29 and 7.37 (br. s, NH) and 7.37 (s, 1H).	462.3	N
313		A	1H NMR (DMSO- d6) δ 1.18-1.26 (m, 1H), 1.96-2.03 (m, 1H), 2.35-2.43 (m, 1H), 2.60 (s, 3H, CH3), 3.17 (s, 6H, 2xNCH3) 3.40-3.52 (m, 2H), 3.73-3.81 (m, 2H), 4.27-4.33 (m, 1H), 4.48 (d, 1 OH, J = 5.0 Hz), 4.61 (t, 1 OH, J = 5.2 Hz), 4.65 (d, 1 OH, J = 5.2 Hz), 7.38-7.42 (m, 1 H), 7.50-7.54 (m, 1 H), 7.99 (d, 1 H, J = 8.0 Hz), 8.09 (d, 1H, J = 8.0 Hz) and 9.70 (d, 1H, J = 6.4 Hz). 13C NMR (DMSO- d6) δ25.89, 30.67, 36.24 (2xC), 44.95, 55.57, 62.67, 72.58, 76.70, 98.77, 121.22, 121.49, 124.49, 126.26, 133.06, 151.11, 159.32, 159.47, 164.62 and 164.81.	416.2	O
314		C	1H NMR (CD3OD) δ 1.27 (t, 3H, J = 7.5 Hz), 1.30-1.35 (m, 1H), 2.09-2.18 (m, 1H), 2.44-2.51 (m, 1H), 2.84 (q, 2H, J = 7.5 Hz), 3.22 (s, 6H, 2xNCH3) 3.54-3.62 (m, 2H), 3.87-3.90 (m, 2H), 4.41-4.48 (m, 1H), 7.38-7.42 (m, 1H), 7.48-7.52 (m, 1H) and 7.94-7.98 (s, 2H).	430.1	O
412		A	1H NMR (DMSO- d6 + DCl) δ 1.12 (t, 3H, J = 7.5 Hz), 1.15-1.25 (m, 1H), 1.92-2.01 (m, 1H), 2.28-2.38 (m, 1H), 3.32 (q, 2H, J = 7.5 Hz), 3.36-3.46 (m, 2H), 3.71-3.76 (m, 1H), 3.78-3.82 (m, 1H), 4.23-4.31 (m, 1H), 7.37-7.44 (m, 1 H), 7.46-7.53 (m, 1 H), 7.99 (d, 1 H, J = 8.0 Hz), 8.05 (d, 1H, J = 8.0 Hz) and 10.60 (br. s, NH).	436.2	H
317			1H NMR (DMSO- d6) δ 1.14 (t, 3H, CH3, J = 7.1 Hz), 1.14-1.27 (m, 1H), 1.89-2.04 (m, 1H), 2.29-2.41 (m, 1H), 2.56 (s, 3H, CH3), 3.35 (q, 2H) 3.38-3.51 (m, 2H), 3.69-3.87 (m, 2H), 4.27-4.35 (m, 1H), 4.45 (br. s, 1 OH), 4.60 (t, 1 OH, J = 5.2 Hz), 4.68 (d, 1 OH, J = 5.2 Hz), 7.20 (br. s, 1H, NH), 7.32- 7.41 (m, 1 H), 7.46- 7.53 (m, 1 H), 7.99 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1 H, J = 8.0 Hz) and 9.82 (br. s, 1H, NH). 13C NMR (DMSO- d6) δ 14.84, 25.42, 30.80, 35.22, 45.01, 55.54, 62.76, 72.55, 76.74, 98.77, 121.21, 121.42, 124.42, 126.23, 133.00, 151.10, 159.73, 159.89, 164.87 and 164.96.	416.06	O
318		A		450.2	H
319		A	1H NMR (DMSO- d6 + DCl) δ 1.12-1.25 (m, 1H), 1.90-2.04 (m, 1H), 2.26-2.42 (m, 1H), 2.55 (s, 3H, CH3), 2.82 (s, 3H, NHCH3), 3.37-3.51 (m, 2H), 3.68-3.86 (m, 2H), 4.26-4.39 (m, 1H), 7.30-7.58 m, 2 H), 7.99 (d, 1 H, J = 7.9 Hz) and 8.09 (d, 1H, J = 7.9 Hz).	402.2	O
321		A	1H NMR (DMSO- d6 + DCl) δ 0.93 (d, 6H, 2xCH3, J = 7.6 Hz), 1.16- 1.27 (m, 1H), 1.86- 1.99 (m, 2H), 2.18- 2.27 (m, 1H), 2.48 (s, 3H, CH3), 3.22-3.41 (m, 4H), 3.66-3.70 (m, 1H), 3.77-3.82 (m, 1H), 4.31-4.38 (m, 1H), 7.49-7.52 (m, 1 H), 7.56-7.61 (m, 1H), 8.13 (d, 1 H, J = 8.0 Hz) and 8.19 (d, 1H, J = 8.0 Hz).	444.2	O
320		A	1H NMR (DMSO- d6 + DCl) δ 0.88 (d, 6H, 2xCH3, J = 7.6 Hz), 1.19- 1.27 (m, 1H), 1.80- 1.90 (m, 1H), 1.93- 2.01 (m, 1H), 2.30- 2.39 (m, 1H), 3.08- 3.22 (m, 2H), 3.36- 3.46 (m, 2H), 3.72- 3.75 (m, 1H), 3.79- 3.82 (m, 1H), 4.24- 4.30 (m, 1H), 7.40- 7.44 (m, 1 H), 7.49- 7.54 (m, 1H), 8.02 (d, 1 H, J = 8.0 Hz) and 8.08 (d, 1H, J = 8.0 Hz).	464.3	H
401		A	1H NMR (DMSO- d6) δ 1.10-1.02 (m, 1H), 1.82-1.91 (m, 1H), 2.10-2.20 (m, 1H), 2.74 (s, 3H), 2.89 (s, 3H), 3.28- 3.35 (m, 2H), 3.66- 3.72 (m, 2H), 4.30- 4.39 (m, 1H), 6.86 (d, 1 H, J = Hz), 7.10 (br. s, NH2), 7.34 (s, 1H) and 7.86 (s, 1H).	420.1	L
402		C		393.1	L
404		C		436.1	K
406		A	1H NMR (DMSO- d6) δ 1.01-1.08 (m, 1H), 1.33 (t, 3H, J = 7.6 Hz), 1.80-1.88 (m, 1H), 2.07-2.15 (m, 1H), 3.05-3.12 (m, 2H), 3.28-3.34 (m, 2H), 3.63-3.69 (m, 2H), 4.30-4.38 (m, 1H), 6.84 (d, 1 NH, J = 7.2 Hz), 7.40 (s, 1 H), 8.11 (s, 1H) and 9.34 (s, 1 H).	420.05	Combi- nation of M and N.
407		A	1H NMR (DMSO- d6) δ 0.98-1.06 (m, 1H), 1.33 (t, 3H, J = 7.2 Hz), 1.41 (t, 3H, J = 7.4 Hz), 1.80- 1.89 (m, 1H), 2.07- 2.16 (m, 1H), 3.08 (q, 2H, J = 7.2 Hz), 3.24-3.34 (m, 4H), 3.62-3.67 (m, 2H), 4.30-4.39 (m, 1H), 6.90 (d, 1 NH, J = 7.5 Hz), 7.34 (s, 1 H) and 7.91 (s, 1 H).	448.2	L
410		A		434.2	Combi- nation of M and N.
411		B	1H NMR (DMSO- d6) δ 1.10-1.22 (m, 2xCH3), 1.22-1.32 (m, 1H), 1.97-2.05 (m, 1H), 2.33-2.42 (m, 1H), 3.40-3.52 (m, 2H), 3.52-3.71 (m, 4H), 3.76-3.87 (m, 2H), 4.23-4.31 (m, 1H), 4.54 (br. s, 1 OH), 4.61-4.72 (m, 2x OH), 7.39-7.47 (m, 1 H), 7.50-7.57 (m, 1 H), 8.00 (d, 1 H, J = 7.7 Hz), 8.08 (d, 1H, J = 7.7 Hz) and 10.49 (d, 1H, J = 5.8 Hz).	464.3	H
413		B	1H NMR (DMSO- d6) δ 1.19-1.27 (m, 1H). l.94-2.02 (m, 1H), 2.26-2.40 (m, 3H), 3.38-3.49 (m, 2H), 3.74-3.78 (m, 1H), 3.79-3.84 (m, 1H), 4.05-4.14 (m, 4H), 4.23-4.30 (m, 1H), 4.49 (d, 1 OH, J = 4.6 Hz), 4.63 (t, 1 OH, J = 5.0 Hz), 4.74 (d, 1 OH, J = 5.0 Hz), 7.40-7.45 (m, 1 H), 7.50-7.55 (m, 1 H), 8.01 (d, 1 H, J = 7.9 Hz), 8.09 (d, 1H, J = 7.9 Hz) and 10.48 (d, 1H, J = 6.5 Hz).	448.2	H
414		C		478.3	O
415		C	1H NMR (DMSO- d6) δ 1.10-1.17 (m, 1H), 1.96-2.04 (m, 1H), 2.36-2.43 (m, 1H), 3.33 (s, 6H, 2xNCH3) 3.39-3.50 (m, 2H), 3.73-3.76 (m, 2H), 4.28-4.34 (m, 1H), 4.99 (d, OH, J = 5.1 Hz), 4.62 (t, 1 OH, J = 5.2 Hz), 4.68 (d, OH, J = 5.2 Hz), 7.08-7.13 (m, 1 H), 7.26-7.34 (m, 1H), 7.41-7.47 (m, 1 H), 7.57-7.62 (m, 1H), 7.70-7.74 (m, 1H), 7.84 (d, 1 H, J = 8.0 Hz), 8.94 (d, 1H, J = 8.0 Hz) and 9.49 (d, 1H, J = 6.7 Hz). 13C NMR (DMSO- d6) δ 30.61, 36.37 (2xC), 44.96, 55.63, 62.63, 72.57, 76.72, 98.48, 121.05, 121.56, 124.61, 125.91, 126.68, 127.87, 128.70, 133.94, 139.97, 151.01, 159.21, 159.68, 161.57 and 165.70.	484.3	O
416		B	1H NMR (DMSO- d6) δ 0.97-1.03 (m, 2H), 1.13-1.22 (m, 3H), 1.92-2.00 (m, 1H), 2.30-2.44 (m, 2H), 3.02 (s, 6H, 2xNCH3) 3.35-3.49 (m, 2H), 3.68-3.77 (m, 2H), 4.22-4.28 (m, 1H), 4.45 (br. s, 1 OH), 4.58 (br. s, 1 OH), 4.64 (br. s, 1 OH), 7.38-7.43 (m, 1 H), 7.49-7.54 (m, 1 H), 8.00 (d, 1 H, J = 8.0 Hz), 8.07 (d, 1H, J = 8.0 Hz) and 9.04 (d, 1H, J = 6.6 Hz). 13C NMR (DMSO- d6) δ 9.91 (2xC), 15.57, 30.55. 36.05 (2xC), 44.88, 55.51, 62.60, 72.42, 76.56, 98.78, 121.24, 121.59, 124.53, 126.05, 133.58, 151.47, 159.08, 159.62, 164.65 and 167.40.	442.2	O
418		—		372.2	O
420		C	1H NMR (DMSO- d6) δ 1.07-1.17 (m, 1H), 1.85-1.94 (m, 1H), 2.17-2.27 (m, 1H), 2.68 (s, 3H), 2.72 (s, 3H), @ 3.05 (s, 6H), @3.40 (m, 2H), 3.65-3.77 (m, 2H), 4.24-4.32 (m, 1H), 4.53 (br. s, 3x OH), 6.80 (d, NH, J = 6.0 Hz), 7.12 (s, 1H) and 7.57 (s, 1H).	448.2	L
419		A	1H NMR (DMSO- d6) δ 0.92 (t, 3H, CH3, J = 7.3 Hz), 1.26-1.33 (m, 1H), 1.52-1.60 (m, 2H), 1.93-2.05 (m, 1H), 2.33-2.43 (m, 1H), 3.20-3.30 (m, 2H), 3.39-3.51 (m, 2H), 3.72-3.80 (m, 1H), 3.81-3.87 (m, 1H), 4.26-4.33 (m, 1H), 4.54 (br. s, OH), 4.64 (br. s, OH), 4.70 (br. s, OH), 7.40-7.49 (m, 1 H), 7.57-7.60 (m, 1H), 7.80 (t, NH, J = 4.6 Hz), 8.00 (d, 1 H, J = 7.9 Hz), 8.10 (d, 1H,J = 7.9 Hz), and 10.60 (d, 1H, J = 6.4 Hz). 13C NMR (DMSO- d6) δ 11.37, 22.06, 30.47, 42.39, 44.90, 56.03, 62.46, 72.44, 76.53, 96.71, 121.09, 121.43, 124.84, 126.25, 131.50, 150.22, 158.70, 160.28, 163.01 and 166.88.	450.2	H
422		A		430.2	O
423		C	1H NMR (CD3OD + DCl) δ 1.28-1.39 (m, 1H), 2.06-2.14 (m, 1H), 2.33-2.42 (m, 1H), 2.85 (s, 3H), 3.30 (s, 6H), 3.50-3.56 (m, 2H), 3.87-3.92 (m, 1H), 3.99-4.02 (m, 1H), 4.49-4.57 (m, 1H), 7.77 (s, 1 H), 8.06 (m, 1H) and 9.06 (s, 1H).	428.2	L
424		A	1H NMR (DMSO- d6) δ 1.25-1.34 (m, 1H), 1.44-1.58 (m, 2H), l.83-2.04 (m, 3H), 2.30-2.40 (m, 1H), 3.29-3.52 (m, 4H), 3.72-3.79 (m, 1H), 3.80-3.90 (m, 3H), 3.91-4.01 (m, 1H), 4.20-4.28 (m, 1H), 4.53 (br. s, OH), 4.60-4.73 (m, 2xOH), 7.38-7.46 (m, 1 H), 7.50-7.60 (m, 1H), 7.80 (d, NH, J = 7.3 Hz), 8.00 (d, 1 H, J = 8.0 Hz), 8.10 (d, 1H, J = 8.0 Hz), and 10.55 (d, 1H, J = 6.3 Hz).	492.3	H
425		A	1H NMR (DMSO- d6 + DCl) δ 1.19-1.32 (m, 1H), 1.50-1.64 (m, 2H), 1.87-2.02 (m, 3H), 2.13-2.25 (m, 1H), 2.49 (s, 3H), 3.29-3.53 (m, 4H), 3.64-3.72 (m, 1H), 3.77-3.92 (m, 3H), 4.05-4.16 (m, 1H), 7.47-7.62 (m, 2 H), 8.12 (d, 1 H, J = 8.0 Hz), and 8.19 (d, 1H, J = 8.0 Hz).	472.3	O
426		A	1H NMR (DMSO- d6 + CD3OD) δ 1.15 (d, 3H, J = 6.5 Hz), 1.16 (d, 3H, J = 6.5 Hz), 1.12-1.26 (m, 1H), 1.93-2.04 (m, 1H), 2.30-2.40 (m, 1H), 3.37-3.48 (m, 2H), 3.72-3.76 (m, 1H), 3.77-3.84 (m, 1H), 4.24-4.31 (m, 1H), 7.38-7.44 (m, 1H), 7.48-7.54 (m, 1H), 7.99 (d, 1 H, J = 8.0 Hz), and 8.05 (d, 1H, J = 8.0 Hz).	450.2	H
427		A		430.2	O
428		A	1H NMR (DMSO- d6) δ 1.24-1.33 (m, 1H), 1.43 (s, 9H), 1.96-2.04 (m, 1H), 2.34-2.42 (m, 1H), 3.40-3.53 (m, 2H), 3.76-3.87 (m, 2H), 4.30-4.37 (m, 1H), 4.56 (br. s, OH), 4.62-4.67 (m, 2x OH), 7.38-7.46 (m, 2 H), 7.50-7.56 (m, 1H), 8.00 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), and 10.61 (d, 1H, J = 5.7 Hz). 13C NMR (DMSO- d6) δ28.72 (3xC), 30.94, 44.90, 50.59, 56.03, 62.49, 72.63, 76.78, 96.30, 121.17, 121.53, 124.92, 126.31, 131.82, 150.30, 157.46, 158.19, 159.94 and 163.11.	464.3	H
429		A	1H NMR (DMSO- d6) δ 1.23-1.30 (m, 1H), 1.41 (s, 9H), 1.93-2.00 (m, 1H), 2.30-2.38 (m, 1H), 2.53 (s, 3H), 3.37- 3.50 (m, 2H), 3.73- 3.78 (m, 2H), 4.26- 4.32 (m, 1H), 4.49 (br. s, OH), 4.65 (br. s, OH), 4.59 (t, OH, J = 5.1 Hz), 6.71 (br. s, NH), 7.34-7.40 (m, 1 H), 7.46-7.51 (m, 1H), 7.96 (d, 1 H, J = 8.0 Hz), 8.05 (d, 1H, J = 8.0 Hz), and 9.77 (br. s, NH).	444.2	O
430		A	1H NMR (DMSO- d6) δ 1.12-1.22 (m, 1H), 1.93-2.01 (m, 1H), 2.19-2.26 (m, 1H), 3.40-3.50 (m, 2H), 3.73-3.83 (m, 2H), 4.28-4.34 (m, 1H), 4.45-4.59 (m, 3H), 4.63 (t, OH, J = 5.2 Hz), 4.67 (d, OH, J = 5.3 Hz), 7.19-7.26 (m, 1H), 7.29-7.45 (m, 5H), 7.49-7.55 (m, 1H), 8.00 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), 8.31 (t, NH, J = 6.0 Hz) and 10.53 (d, NH, J = 6.5 Hz). 13C NMR (DMSO- d6) δ 30.32, 44.23, 44.99, 55.97, 62.42, 72.37, 76.51, 97.20, 121.17, 121.57, 124.97, 126.31, 126.70, 127.53 (2xC), 128.19 (2xC), 132.81, 139.85, 150.28, 157.88, 158.69, 160.32 and 162.94.	498.3	H
431		A		478.3	O
432		A	1H NMR (DMSO- d6) δ 0.91 (t, 3H, J = 7.3 Hz), 1.22-1.28 (m, 1H), 1.30-1.39 (m, 2H), 1.48-1.58 (m, 2H), 1.93-2.03 (m, 1H), 2.31-2.43 (m, 1H), 3.25-3.37 (m, 2H), 3.40-3.51 (m, 2H), 3.74-3.80 (m, 1H), 3.82-3.86 (m, 1H), 4.28-4.38 (m, 1H), 4.52 (d, OH, J = 4.8 Hz), 4.64 (t, OH, J = 5.1 Hz), 4.69 (d, OH, J = 5.4 Hz), 7.40-7.46 (m, 1H), 7.50-7.56 (m, 1H), 7.77 (d, NH, J = 5.4 Hz), 8.00 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), and 10.60 (d, NH, J = 6.3 Hz). 13C NMR (DMSO- d6) 513.63, 19.52, 30.48, 30.87, 40.25, 44.94, 56.03, 62.48, 72.38, 76.50, 96.69, 121.09, 121.42, 124.83, 126.24, 132.69, 150.22, 157.68. 158.65, 160.31 and 163.02.	464.3	H
433		A	1H NMR (DMSO- d6) δ 0.87 (t, 3H, J = 6.5 Hz), 1.21-1.37 (m, 5H), 1.49-1.60 (m, 2H), 1.93-2.03 (m, 1H), 2.30-2.43 (m, 1H), 3.25-3.39 (m, 2H), 3.40-3.50 (m, 2H), 3.74-3.80 (m, 1H), 3.82-3.86 (m, 1H), 4.28-4.38 (m, 1H), 4.52 (d, OH, J = 4.9 Hz), 4.65 (t, OH, J = 5.3 Hz), 4.69 (d, OH, J = 5.4 Hz), 7.40-7.46 (m, 1H), 7.50-7.55 (m, 1H), 7.78 (d, NH, J = 5.7 Hz), 8.00 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), and 10.60 (d, NH, J = 6.3 Hz).	478.3	H
434		A		444.2	O
435		A		458.3	O
436		A	1H NMR (DMSO- d6) δ 0.92 (s, 9H), 1.24-1.32 (m, 1H), 1.93-2.05 (m, 1H), 2.33-2.44 (m, 1H), 3.17-3.28 (m, 2H), 3.40-3.53 (m, 2H), 3.74-3.86 (m, 2H), 4.26-4.32 (m, 1H), 4.54 (d, OH, J = 5.1 Hz), 4.60-4.67 (m, 2x OH), 7.39-7.40 (m, 1H), 7.49-7.56 (m, 1H), 7.80 (t, NH, J = 6.4 Hz), 7.99 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), and 10.57 (d, 1H, J = 6.3 Hz). 13C NMR (DMSO- d6) 827.36 (3xC), 30.56, 32.51, 44.84, 51.61, 55.96, 62.31, 72.47, 76.56, 96.77, 121.09, 121.42, 124.83, 126.24, 132.66, 150.22, 157.67, 159.36, 160.11 and 162.97.	478.3	H
437		A	1H NMR (DMSO- d6) δ 0.90 (s, 9H), 1.16-1.31 (m, 1H), 1.93-2.04 (m, 1H), 2.32-2.45 (m, 1H), 2.56 (s, 3H), 3.16-3.30 (m, 2H), 3.38-3.54 (m, 2H), 3.70-3.86 (m, 2H), 4.22-4.33 (m, 1H), 4.51-4.73 (m, 3x OH), 7.24 (br. s, NH), 7.36-7.42 (m, 1H), 7.49-7.54 (m, 1H), 7.98 (d, 1 H, J = 8.0 Hz), 8.07 (d, 1H, J = 8.0 Hz), and 9.82 (d, 1H, J = 5.0 Hz).	458.3	O
438		A	1H NMR (DMSO- d6) δ 1.15 (d, 3H, J = 6.6 Hz), 1.20-1.29 (m, 1H), 1.93-2.03 (m, 1H), 2.31-2.43 (m, 1H), 3.29 (s, 3H), @3.30 (m, 1H), 3.41- 3.51 (m, 3H), 3.73- 3.79 (m, 1H), 3.81 (m, 1H), 4.16-4.24 (m, 1H), 4.26-4.33 (m, 1H), 4.52 (d, OH, J = 4.1 Hz), 4.65 (t, OH, J = 4.3 Hz), 4.68 (d, OH, J = 4.3 Hz), 7.40-7.46 (m, 1H), 7.50-7.56 (m, 1H), 7.65 (d, NH, J = 7.8 Hz), 8.01 (d, 1 H, J = 8.0 Hz), 8.09 (d, 1H, J = 8.0 Hz), and 10.6 (d, 1H, J = 6.2 Hz).	480.3	H
439		A	1H NMR (DMSO- d6) δ 1.14 (d, 3H, J = 6.7 Hz), @ 1.20 (m, 1H), 1.92-2.01 (m, 1H), 2.28-2.41 (m, H), 2.56 (s, 3H), 3.23-3.30 (m, 1H), 3.28 (s, 3H), 3.37- 3.51 (m, 3H), 3.70- 3.81 (m, 2H), 4.17- 4.33 (m, 2H), 4.46 (br. s, OH), 4.57-4.63 (m, 2x OH), 7.03 (br. s, NH), 7.37-7.42 (m, 1H), 7.49-7.54 (m, 1H), 7.98 (d, 1 H, J = 7.9 Hz), 8.07 (d, 1H, J = 7.9 Hz), and 9.79 (br. s, NH).	460.3	O
440		B	1H NMR (DMSO- d6) δ 1.22-1.29 (m, 1H), 1.46 (d, 3H, J = 7.0 Hz), 2.00-2.09 (m, 1H), 2.44-2.53 (m, 1H), 3.40-3.54 (m, 2H), 3.71-3.80 (m, 2H), 4.20-4.28 (m, 1H), 4.52 (d, OH, J = 4.6 Hz), 4.55 (d, OH, J = 4.6 Hz), 4.67 (t, OH, J = 5.0 Hz), 5.08-5.18 (m, 1H), 7.17-7.24 (m, 1H), 7.28-7.37 (m, 2H), 7.39-7.47 (m, 3H), 7.49-7.55 (m, 1H), 8.00 (d, 1 H, J = 8.0 Hz), 8.08 (d, 1H, J = 8.0 Hz), 8.35 (d, NH, J = 8.0 Hz) and 10.6 (d, 1H, J = 6.2 Hz).	512.3	H
441		—	1H NMR (DMSO- d6) δ 1.22-1.28 (m, 1H), 1.45 (d, 3H, J = 7.0 Hz), 1.99-2.08 (m, 1H), 2.42-2.51 (m, 1H), 2.52 (s, 3H), 3.39-3.57 (m, 2H), 3.67-3.76 (m, 2H), 4.19-4.28 (m, 1H), 4.42 (br. s, OH), 4.50 (br. s, OH), 4.61 (br. s, OH), 5.10-5.19 (m, 1H), 7.16-7.22 (m, 1H), 7.25-7.33 (m, 2H), 7.36-7.54 (m, 4H), 7.79 (d, NH, J = 8.0 Hz), 7.97 (d, 1 H, J = 7.8 Hz), 8.06 (d, 1H, J = 7.9 Hz) and 9.69 (d, 1H, J = 4.5 Hz).	492.3	O
501		A	1H NMR (DMSO- d6) δ 0.98-1.06 (m, 1H), 1.2-1.3 (t, 3H), 1.78-1.87 (m, 1H), 2.04- 2.2 (m, 1H), 2.79- 2.84 (m, 2H), 3.22-3.25 (s, 3H), 3.40-3.50 (m, 4H), 3.60-3.70 (m, 2H), 4.20-4.38 (m, 2H), 4.45-4.50 (m, 2H), 6.50-6.7 (m, 1 H), 6.95-6.97 (s, 1 H), 7.25-7.45 (m, 1 H), 7.5- 7.7 (m, 1 H) and 8.78-8.8 (m, 1H).	478.3	Q
502		A	1H NMR (DMSO- d6) δ 0.98-1.06 (m, 7H), 1.2-1.3 (t, 3H), 1.78- 1.87 (m, 1H), 2.04- 2.2 (m, 1H), 2.79- 2.84 (m, 2H), 3.0-3.1 (m, 1H), 3.59-3.65 (m, 2H), 3.70-3.80 (m, 2H), 4.20-4.4 (m, 2H), 4.45-4.60 (m, 2H), 6.60- 6.7 (m, 1 H), 6.95-6.97 (s, 1 H), 7.35-7.45 (m, 1 H), 7.5- 7.6 (m, 1 H) and 8.78-8.8 (m, 1H).	462.3	Q
503		A	1H NMR (DMSO- d6) δ 0.19-0.22 (m, 2H), 0.38-0.44 (m, 2H), 1.0-1.1 (m, 1H), 1.2-1.3 (t, 3H), 1.32-1.36 (m, 1H), 1.78-1.87 (m, 1H), 2.04- 2.2 (m, 1H), 2.75-2.85 (m, 2H), 3.1-3.2 (m, 2H), 3.59-3.75 (m, 2H), 4.20-4.4 (m, 2H), 4.45-4.55 (m, 2H), 6.50-6.65 (m, 1 H), 6.95-7.0 (s, 1 H), 7.40-7.58 (m, 1 H), 7.5- 7.6 (m, 1 H) and 8.75-8.8 (m, 1H).	474.3	Q
504		A	1H NMR (DMSO- d6) δ 0.2-0.25 (m, 2H), 0.4-0.45 (m, 2H), 1.0-1.15 (m, 1H), 1.15-1.3 (m. 1H), 1.9-2.05 (m, 1H), 2.3-2.42 (m. 1H), 3.1-3.25 (m, 2H), 3.40-3.5 (m, 2H), 3.72-3.85 (m, 2H), 4.25-4.4 (m, 1H), 4.4-4.5 (m, 1H), 4.6-4.7 (m, 2H), 7.4- 7.55 (m, 2 H), @7.6, 7.8 and 8.2 (m, NHCH2cyclopropyl), 7.95-8.1 (m, 2H), 10.55-10.6 (m, 1H).	462.3	H
505		A	1H NMR (DMSO- d6) δ 0.2-0.25 (m, 2H), 0.4-0.45 (m, 2H), 1-0-1.15 (m, 1H), 1.15-1.3 (m, 1H), 1.9-2.05 (m, 1H), 2.3-2.42 (m, 1H), 2.55 (s, 3H), 3.1-3.25 (m, 2H), 3.40-3.5 (m, 2H), 3.72-3.85 (m, 2H), 4.25-4.4 (m, 1H), 4.4-4.5 (m, 1H), 4.6- 4.7 (m, 2H), 7.25- 7.55 (m, 2 H), 7.85- 8.0 (m, NHCH2cyclopropyl), 8.0-8.1 (m, 2H), 9.4- 9.8 (m, 1H).	442.2	I
506		A	1H NMR (DMSO- d6) δ 0.79-0.80 (t, 3H), 1.0-1.15 (m, 2H), 1.35 (s, 6H), 1.8-2.05 (m, 2H), 2.3- 2.42 (m, 1H), 3.4-3.5 (m, 3H), 3.75-3.85 (m, 2H), 4.2-4.6 (m, 1H), 4.6- 4.7 (m, 2H), 7.25 (bs, 1H), 7.39-7.55 (m, 2H), 7.95-8.1 (m, 2H), 10.6 (bs, 1H)	478.3	H
507		A	1H NMR (DMSO- d6) δ 1.25-1.45 (m, 2H), 1.8-2.0 (m, 4 H), 2.0 (s, 3H), 2.3- 2.4 (m, 1H), 2.6-2.8 (m, 1H), 3.0-3.2 (m, 1H), 3.4-3.55 (m, 2H), 3.75-3.85 (m, 4H), 3.9-4.0 (m, 1H), 4.2-4.5 (m, 3H), 4.6- 4.7 (m, 2H), 7.4-7.6 (m, 2H), 7.8-7.82 (m, 1H), 8.0-8.1 (m, 2H), 10.2-10.6 (m, 1H).	533.3	H
508		A	1H NMR (DMSO- d6) δ 1.0-1.1 (m, 1H), 1.2-1.3 (t, 3H), 1.78-1.87 (m, 1H), 2.05 (s, 3H), 2.04-2.2 (m, 1H), 2.79-2.84 (m, 2H), 3.22-3.25 (s, 3H), 3.40-3.50 (m, 4H), 3.60-3.70 (m, 2H), 4.20-4.38 (m, 2H), 4.45-4.50 (m, 2H), 6.20-6.25 (m, 1 H), 6.85-6.90 (s, 1 H), 7.45-7.5 (m, 1H), 7.5-7.7 (m, 2 H) and 8.78-8.8 (m, 1H).	458.3	R
509		A	1H NMR (DMSO- d6) δ 0.19-0.22 (m, 2H), 0.38-0.44 (m, 2H), 1.0-1.1 (m, 1H), 1.25 (m, 1H), 1.2-1.3 (t, 3H), 1.78- 1.87 (m, 1H), 2.04- 2.2 (m, 1H), 2.05 (s, 3H), 2.75-2.85 (m, 2H), 3.1-3.2 (m, 2H), 3.59-3.75 (m, 2H), 4.20-4.4 (m, 2H), 4.45-4.55 (m, 2H), 6.10-6.20 (m, 1 H), 6.85-6.9 (s, 1 H), 7.45-7.6 (m, 1 H), 7.5-7.6 (m, 1 H) and 8.75-8.8 (m, 1H).	454.2	R
510		C	1H NMR (DMSO- d6) δ 1.25-1.45 (m, 1H), 1.8-2.0 (m, 2 H), 2.0-2.2 (m, 2H), 2.3-2.4 (m, 1H), 3.0- 3.2 (m, 2H), 3.4-3.55 (m, 4H), 3.75-3.85 (m, 2H), 3.9-4.0 (m, 1H), 4.2-4.5 (m, 2H), 7.4- 7.6 (m, 2H), 7.8- 7.82 (m, 1H), 8.0-8.1 (m, 2H), 8.4-8.5 (bs, 1H), 8.6-8.8 (bs, 1H), 10.2-10.6 (m, 1H).	491.3	H
511		A	1H NMR (DMSO- d6) δ 0.8-0.9 (m, 3H), 1.0-1.1 (m, 1H), 1.2-1.4 (m, 7H), 1.4- 1.6 (m, 2H), 1.8-2.2 (m, 2H), 2.75-2.85 (m, 2H), 3.2-3.25 (m, 2H), 3.6-3.8 (m, 2H), 4.2-4.4 (m, 2H), 4.45-4.55 (m, 2H), 6.5-6.65 (m, 1H), 6.95 (s, 1H), 7.45-7.5 (m, 2H), 8.75-8.8 (m, 1H).	490.4	Q
512		A	1H NMR (DMSO- d6) δ 1.0-1.1 (m, 4H), 1.1-1.15 (t, 3H), 1.2-1.25 (t, 3H), 1.8- 1.85 (m, 1H), 2.0-2.2 (m, 1H), 2.8-2.85 (m, 2H), 3.35-3.5 (m, 5H), 3.6-3.75 (m, 2H), 4.2-4.4 (m, 2H), 4.45-4.55 (m, 2H), 6.5-6.7 (m, 1H), 6.95 (s, 1H), 7.2-7.4 (m, 1H), 7.5-7.55 (m, 1H), 8.8-8.85 (m, 1H).	492.3	Q
513		A	1H NMR (DMSO- d6) δ 0.79-0.80 (t, 3H), 1.1-1.25 (m, 1H), 1.35-1.4 (m, 7H), 1.8-1.9 (m, 1H), 1.9-2.0 (m, 1H), 2.3- 2.42 (m, 1H), 2.5- 2.55 (s, 3H), 3.34-3.5 (m, 2H), 3.75-3.8 (m, 2H), 4.2-4.3 (m, 1H), 4.45-4.65 (m, 3H), 7.35-7.4 (m, 1H), 7.45-7.5 (m, 1H), 7.55-7.65 (m, 1H), 7.95-8.1 (m, 2H), 8.2-8.25 and 9.8 (m, 1H)	458.2	I
514		A	1H NMR (DMSO- d6) δ 0.8-0.9 (m, 3H), 1.0-1.1 (m, 1H), 1.2-1.4 (m, 7H), 1.4- 1.6 (m, 2H), 1.8-1.9 (m, 1H), 2.05 (s, 3H), 2.1-2.2 (m, 1H), 2.75-2.85 (m, 2H), 3.2-3.25 (m, 2H), 3.6-3.7 (m, 2H), 4.2- 4.35 (m, 2H), 4.45- 4.55 (m, 2H), 6.2-6.3 (m, 1H), 6.85 (s, 1H), 7.45-7.5 (m, 2H), 8.75-8.8 (m, 1H).	470.3	R
515		A	1H NMR (DMSO- d6) δ 1.0-1.1 (m, 1H), 1.1-1.15 (t, 3H), 1.2-1.25 (t, 3H), 1.8- 1.85 (m, 1H), 2.0 (s, 3H), 2.0-2.2 (m, 1H), 2.8-2.85 (m, 2H), 3.35-3.5 (m, 6H), 3.6-3.75 (m, 2H), 4.2-4.4 (m, 1H), 4.45-4.55 (m, 2H), 6.2-6.3 (bs, 1H), 6.95 (s, 1H), 7.45-7.5 (m, 1H), 7.5-7.55 (m, 1H), 8.8-8.85 (m, 1H).	472.3	R
516		A	1H NMR (DMSO- d6) δ 0.8-1.1 (m, 1H), 1.2-1.3 (m, 3H), l.8-l.9 (m, 1H), 2.0- 2.2 (m, 1H), 2.8-2.85 (m, 2H), 3.6-3.8 (m, 2H), 4.0-4.15 (m, 1H), 4.2-4.4 (m, 2H), 4.4-4.5 (m, 2H), 6.8- 6.85 (bs, 1H), 7.0 (s, 1H), 7.2-7.4 (m, 1H), 7.5-7.55 (m, 1H), 8.8-8.85 (s, 1H).	502.3	Q
517		A	1H NMR (DMSO- d6) δ 1.0-1.1 (m, 1H), 1.2-1.3 (m, 3H), 1.8-1.9 (m, 1H), 2.05-2.1 (s, 3H), 2.1- 2.35 (m, 1H), 2.8- 2.85 (m, 2H), 3.3-3.4 (m, 2H), 3.6-3.8 (m, 2H), 4.0-4.25 (m, 2H), 4.2-4.5 (m, 2H), 4.4- 4.5 (m, 2H), 6.3- 6.4 (bs, 1H), 6.9 (s, 1H), 7.5 (m, 1H), 7.5-7.65 (m, 1H), 8.7-8.75 (s, 1H).	482.3	R
518		A		476.3	Q
519		A		456.3	R
520		A		516.3	Q
521		A		496.3	R
128		C		496.3	I
129		A		486.3	H
130		C		466.3	I
131		A		504.3	H
132		B		484.3	I
133		C		478.3	Z (steps 4-6)
134		C		552.3	Y
135		C		538.3	Y
136		B		506.3	Z3
137		B		438.2	Z (steps 4-7)
138		A		512.3	Y
139		B		498.3	Y
140		B		562.3	Y
141		B		534.3	Y
142		B		522.3	Y
143		B		494.3	Y
230		A		480.3	H
231		A		460.3	I
232		A	1H NMR (DMSO) δ 1.04-1.22 (m, 1H), 1.88-2.00 (m, 1H), 2.11-2.20 (m, 1H), 3.40-3.48 (m, 1H), 3.72-3.81 (m, 1H), 4.22-4.38 (m, 1H), 4.47-4.57 (m, 2H), 4.60-4.75 (m, 2H), 7.13-7.22 (m, 2H), 7.25- 7.32 (m, 1 H), 7.39-7.57 (m, 2H), 7.95-8.04 (m, 1H), 8.06-8.13 (m, 1H), 8.26- 8.32 (m, 1H) 10.32-10.36 (m, 1 H).		H
233		A	1H NMR (DMSO) δ 0.98-1.23 (m, 1H), 1.89-1.99 (m, 1H), 2.07-2.24 (m, 1H), 2.49 (s, 3H), 3.38- 3.47 (m, 1H) 3.72- 3.81 (m, 1H), 4.18- 4.33 (m, 1H) 4.36- 4.53 (m, 1H), 4.53- 4.71 (m, 2H), 7.10- 7.18 (m, 1H), 7.20- 7.29 (m, 2H), 7.31- 7.44 (m, 2H), 7.46- 7.54 (m, 1H), 7.83- 7.93 (m, 1H), 7.93- 8.03 (m, 1H) 8.06 (d, 1H, J = 8.0 Hz) 9.65- 9.74 (m, 1 H).	496.4	I
234		A	1H NMR (DMSO) δ 1.08-1.22 (m, 1H), 1.88-1.99 (m, 1H), 2.09-2.22 (m, 1H), 3.47-3.70 (m, 2H) 3.82-4.21 (m, 2H), 4.21-4.30 (m, 1H) 4.32-4.40 (m, 1H), 4.46-4.70 (m, 4H), 7.00-7.08 (m, 1H), 7.11-7.24 (m, 2H), 7.31-7.46 (m, 2H), 7.49-7.55 (m, 1H), 8.04-8.06 (m, 1H), 8.28-8.35 (m, 1H) 10.47-10.54 (m, 1 H).	516.3	H
235		A		536.3	Z3
236		C	1H NMR (CDCl3) δ 1.22 (s, 3H), 1.44 (s, 3H), 1.60-1.66 (m, 1H), 2.27-2.44 (m, 1H), 2.67 (s, 3H), 3.68-3.79 (m, 2H), 4.47-4.54 (m, 2H), 4.56-4.60 (m, 1H), 4.89-5.00 (m, 2H), 5.47-5.56 (m, 1H), 7.31-7.39 (m, 2H), 7.44-7.51 (m, 2H), 7.64-7.72 (m, 2H), 7.87 (d, 1H J = 8.0 Hz), 7.96 (d, 1H J = 8.0 Hz) 9.66-9.79 (m, 1H).	586.3	Z3
237		B	1H NMR(CDCl3) δ 1.22 (s, 3H), 1.47 (s, 3H), 1.61-1.71 (m, 1H), 2.32-2.54 (m, 1H), 2.66 (s, 3H), 3.71-3.81 (m, 2H), 4.42-4.50 (m, 1H), 4.51-4.56 (m, 1H), 4.57-4.62 (m, 1H), 4.77-4.83 (m, 1H), 5.51-5.62 (m, 1H), 7.34-7.356 (m, 4H), 7.57-7.63 (m, 1H), 7.69-7.73 (m, 1H), 7.87 (m, 1H J = 8.0 Hz), 7.96 (d, 1H J = 8.0 Hz) 9.61-9.80 (m, 1H).	586.3	Z3
238		A		496.3	Z3
239		B		546.3	Z3
240		A		546.3	Z3
241		B	1H NMR (CDCI3) δ 1.22 (s, 3H), 1.46 (s, 3H), 1.62-1.68 (m, 1H), 2.29-2.47 (m, 1H), 2.67 (s, 3H), 3.70-3.80 (m, 2H), 4.40-4.60 (m, 3H), 4.73-4.86 (m, 2H), 5.42-5.66 (m, 1H), 7.33-7.40 (m, 1H), 7.44-7.60 (m, 5H), 7.87 (d, 1H J = 8.0 Hz), 7.96 (d, 1H J = 8.0 Hz) 9.59-9.76 (m, 1H).	586.3	Z3
242		A		546.3	Z3
243		A	1H NMR (CDCl3) δ 1.24 (s, 3H), 1.48 (s, 3H), 1.59-1.72 (m, 1H), 2.31-2.50 (m, 2H), 2.66 (s, 3H), 3.70-3.80 (m, 2H), 4.44-4.56 (m, 2H), 4.56-4.61 (m, 1H), 4.65-4.81 (m, 2H), 5.51-5.62 (m, 1H), 6.89-6.97 (m, 1H), 7.09-7.19 (m, 2H), 7.32-7.33 (m, 1H), 7.39-7.45 (m, 1H), 7.69 (d, 1H J = 8.0 Hz), 7.93 (d, 1H J = 8.0 Hz), 9.62- 9.77 (m, 1H).	536.3	Z3
244		A		496.3	Z3
245		C		499.3	Z3
246		C		459.3	Z3
247		A		513.3	Z (steps 4-7)
248		A		541.3	Z3
249		C		570.3	Z3
250		B		530.3	Z3
251		A		5156.3	H
252		A		501.3	Z3
253		B	1H NMR (CDCl3) 1.26 (s, 3H), 1.47 (s, 3H), 1.63-1.81 (m, 1H), 2.33-2.46 (m, 2H), 2.46-2.56 (m, 1H), 2.65 (s, 3H), 3.42-3.48 (m, 2H), 3.49-3.57 (m, 1H), 3.62-3.72 (m, 2H), 4.40-4.54 (m, 2H), 4.57-4.64 (m, 1H), 4.65-4.81 (m, 2H), 5.00-5.14 (m, 2H), 5.36-5.45 (m, 1H), 5.79-6.04 (m, 1H), 7.29-7.34 (m, 6H), 7.34-7.40 (m, 3H). 7.45-7.50 (m, 2H), 7.87 (d, 1H J = 8.0 Hz), 7.96 (d, 1H J = 8.0 Hz), 9.71-9.86 (m, 1H).	605.3	Z3
254		B		565.3	Z3
255		A		543.3	Z3
256		A		503.3	Z3
257		A		549.3	Z3
258		B		509.3	Z3
259		A		489.4	Z (steps 4-7)
260		A		499.4	Z (steps 4-7)
321		C	1H NMR (DMSO- d6) δ 0.84-0.92 (m, 3H, CH3), 1.00-1.09 (m, 1H), 1.26-1.38 (m, 4H), 1.50-1.63 (m, 2H), 1.79-1.91 (m, 1H), 2.04-2.19 (m, 1H), 3.21-3.39 (m, 4H), 3.56-3.73 (m, 2H), 4.27-4.5 l (m, 4H, including 3xOH), {6.73 (d, J = 6.9 Hz) and 6.94 (d, J = 6.9 Hz, 1NH)}, {7.42 (br. s) and 7.66 (t, J = 5.5 Hz, 1NH)}, 7.47-7.52 (m, 1 H), 7.54-7.58 (m, 1H), 8.09 (d, 1 H, J = 7.9 Hz) and 8.14 (d, 1H, J = 7.9 Hz), 19F NMR (DMSO- d6) δ-62.55 and -62.96.	512.3	S
322		A		504.3	H
323		A		484.3	O
324		C	1H NMR (DMSO- d6) δ 1.13-1.21 (m, 1H), 1.89-1.98 (m, 1H), 2.18-2.26 (m, 1H), 2.51 (s, CH3), 3.31-3.43 (m, 2H), 3.36 (s, CH3), 3.66- 3.70 (m, 1H), 3.75- 3.80 (m, 1H), 4.33- 4.41 (m, 1H), 4.49 (d, J = 5.2 Hz, 1xOH), 4.57 (t, J = 5.0 Hz, 1xOH), 4.65 (d, J = 5.8 Hz, 1xOH), 7.54- 7.59 (m, 1H) 7.60- 7.66 (m, 1H), 8.18 (d, 1 H, J = 8.1 Hz), 8.24 (d, 1H, J = 8.1 Hz) and 8.76 (d, J = 8.1 Hz, NH).	451.2	T
325		A		472.3	U
326		B	1H NMR (DMSO- d6) δ 1.14-1.21 (m, 1H), 1.92-2.00 (m, 1H), 2.25-2.33 (m, 1H), 2.51 (s, CH3), 2.52 (s, CH3), 3.35- 3.46 (m, 2H), 3.70- 3.80 (m, 2H), 4.34- 4.42 (m, 1H), 4.48 (d, J = 5.0 Hz, 1xOH), 4.60 (t, J = 5.2 Hz, 1xOH), 4.64 (d, J = 5.6 Hz, 1xOH), 7.48- 7.53 (m, 1H) 7.56- 7.61 (m, 1H), 8.12 (d, 1 H, J = 7.8 Hz), 8.18 (d, 1H, J = 7.8 Hz) and 9.08 (d, J = 7.1 Hz, NH).	419.2	From removal of dimethyl- ketal on 252a as described in pro- cedure U
327		A	1H NMR (DMSO- d6) δ 0.89 (s, 3H, CH3), 1.25-1.40 (m, 5H), 1.49-1.61 (m, 3H), 1.87-1.97 (m, 1H), 2.21-2.38 (m, 1H), 2.55 (s, 3H, CH3), 3.19-3.38 (m, 2H), 3.72-3.87 (m, 1H), 3.90-3.99 (m, 1H), 4.22- 4.33 (m, 1H), 4.37-4.52 (m, 1xOH), 4.77 (d, J = 5.6 Hz, 1xOH), {7.12 (br. s) and 7.24 (br. s), NH}, {7.36-7.44 (m) and 7.58-7.63 (m), 1H}, {7.48-7.54 (m) and 7.63-7.68 (m), 1H}, {7.96 (d, J = 7.9 Hz) and 8.21 (d, J = 7.9 Hz), 1H}, {8.08 (d, J = 7.9 Hz) and 8.27 (d, J = 7.9 Hz), 1H} and {9.46 (br. s) and 9.88 (br. s), NH}.	428.3	V
328		A	1H NMR (DMSO- d6) δ 1.20 (s, CH3), 1.30 (s, CH3), 1.54-1.64 (m, 1H), 2.11-2.20 (m, 1H), 2.25-2.36 (m, 1H), 2.53 (s, CH3), 3.45-3.54 (m, 2H), 3.41-4.57 (m, 3H, including 2xOH), 4.65-4.82 (m, 3H, including 1xOH), 7.14 (dd, 1H, J = 5.0 and 3.4 Hz), 7.06 (br. s, 1H), 7.36 (dd, 1H, J = 5.0 and 1 Hz), 7.41-7.46 (m, 1H) 7.51-7.56 (m, 1H), 8.02 (br. s, 1H), 8.07 (d, 1 H, J = 8.0 Hz), 8.11 (d, 1 H, J = 8.0 Hz), and 9.62 (br. s, NH).	524.3	U
329		A		484.3	U
330		A		524.3	U
331		A		484.3	U
332		C		508.3	V
333		A	1H NMR (CDCl3 and CD3OD) δ 1.53-1.66 (m, 2H), 1.67-1.83 (m, 2H), 1.91-2.01 (m, 1H), 2.14-2.23 (m, 1H), 2.62 (s, 3H, CH3), 3.98-4.07 (m, 1H), 4.12-4.20 (m, 1H), 4.65-4.79 (m, 2H), 6.86 (dd, 1H, J = 5.1 and 3.4 Hz), 6.95- 6.98 (m, 1H), 7.10 (dd, 1H, J = 5.1 and 1.2 Hz), 7.27-7.32 (m, 1H) 7.38-7.42 (m, 1H), 7.79-7.81 (m, 1H), 7.82-7.83 (m, 1H) and 7.84 (app. d, 1 H, J = 8.1 Hz).	438.2	X
334		C		534.3	V
335		C		548.3	W
336		A		454.2	V
337		A	1H NMR (DMSO- d6) δ 0.92-1.01 (m, 1H), 1.00 (d, 3H, CH3, J = 6.9), 1.81-1.90 (m, 1H), 2.16-2.25 (m, 1H), 2.45 (s, 3H, CH3), 3.40 (app. t, 1H, J = 6 Hz), 3.87 (app. t, 1H, J = 6 Hz), 4.40- 4.49 (m, 1H), 4.74- 4.92 (m, 2H), 7.00 (dd, 1H, J = 5.1 and 3.4 Hz), 7.16 (dd, 1H, J = 3.4 and 1 Hz), 7.46 (dd, 1H, J = 5.1 and 1.1 Hz), 7.51-7.56 (m, 1H) 7.59-7.64 (m, 1H), 8.14 (d, 1H, J = 8.0 Hz), 8.22 (d, 1 H, J = 8.0 Hz), 8.44 (br. s, NH), and 9.37 (br. s, NH).	468.3	W
338		A	1H NMR(CDCl3) δ 1.73-1.83 (m, 1H), 1.86-1.98 (m, 1H), 2.04-2.12 (m, 1H), 2.21-2.31 (m, 1H), 2.42-2.51 (m, 1H), 2.66-2.75 (m, 1H), 2.70 (s, 3H, CH3), 4.43-4.52 (m, 1H), 4.74-4.84 (m, 2H), 5.50 (br. s, 1H, NH), 6.95 (dd, 1H, J = 5.1 and 3.5 Hz), 6.99- 7.02 (m, 1H), 7.20 (dd, 1H, J = 5.1 and 1.2 Hz), 7.34-7.38 (m, 1H) 7.46-7.50 (m, 1H), 7.87 (d, 1H, J = 8.1 Hz), 8.02 (d, 1 H, J = 8.1 Hz) and 10.20 (br. s, 1H, NH).	468.3	X
339		A		553.3	Combi- nation of M and Y
340		A		513.3	Combi- nation of M and Y
341		A		5374.3	Y
342		A		497.3	Y
343		C		531.3	Y
344		A		491.3	Y
345		A		590.6	Y
346		A		550.3	Y
347		A		606.3	Combi- nation of A-2 and Y
348		A		566.3	Combi- nation of A-2 and Y
349		B		547.3	Combi- nation of A-2 and Y
350		—		507.3	Combi- nation of A-2 and Y
351		—		522.3	U
442		—		512.4	H
443		—		492.3	O
444		A		512.3	H
445		A		492.3	O
446		A		518.3	N
447		A		506.3	H
448		A		498.3	O
449		A		486.3	O
450		A		490.3	L
451		A		476.3	L
452		A		470.3	O
453		A		456.3	O
454		A		492.3	H
455		A		472.3	O
456		A		502.3	L
457		A		482.3	O
458		A		518.3	L
459		A		498.3	O
460		A		516.3	L
461		A		496.3	O
462		B		519.3	U
463		A		519.3	U
464		A		519.3	U
465		A		479.3	U
466		A		479.3	U
467		—		479.3	U
468		A		521.2	U
469		A		508.3	O
470		A		468.3	U
471		A		514.2	U
472		A		525.4	U
473		A		474.2	U
474		A		485.4	U
475		B		574.5	U
476		A		538.5	U
477		A		538.5	U
478		A		534.5	U
479		A		498.5	U
480		A		498.2	U
481		C		535.5	U
482		B		495.2	U
483		B		548.2	U
484		A		495.2	U
485		B		532.2	U
486		A		492.2	U
487		C		532.2	U
488		A		492.2	U
489		B		532.2	U
490		A		492.2	U
491		B		523.2	U
492		A		483.2	U
493		A		483.2	U
494		C		539.2	U
495		A		499.2	U
496		A		538.2	U
497		A		498.2	U
498		C		533.2	U
499		A		493.2	U
500		A		578.2	U
701		A		538.2	U
702		A		535.5	U
703		A		495.2	U
704		A		520.2	U
705		A		480.2	U
706		B		539.2	U
707		A		499.2	U
708		A		578.2	U
709		A		538.2	U
710		A		608.2	U
711		A		568.2	U
712		A		546.2	U
713		A		506.2	U
714		B		526.2	Combi- nation of M and Y
715		A		486.2	Combi- nation of M and Y
716		B		502.2	U
717		A		480.2	U
522		B		420.2	Q
523		A	1H NMR (DMSO- d6) 0.25 (m, 2H), 0.5 (m, 2H), 1.0-1.1 (m, 1H), 1.9-2.0 (m, 1H), 2.0-2.2 (m, 1H), 2.4 (s, 3H), 3.2-3.4 (m, 4H), 3.6-3.8 (m, 2H), 4.2-4.4 (m, 2H), 4.4- 4.5 (m, 2H), 8.0 (m, 1H), 8.4 (m, 1H), 8.6 (m, 1H), 8.95 (m, 1H), 9.5 (s, 1H).	443.3	Z
524		A		440.3	Y
524		A	1H NMR (DMSO- d6) 0.9 (s, 9H), 1.0- 1.1 (m, 1H), 1.2-1.3 (m, 3H), 1.9-2.0 (m, 1H), 2.0-2.2 (m, 1H), 2.4 (m, 3H), 3.0-3.2 (m, 2H), 3.2-3.4 (m, 4H), 3.6-3.8 (m, 2H), 4.4-4.5 (m, 2H), 7.4 (s, 1H), 8.0 (m, 1H), 8.15 (m, 1H), 8.2 (m, 1H) 9.3 (s, 1H).	470.4	Y
525		A	1H NMR (DMSO- d6) 1.0 (t, 3H), 1.0- 1.1 (m, 1H), 1.9-2.0 (m, 1H), 2.0-2.2 (m, 1H), 2.4 (s, 3H), 3.4 (m, 3H), 3.6-3.7 (m, 6H), 3.7-3.8 (m, 2H), 4.4-4.5 (m, 2H), 7.8 (m, 1H), 8.4 (m, 1H), 8.6 (m, 1H), 8.95 (m, 1H), 9.5 (s, 1H).	461.5	Z
526		A	1H NMR (DMSO- d6) 1.0-1.1 (m, 1H), 1.9-2.0 (m, 1H), 2.0- 2.2 (m, 1H), 2.4 (s, 3H), 3.3-3.4 (m, 6H), 3.6-3.7 (m, 4H), 3.7- 3.8 (m, 2H), 4.4-4.5 (m, 2H), 7.8 (m, 1H), 8.4 (m, 1H), 8.6 (m, 1H), 8.95 (m, 1H), 9.5 (s, 1H).	447.4	Z
527		A	1H NMR (DMSO- d6) δ 1.0-1.1 (m, 1H), 1.2-1.3 (m, 3H), 1.8- 1.9 (m, 1H), 2.1-2.35 (m, 1H), 2.4 (s, 3H), 3.0 (s, 3H), 3.0-3.2 (m, 2H), 3.4-3.5 (m, 2H), 3.6-3.8 (m, 3H), 4.4-4.5 (m, 2H), 7.4 (s, 1H), 7.5-8.0 (m, 3H), 9.3 (s, 1H).	414.5	Y
528		B	1H NMR (DMSO- d6) 0.25 (m, 2H), 0.5 (m, 2H), 1.0-1.1 (m, 1H), 1.2 (m, 1H), 1.9-2.0 (m, 1H), 2.25- 2.3 (m, 1H), 2.7 (s, 3H), 3.2-3.5 (m, 4H), 3.8-3.95 (m, 4H), 4.4- 4.5 (m, 1H), 7.4 (m, 2H), 7.8 (m, 2H), 8.1 (m, 1H), 10.0 (s, 1H).	426.4	Z
529		A	1H NMR (DMSO-d6 1.0 (t, 3H), 1.1-1.2 (m, 1H), 1.2 (m, 1H), 1.9-2.0 (m, 1H), 2.25- 2.3 (m, 1H), 2.7 (s, 3H), 3.2-3.5 (m, 7H), 3.8-3.95 (m, 4H), 4.4- 4.5 (m, 2H), 7.4 (m, 2H), 7.8 (m, 3H), 10.0 (s, 1H).	444.4	Z
530		C	1H NMR (DMSO- d6) 0.25 (m, 2H), 0.5 (m, 2H), 1.0-1.1 (m, 2H), 1.9-2.0 (m, 1H), 2.25-2.3 (m, 2H), 2.5- 2.7 (m, 3H), 3.2-3.4 (m, 2H), 3.6-4.0 (m, 9H), 4.4-4.5 (m, 1H), 7.4 (m, 2H), 7.8 (m, 4H), 7.9-8.0 (m, 2H).	439.4	Z
531		C	1H NMR (DMSO- d6) 0.095-1.1 (m, 5H), 1.9-2.0 (m, 1H), 2.0 (m, 3H), 2.25-2.3 (m, 2H), 3.0-3.1 (m, 1H), 3.6-4.0 (m, 14H), 4.4-4.5 (m, 1H), 7.4 (m, 2H), 7.8 (m, 4H), 7.9-8.0 (m, 2H).	457.4	Z
532		A	1H NMR (DMSO- d6) 1.0-1.1 (m, 1H), 1.9-2.0 (m, 1H), 2.0- 2.2 (m, 1H), 2.4 (s, 3H), 3.3-3.4 (m, 2H), 3.6-3.7 (m, 2H), 4.2- 4.5 (m, 5H), 8.4 (m, 1H), 8.6 (m, 1H), 8.8 (m, 1H), 8.95 (m, 1H), 9.5 (s, 1H).	471.3	Z
533		C		416.2	Z
534		A		429.4	Z
535		A		475.2	Z1
536		A		459.4	Z
537		A		539.5	Z
538		A		484.4	Z
539		A		499.4	Z
540		A		479.4	Z
541		A		486.3	Z
542		B		475.4	Z2
543		A		493.2	Z
544		A		507.2	Z
Compd		EC90		LC-MS	Pro-
#	Structure	(uM)	NMR data	(M + H)+	cedure
1001		C		632.3	Combi- nation of E and Z
1002		B		592.3	U (last step)
1003		C		618.3	Combi- nation of E and Z
1004		B		578.3	U (last step)
1005		C		614.3	Combi- nation of E and Z
1006		B		574.3	U (last step)
1007		B		464.3	Z3
1008		B		490.3	Combi- nation of E and Z
1009		B		476.3	Combi- nation of E and Z
1010		B		500.3	Combi- nation of E and Z
1011		B		446.2	Z3
1012		C		460.3	Z3
1013		B		471.3	Z3
1014		A		460.3	Z3
1015		B		539.3	Z10
1016		B		497.3	Z10
1017		B		523.3	Z10
1018		B		497.3	Z10
1019		A		480.3	Z11
1041		B		474.3	Z3
1042		C		482.3	Z3
1043		C		482.3	Z3
1044		B		482.3	Z3
1045		C		478.3	Z3
1046		B		478.3	Z3
1047		B		478.3	Z3
1048		A		474.3	Z3
1050		A		475.3	Z
1051		B		465.3	Z3
1052		A		488.3	Z3
1053		A		483.3	Z
1054		B		512.3	Combi- nation of A-2 and Z3
1055		B		540.3	Combi- nation of A-2 and Z3
1056		A		483.3	Z
1057		C		471.3	Z13
1058		B		456.3	Z14
1059		C		524.3	Combi- nation of A-2 and Z3
1060		C		470.3	U
1061		B		498.3	Combi- nation of E and Z
1062		C		476.3	Z3
1063		B		484.3	Combi- nation of E and Z
1064		C		483.3	Z (steps 4-7)
1065		B		455.3	Z (steps 4-7)
1066		A		500.3	Z3
1067		A		472.3	Combi- nation of E and Z
1068		B		536.3	Combi- nation of E and Z
1069		B		527.3	Z10
1070		B		500.2	Combi- nation of E and Z
1071		B		483.3	Z10
1072		B		514.3	new
1073		B		486.3	new
1074		B		450.2	Z11
1101		C		522.3	Combi- nation of T and U
1102		B		482.3	Combi- nation of T and U
1103		C		538.3	Z15
1104		C		498.3	Z15
1105		B		561.3	Combi- nation of T and U.
1106		A		521.3	Combi- nation of T and U
1107		B		536.3	Combi- nation of M and Y
1108		A		496.2	Combi- nation of M and Y.
1109		B		508.3	U
1110		A		468.3	U
1111		B		533.3	U
1112		B		493.3	U
1113		B		586.3	U
1114		B		546.3	U
1115		C		532.3	U
1116		C		492.3	U
1117		C		512.3	U
1118		C		575.3	U
1119		B		535.3	U
1120		C		476.28	Z16
1121		B		556.3	Z16
1122		B		494.3	U
1123		B		494.3	U
1124		C		610.3	U
1125		C		524.3	U
1126		B		526.3	Y
1127		A		486.3	Y
1128		C		564.3	U
1129		C		524.3	U
1130		C		535.3	U
1131		C		495.3	U
1132		C		443.2	Z17
1133		B		569.3	Z18
1134		A		471	Z19
1135		A		499.34	Z19
1136		B		504.4	Z20
1137		A		605	Z19
1201		B		486.2	General Method II
1202		B		493.2	U
1203		B		522.2	U
1204		A		499.3	U
1205		B		508.2	V
1206		B		508.0	V
1207		B		508.2	U
1208		B		493.2	U
1209		B		552.2	U
1210		C		539.2	Z21
1211		C		524.2	Z21
1212		A		493.8	U
1213		C		429.0	Combi- nation of V and Z
1214		A		454.8	Combi- nation of V and Z
1215		A		468.8	Z
1216		B		465.2	Z
1217		C		479.2	Z
1218		B		536.2	U
1219		C		522.2	Z21
1220		A		494.2	U
1221		B		494.2	U
1222		C		454.2	U
1223		C		412.2	Z22
1224		C		438.2	Z22
1225		B		556.2	U
1226		C		455.2	U
1227				390.2	Z23
1228		B		506.5	U
1229		B		507.2	Z
1230		C		524.2	U
1231		B			U
1232		B		504.2	U
1233		B		508.2	U
1234		C		506.2	U
1235		B		524.2	U
1236		C		548.1	U
1237		C		548.1	U
1238		B		484.2	Z24
1239		B		470.2	Z24
1240		B		426.0	Z25
1241		A		522.0	Z25
1242		B		466.2	U
1243		B		462.2	U
1244		A		540.2	Z26
1245		A		480.2	U
1246		A		512.2	Z24
1247		A		526.2	Z24
1248		B		580.2	Z24
1249		B		548.2	Z24
1250		B		472.2	Z26
1251		B		426.2	Z27
1252		C		442.2	Z28
1253		B		470.0	Z28
1301		C		457.3	Z29
1302		B		447.2	Z30
1303		B		401.39	Y
1304		S		527.4	Z
1305		B		493.4	Z
1306		A		553.3	Z
1307		A		553.3	Z
1308		B		473.3	Z
1309		A		515.3	Z
1310		B		473.5	Z
1311		A		511.48	Z
1312		B		505.49	Z
1313		B		493.43	Z
1314		B		507.4	Z
1315		B		519.5	Z, Z31
1316		A		445.4	Z
1317		A		475.5	Z
1318		A		499.5	Z, Z32
1319		A		473.5	Z1
1320		A		521.5	Z1
1321		B		477.5	Z, Z33
1322		C		452.5	F
1323		C		500.5	F
1324		C		454.5	F
1325		B		389.3	Z
1326		A		403.3	Z
1327		A		509.49	U, Z34
1328		A		483.49	U, Z35
1330		A		561.5	U, Z36
1331		A		525.5	U, Z37
1333		A		471.51	Z1
1334		A		487.5	Z1
1335		A		535.6	Z1
1336		A		537.5	Z, Z38
1337		B		473.4	Z, Z38
1338		A		513.5	Z, Z38
1339		A		577.57	Z, Z38
1340		A		499.3	Z1
1341		A		484.2	Z39, U
1342		A		498.4	Z39, U
1343		A		551.48	Z, Z38
1344		A		487.4	Z, Z38
1347		A		561.4	Y, Z34, Z35, Z36
1348		C		539.37	U
1349		C		439.28	U
1350		A		521.37	Z, Z39
1351		A		499.31	Z1
1352		A		498.2	Z, Z39
1353		A		561.43	Z1
1354		A		468.27	Z, Z39
1355		A		573.2	Z1,
1356		A		575.41	Z1
1357		A		532.27	U, Z40
1358		A		539.3	V
1359		A		442.31	Z
1360		B		490.31	Z
1361		A		567.28	Z1,
1362		A		547.38	Z1,
1363		A		535.37	Z1,
1364		B		537.34	Z1
1365		A		558.34	T
1366		B		456.2	Z41
1367		A		533.34	Z, Z40
1368		A		569.34	Z, Z40
1369		A		485.31	Z1
1370		A		499.34	Z1
1371		A		549.40	Z1
1346		A		499.34	Z1
1372		A		563.45	Z1
1373		A		513.36	Z1
1374		B		501.31	Z, Z42
1375		A		565.6	Z, Z42
1376		A		519.6	Z, Z42
1377		B		540.6	T, Z37
1378		C		575.5	T, Z48
1379		A		561.5	T, Z48
1380		A		527.31	Z1
1381		A		561.37	Z1, Z40
1382		A		547.33	Z1, Z40
1383		A		457.30	Z43
1384		A		471.30	Z43
1385		A		471.3	Z43
1386		A		550.45	Z1
1387		A		576.41	Z1, Z36
1388		A		556.41	Z1, Z36
1389		A		590.48	Z1, Z48
1390		B		541.34	T, Z48
1391		A		555.37	T, Z48
1393		B		575.39	T, Z48
1392		A		575.39	T, Z48
1394		B		601.42	T, Z48
1395		A		601.41	T, Z48
1396		A		573.29	T, Z44
1397		A		591.38	Z43
1398		A		457.2	Z1, Z47
1399		A		605.5	Z1, Z47
1400		A		539.33	T, Z45
1401		A		617.3	Z46
1402		A		469.29	Z46
1501		B		538.56	U
1502		C		458.53	U
1503		B		442.45	U
1504		A		489.3	Z1
1505		A		485.3	Z1
1506		B		511.3	U, Z37
1507		A		547.4	U, Z36
1508		B		527.3	U, Z37
1509		A		454.4	F
1510		B		313.25	Z
1511		A		377.28	Z
1512		B		589.3	U, Z36
1513		B		573.42	U, Z36
1514		C		523.37	U
1515		B		509.43	U
1516		B		423.26	U
1517		C		409.2	U
1518		C		576.3	Z36, U
1519		B		469.29	U, Z35
1520		B		615.3	U, Z36
1521		B		561.3	U, Z36
1522		B		527.31	U, Z36
1523		B		601.28	U, Z36
1524		A		525.33	Z1
1525		A		521.3	Z1, Z49
1526		A		535.35	Z1, Z49
1527		A		521.36	Z1, Z49
1528		A		591.37	Z1, Z49
1529		A		537.36	Z1, Z49
1530		C		627.36	Z1, Z51
1531		C		629.33	Z1, Z51
1532		C		537.31	Z2, Z49
1533		C		607.36	Z2, Z49
1534		C		403.2	Z1
1535		A		471.2	Z1
1536		A		501.41	Z1
1537		A		485.2	Z1
1538		A		521.25	Z50
1539		A		575.39	Z1, Z51
1540		A		591.37	Z1, Z51
1541		A		627.40	Z1, Z51
1542		B		561.2	Z, Z50
1543		A		443.2	Z1
1544		A		457.29	Z1
1545		A		573.38	Z1, Z50
1546		A		645.36	Z1, Z51
1601		C		445.2	B, Z
1602		C		483.2	B, Z
1603		C		441.2	B, Z
1604		C		469.3	B, Z
1605		C		388.2	B, Z
1610		B		426.2	Z56
1611		B		454.2	Z56
1616		C		441.0	Z57
1617		C		426.2	Z58
1618		B		454.2	Z58
1619		C		505.3	Z57
1620		C		515.3	Z
1623		B		484.3	Z
1625		B		440.2	Z67
1626		B		412.2	Z67
1627		C		412.2	Z67
1628		A		541.25	Z59
1629		B		513.2	Z59
1630		A		454.2	Z60
1632		A		484.2	Z61
1633		A		455.2	Z60
1634		A		427.2	Z60
1635		A		479.2	Z40, repalce NaSMe with NaCN
1636		A		464.2	Z63
1637		B		498.2	Z62
1638		B		512.2	Z62
1639		A		553.0	Z66
1640		B		498.2	Z63
1641		A		457.2	Z62
1642		A		471.2	Z62
1643	isomer 1	A		484.2	Z64
1644	isomer 1	A		456.2	Z64
1645	isomer 1	B		590.2	Z64
1646	isomer 2	B		590.2	Z64
1647	isomer 2	B		456.2	Z64
1648	isomer 2	B		484.2	Z64
1649		A		591.2	Z64
1650		A		457.2	Z64
1651		A		471.2	Z64
1652		A		591.2	Z64
1653		A		550.2	Z66
1654		B		536.2	Z66
1701		B	1H NMR (CDCl3, 400 MHz): δ 10.24 (1H, broad s), 7.92 (1H, d, J = 8.54 Hz), 7.88 (1H, d, J = 7.93 Hz), 7.48 (1H, ddd, J = 1.22, 7.93, 8.54 Hz), 7.37 (1H, t, J = 7.93 Hz), 5.26 (1H, broad s), 4.57 (1H, broad s), 3.84 (1H, d, J = 4.88 Hz), 3.40 (1H, s), 3.36 (1H, m), 3.11 (1H, broad s), 2.70 (3H, s), 2.37 (1H, ddt, J = 4.27, 9.76, 13.42 Hz), 2.08 (1H, ddt, J = 4.88, 10.98, 15.25 Hz), 1.87 (1H, m), 1.65 (2H, m), 1.12 (3H, s), 1.09 (1H, m), 0.56 (2H, dd, J = 1.22, 7.93 Hz), 0.28 (2H, m)	426.27	Z67
1702		B	1H NMR (dmso- d6, 400 MHz): δ 10.32 (1H, broad s), 8.38 (1H, broad s), 8.24 (1H, d, J = 7.93 Hz), 8.07 (1H,d, J = 8.54 Hz), 7.63 (1H, dd, J = 7.32, 7.93 Hz), 7.55 (1H, t, J = 7.32 Hz), 4.54 (1H, dd, J = 7.93, 16.47 Hz), 4.36 (2H, m), 3.62 (1H, dd, J = 5.49, 6.10 Hz), 2.65 (3H, s), 2.21 (1H, ddt, J = 3.05, 9.50, 12.81 Hz), 1.91 (1H, m), 1.56 (1H, m), 1.38 (1H, m), 1.19 (3H, s)	454.24	Z68
1703		B	1H NMR (dmso- d6, 400 MHz): δ 9.61 (1H,d, J = 4.88 Hz), 9.44 (1H, broad s), 8.20 (1H, d, J = 7.93 Hz), 8.13 (1H, d, J = 8.54 Hz), 7.85 (1H, s), 7.69 (1H, s), 7.60 (1H, dd, J = 7.32, 7.93 Hz), 7.53 (1H, dd, J = 7.32, 7.93 Hz), 7.35 (1H, d, J = 3.66 Hz), 6.26 (1H, broad s), 4.41 (1H, dd, J = 6.10, 7.32 Hz), 3.81 (1H, broad s), 3.71 (1H, dd, J = 4.88, 5.49 Hz), 3.40 (2H, m), 2.48 (3H, s), 2.14 (1H, m), 2.01 (1H, m), 1.20 (1H, m)	552.0	Z69
1704		A	1H NMR (dmso- d6, 400 MHz): δ 10.05 (1H, d, J = 6.71 Hz), 9.12 (1H, s), 8.45 (1H, d, J = 5.49 Hz), 8.14 (1H, d, J = 5.49 Hz), 7.46 (1H, broad s), 4.69 (1H, d, J = 3.05 Hz), 4.44 (2H, m), 3.63 (1H, broad s), 3.18 (2H, m), 2.59 (3H, s), 2.27 (1H, m), 1.92 (1H, m), 1.53 (1H, m), 1.30 (1H, m), 1.20 (3H, s), 1.06 (1H, m), 0.39 (2H, dd, J = 1.83, 7.93 Hz), 0.19 (2H, dd, J = 4.88, 9.76 Hz)	427.28	Z67
1705		A	1H NMR (dmso- d6, 400 MHz): δ 13.20-13.70 (1H, broad s), 9.66 (1H, s), 8.96 (1H, d, J = 6.71 Hz), 8.74 (1H, d, J = 5.49 Hz), 8.62 (1H, d, J = 5.49 Hz), 8.09 (1H, broad s), 7.23 (2H, d, J = 7.93 Hz), 6.87 (2H, d, J = 7.93 Hz), 4.51 (1H, dd, J = 6.71, 7.93 Hz), 3.99 (2H, q, J = 6.71 Hz), 3.82 (1H, m), 3.71 (1H, m), 3.61 (2H, m), 3.37 (2H, d, J = 3.66 Hz), 2.85 (2H, t, J = 7.32 Hz), 2.42 (3H, s), 2.25 (1H, m), 1.97 (1H, m), 1.31 (3H, t, J = 6.71 Hz), 1.18 (1H, m)	537.2	U
1706		B	1H NMR (dmso- d6, 400 MHz): δ 7.33 (1H, d, J = 8.54 Hz), 7.28 (1H, d, J = 7.32 Hz), 6.81 (1H, ddd, J = 1.22, 7.32, 7.93 Hz), 6.73 (1H, ddd, J = 1.22, 7.32, 7.93 Hz), 6.33 (1H, d, J = 4.88 Hz), 6.01 (1H, d, J = 5.49 Hz), 3.83 (1H, q, J = 7.32 Hz), 3.15 (1H, dd, J = 5.49, 6.10 Hz), 3.10 (1H, t, J = 4.88 Hz), 3.01 (1H, m), 2.91 (1H, dd, J = 6.71, 7.32 Hz), 2.77 (2H,d, J = 5.49 Hz), 2.34 (2H, dd, J = 6.71, 7.32 Hz), 1.77 (3H, s), 1.67 (1H, m), 1.42 (3H, s), 1.37 (1H, m), 0.53 (1H, dt, J = 7.93, 13.42 Hz)	512.2	U
1707		A	1H NMR (CD3OD), 400 MHz): δ 9.74 (1H, s), 8.78 (2H, s), 7.09 (1H, d, J = 4.88 Hz), 6.78 (1H, d, J = 5.49 Hz), 4.60 (1H, m), 3.90 (2H, m), 3.83 (1H, dd, J = 7.32, 14.03 Hz), 3.71 (1H, dt, J = 6.10, 7.32 Hz), 3.57 (2H, dd, J = 4.88, 6.71 Hz), 3.12 (2H, t, J = 6.71 Hz), 2.59 (3H, s), 2.44 (1H, m), 2.20 (3H, s), 2.13 (1H, m), 1.33 (1H, m)	513.2	U
1708		A	1H NMR (CD3OD), 400 MHz): δ 9.70 (1H, s), 8.81 (1H, d, J = 6.25 Hz), 8.79 (1H, d, J = 6.25 Hz), 7.37 (2H, d, J = 8.59 Hz), 7.19 (2H, d, J = 7.81 Hz), 5.28 (1H, q, J = 7.03 Hz), 4.63 (1H, dd, J = 4.68, 7.03 Hz), 3.64 (1H, d, J = 7.81 Hz), 3.60 (1H, dd, J = 3.90, 10.94 Hz), 3.53 (1H, dd, J = 3.90, 10.94 Hz), 3.24 (1H, m), 2.65 (3H, s), 2.32 (3H, s), 2.24 (1H, m), 2.09 (1H, m), 1.63 (3H, d, J = 7.03 Hz), 1.29 (3H, s)	521.2
1709		A	1H NMR (CD3OD), 400 MHz): δ 9.75 (1H, s), 8.82 (2H, m), 4.70 (1H, m), 4.41 (2H, m), 3.66 (1H, d, J = 7.81 Hz), 3 60 (1H, dd, J = 3.12, 10.94 Hz), 3.53 (1H, dd, J = 3.12, 10.94 Hz), 3.24 (1H, m), 2.64 (3H, S), 2.52 (1H, m), 2.12 (1H, m), 1.66 (1H, m), 1.24 (3H, s)
1801		A	1H NMR (DMSO- d6, 400 MHz) δ 1.67 (m, 1H), 1.98 (m, 1H), 2.11 (m, 1H), 2.25 (m, 1H), 3.65 (m, 2H), 3.68 (m, 2H). 4.33 (m, 1H), 4.40 (m, 1H), (4.44 (m, 1H), 6.58 (m, 1H), 7.11 (m, 1H), 7.39 (dd, 1H, J = 3.13, 7.82 Hz), 7.50 (dd, 1H, J = 7.03, 7.03 Hz), 7.57 (dd, 1H, J = 7.03, 7.82 Hz), 7.64 (dd, 1H, J = 4.69, 6.25 Hz), 8.11 (dd, 1H, J = 3.91, 8.60 Hz), 8.17 (dd, 1H, J = 7.03, 7.03 Hz), 9.29 (broad s, 1H), 9.61 (broad s, 1H).		Z69
1802		B		493.20	Z3
1803		C	1H NMR (DMSO- d6, 400 MHz) δ 1.28 (m, 1H), 1.99 (m, 1H), 2.25 (m, 1H), 3.35 (m, 1H), 3.40 (m, 1H), 3.68 (m. 1H), 3.75 (m, 1H), 4.43 (m, 1H), 6.52 (m, 1H), 7.11 (dd, 1H, J = 4.40, 4.40 Hz), 7.44 (d, 1H, J = 2.93 Hz), 7.50 (dd, 1H, J = 7.32, 7.32 Hz), 7.58 (dd, 1H, J = 7.32, 7.81 Hz), 7.66 (d, 1H, J = 3.91 Hz), 8.11 (d, 1H, J = 7.81 Hz), 8.17 (d, 1H, J = 7.81 Hz), 9.58 (broad s, 1H).	552.26	Z69
1804		A	1H NMR (DMSO- d6, 400 MHz) δ 1.06 (m, 1H), 1.95 (broad s, 1H), 2.07 (m, 1H), 2.36 (s, 3H), 3.35 (s, 3H), 3.76 (m, 2H), 4.45 (m, 1H), 4.67 (dd, 1H, J = 4.69, 14.07 Hz), 4.80 (dd, 1H, J = 5.47, 14.85 Hz), 7.12 (dd, 2H, J = 7.03, 7.82 Hz), 7.42 (m, 1H), 8.43 (broad s, 1H), 8.49 (broad s), 8.68 (broad s, 1H), 8.89 (d, 1H, J = 6.25 Hz), 9.56 (broad s, 1H).	515.30	U
1805		A	1H NMR (DMSO- d6, 400 MHz) δ 1.18 (m, 1H), 1.96 (m, 1H), 2.24 (m, 1H), 2.45 (s, 3H), 3.13 (m, 2H), 3.36 (m, 2H), 3.66 (m, 4H), 3.80 (dd, 1H, J = 5.47, 6.25 Hz), 4.43 (dt, 1H, J = 7.82, 10.94 Hz), 6.97 (m, 2H), 7.36 (dd, 1H, J = 1.56, 6.25 Hz), 7.52 (dd, 1H, J = 7.03, 8.60 Hz), 7.59 (dd, 1H, J = 7.03, 8.60 Hz), 7.94 (broad s, 1H), 8.12 (d, 1H, J = 7.82 Hz), 8.19 (d, 1H, J = 7.82 Hz), 9.50 (d, 1H, J = 6.25 Hz).	498.27	U
1806		C	1H NMR (CD3OD, 400 Hz) δ 1.38 (m, 1H), 2.17 (m, 1H), 2.49 (m, 1H), 2.61 (s, 3H), 3.25 (dd, 1H, J = 6.25, 7.03 Hz), 3.57 (m, 1H), 3.57 (dd, 1H, J = 4.69, 6.25 Hz), 3.82 (m, 1H), 3.87 (dd, 1H, J = 6.25, 7.03 Hz), 3.92 (dd, 1H, J = 4.69, 4.69 Hz), 3.97 (dd, 1H, J = 4.69, 6.25 Hz), 4.63 (m, 1H), 6.97 (m, 2H), 7.25 (d, 1H, J = 6.25 Hz), 8.77 (s, 2H), 9.73 (broad s, 1H).		U
1808		A	1H NMR (DMSO- d6, 400 Hz) δ 1.16 (m, 1H), 1.22 (s, 3H), 1.54 (m, 1H), 1.91 (m, 1H), 2.21 (m, 1H), 2.59 (s, 3H), 3.64 (broad s, 1H), 4.28-4.76 (m, 5H), 7.04 (m, 2H), 7.34 (m, 1H), 7.75 (broad s, 1H), 8.14 (d, 1H, J = 5.37 Hz), 8.45 (d, 1H, J = 5.37 Hz), 9.13 (s, 1H), 10.06 (d, 1H, 5.86 Hz).	499.28	Z67
1809		B	1H NMR (DMSO- d6, 400 Hz) δ 1.28 (s, 3H), 1.54 (m, 1H), 1.72 (m, 1H), 2.07 (m, 1H), 2.32 (m, 1H), 2.74 (s, 3H), 3.74 (t, 1H, J = 5.47 Hz), 4.27 (m, 1H), 4.51 (m, 1H), 8.72 (d, 1H, J = 6.25 Hz), 8.77 (d, 1H, J = 6.25 Hz), 9.69 (s, 1H).	455.22	Z67
1810		A	1H NMR (CD3OD, 400 Hz) δ 1.21 (s, 3H), 1.51 (d, 3H, J = 6.84 Hz), 1.74 (m, 1H), 2.10 (m, 1H), 2.29 (s, 3H), 2.42 (broad s, 1H), 2.64 (s, 3H), 3.77 (dd, 1H, J = 3.42, 5.86 Hz), 4.64 (dd, 1H, J = 8.3, 8.79 Hz), 5.19 (broad s, 1H), 7.13 (d, 2H, J = 7.81 Hz), 7.30 (d, 2H, J = 7.81 Hz), 8.03 (d, 1H, J = 5.37 Hz), 8.38 (d, 1H, J = 5.86 Hz), 9.09 (s, 1H).	491.40	Z67
1811		A	1H NMR (CD3OD, 400 Hz) δ 0.28 (m, 1H), 0.39 (m, 1H), 0.47 (m, 1H), 0.53 (m, 1H), 0.99 (m, 1H), 1.27 (broad s, 2H), 1.29 (s, 2H), 1.31 (s, 2H), 1.53 (m, 1H), 1.72 (m, 1H), 2.09 (m, 1H), 2.38 (m, 1H), 2.66 (s, 1H), 3.60 (m, 1H), 3.80 (dd, 1H, J = 3.91, 6.35 Hz), 4.63 (dd, 1H, J = 8.39, 8.79 Hz), 8.06 (dd, 1H, J = 0.98, 5.37 Hz), 8.41 (d, 1H, J = 5.86 Hz), 9.11 (s, 1H).	441.32	Z67
1812		B	1H NMR (DMSO- d6, 400 Hz) δ 1.16 (m, 1H), 1.94 (m, 1H), 2.22 (m, 1H), 2.37 (s, 3H), 2.44 (s, 3H), 3.03 (dd, 2H, J = 7.32, 7.32 Hz), 3.61 (m, 2H), 3.68 (dd, 1H, J = 4.40, 4.88 Hz), 3.79 (dd, 1H, J = 5.86, 5.86 Hz), 4.42 (dt, 1H, J = 7.32, 15.14 Hz), 6.62 (dd, 1H, J = 0.97, 3.42 Hz), 6.73 (d, 1H, J = 3.42 Hz), 7.52 (dd, 1H, J = 6.84, 7.32 Hz), 7.59 (dd, 1H, J = 6.84, 7.32 Hz), 7.86 (broad s, 1H), 8.12 (d, 1H, J = 7.81 Hz), 8.19 (d, 1H, J = 7.81 Hz), 9.47 (d, 1H, J = 7.81 Hz).	512.33	U
1813		A	1H NMR (DMSO- d6, 400 Hz) δ 1.15 (m, 1H), 1.94 (m, 1H), 1.97 (s, 1H), 2.21 (m, 1H), 2.37 (s, 3H), 2.41 (s, 3H), 3.03 (m, 2H), 3.34 (d, 1H, J = 5.47 Hz), 3.65 (m, 2H), 3.68 (dd, 1H, J = 4.69, 4.69 Hz), 3.79 (dd, 1H, J = 5.47, 6.25 Hz), 4.42 (dt, 1H, J = 7.82, 14.85 Hz), 5.45 (broad s, 3H), 6.62 (d, 1H, J = 2.35 Hz), 6.75 (d, 1H, J = 3.13	513.36	U
1814		A	1H NMR (DMSO- d6, 400 Hz) δ 1.09 (broad s, 3H), 1.30 (m, 1H), 1.56 (m, 1H), 1.92 (m, 1H), 2.22 (m, 1H), 2.58 (s, 3H), 2.84 (s, 3H), 3.64 (broad s, 1H), 4.23-4.74 (m, 5H), 7.04 (dd, 2H, J = 6.84, 7.32 Hz), 7.35 (m, 1H), 7.70 (broad s, 1H), 7.95 (d, 1H, J = 5.37 Hz), 8.30 (d, 1H, J = 5.37 Hz), 9.69 (broad s, 1H).	513.40	Z67
1815		A	1H NMR (DMSO- d6, 400 Hz) δ 0.22 (dd, 2H, J = 4.88, 9.77 Hz), 0.39 (m, 2H), 1.09 (s, 4H), 1.34 (m, 1H), 1.55 (m, 1H), 1.93 (m, 1H), 2.25 (m, 1H), 2.59 (s, 3H), 2.84 (s, 3H), 3.18 (dd, 2H, J = 6.35, 12.70 Hz), 3.64 (m, 1H), 4.39- 4.70 (m, 3H), 7.45 (dd, 1H, J = 4.40, 5.37 Hz), 7.95 (d, 1H, J = 5.37 Hz), 8.30 (d, 1H, J = 5.37 Hz), 9.79 (d, 1H, J = 7.32 Hz).	441.37	Z67
1816		A	1H NMR (CD3OD, 400 Hz) δ 1.20 (m, 4H), 1.53 (m, 1H), 1.74 (m, 1H), 2.10 (m, 1H), 2.39 (m, 1H), 2.70 (s, 3H), 2.94 (s, 3H), 3.79 (m, 1H), 4.19 (m, 1H), 4.28 (m, 1H), 7.91 (d, 1H, J = 5.37 Hz), 8.29 (d, 1H, J = 5.86 Hz).	469.30	Z67
1817		A	1H NMR (DMSO- d6, 400 Hz) δ 0.01 (m, 1H), 0.14-0.32 (m, 3H), 0.82 (m, 1H), 0.94 (s, 3H), 1.04 (d, 3H, J = 7.03 Hz), 1.19 (m, 1H), 1.41 (m, 1H), 1.78 (m, 1H), 2.09 (m, 1H), 2.44 (s, 3H), 2.69 (s, 3H), 3.41 (m, 1H), 3.49 (m, 1H), 4.12-4.55 (m, 3H), 7.18 (d, 1H, J = 7.82 Hz), 7.80 (d, 1H, J = 5.47 Hz), 8.15 (d, 1H, J = 5.47 Hz), 9.63 (d, 1H, J = 7.03 Hz).	455.36	Z67
1818		B	1H NMR (DMSO- d6, 400 Hz) δ 1.18 (broad s, 1H), 1.23 (s, 2H), 1.33 (m, 1H), 1.55 (m, 1H), 1.93 (m, 1H), 2.32 (m, 1H), 2.58 (s, 3H), 2.79 (m, 2H), 3.44 (m, 2H), 3.65 (m, 1H), 3.79 (s, 3H), 4.38-4.77 (m, 3H), 7.04 (d, 1H, J = 8.30 Hz), 7.19 (m, 1H), 7.30 (d, 1H, J = 1.95 Hz), 8.14 (d, 1H, J = 4.88 Hz), 8.45 (d, 1H, J = 5.37 Hz), 9.13 (s, 1H), 10.06 (d, 1H, J = 7.32 Hz)	541.34	Z67
1819		A	1H NMR (CD3OD, 400 Hz) δ 1.21 (t, 3H, J = 7.03 Hz), 1.29 (broad s, 2H), 1.53 (m, 1H), 1.72 (m, 1H), 2.10 (m, 1H), 2.93 (broad s, 1H), 2.64 (s, 3H), 3.56 (q, 2H, J = 7.03 Hz), 3.62 (s, 3H), 3.79 (dd, 1H, J = 3.91, 6.25 Hz), 4.67 (m, 1H), 8.04 (d, 1H, J = 5.47 Hz), 8.40 (d, 1H, J = 5.47 Hz), 9.11 (s, 1H).	446.30	Z67
1820		B	1H NMR (DMSO- d6, 400 Hz) δ 0.49 (m, 2H), 0.67 (d, 2H, J = 3.13 Hz), 1.17 (s, 3H), 1.38 (m, 1H), 1.54 (m, 1H), 1.92 (m, 1H), 2.30 (m, 1H), 2.59 (s, 3H), 2.67 (m, 1H), 3.63 (m, 1H), 4.49 (m, 1H), 4.55 (m, 1H), 4.87 (broad s, 1H), 7.61 (broad s, 1H), 8.15 (d, J = 4.69 Hz), 8.46 (d, 1H, J = 5.47 Hz), 9.15 (s, 1H), 9.92 (broad s, 1H).	413.32	Z67
1821		A	1H NMR (DMSO- d6, 400 Hz) δ 1.18 (s, 4H), 1.49 (m, 1H), 1.89 (m, 1H), 2.05 (m, 1H), 2.59 (s, 3H), 3.62 (s, 1H), 4.27 (s, 1H), 4.34-477 (m, 4H), 7.02 (dd, 1H, J = 7.03, 7.03 Hz), 7.16 (dd, 1H, J = 7.82, 10.16 Hz), 7.44 (dd, 1H, J = 8.60, 15.63 Hz), 7.91 (broad s, 1H), 8.14 (d, 1H, J = 4.69 Hz), 8.45 (d, 1H, J = 4.69 Hz), 9.12 (s, 1H), 9.99 (d, 1H, J = 4.69 Hz).	499.37	Z67
1901		C		438.7	Z70
1902		C		456.7	Z71
1903		C		416.7	Com- pound 1902 was converted to 1903 HCl salt using Pro- cedure F, step 3
1904		C		398.7	Com- pound 1901 was converted to 1904 HCl salt using Pro- cedure F, step 3
1905		B		466.7	Z72
1906		B		428.7	Z3
1907		B		403.7	Z73
1908		B		676.7	Z3
1909		A		536.7	Com- pound 1908 was converted to 1909 HCl salt using Pro- cedure G, step 7
1910		A		514.7	Z3
1911		A		537.3	Z
1912		A		518.7	Z3
1913		B		558.7	Z
1914		A		561.7	Z
1915		C		430.7	Z74
1916		C		402.7	Z75
1917		C		466.7	Z76
1918		A		509.7	Z
1919		B		508.7	Z3
2001		B	1H NMR (400 MHz. CD3OD), δ, 9.57 (s, 1 H), 8.96 (s, 1 H), 8.48 (d, 1 H, J = 5.6 Hz), 4.70- 4.63 (m, 1 H), 4.57-4.49 (m, 1 H), 4.37-4.26 (m, 1 H), 4.06 (bt, 1 H, J = 4.0 Hz), 4.00 (bt, 1 H, J = 4.0 Hz), 3.75- 3.55 (m, 2 H), 2.95 (s, 3 H), 2.59-2.53 (m, 1 H), 2.27-2.17 (m, 1 H), 1.55-1.48 (m, 1 H).	455	Z
2002		C		495	Z
2003		B	1H NMR (400 MHz, CD3OD), δ, 9.54 (s, 1 H), 8.95 (s, 1 H), 8.47 (d, 1 H, J = 6.0 Hz), 4.67- 4.62 (m, 1 H), 4.05-3.97 (m, 2 H), 3.69-3.63 (m, 2 H), 3.48-3.46 (m, 2 H), 2.91 (s, 3 H), 2.59-2.52 (m, 1 H), 2.21- 2.17 (m, 2 H), 1.53-1.45 (m, 1 H), 1.26-1.91 (m, 1 H), 0.60 (d, 2 H, J = 7.6 Hz), 0.38 (d, 2 H, J = 4.4 Hz)	427	Z
2004		B		600	U
2005		B	1H NMR (400 MHz, CD3OD), δ, 7.98 (d, 1 H, J = 8.4 Hz), 7.94 (d, 1 H, J = 7.6 Hz), 7.50-7.46 (m, 3 H), 7.37 (dt, 1 H, J = 0.8 & 8.0 Hz), 7.23 (d, 2 H, J = 8.0 Hz), 4.62- 4.52 (m, 2 H), 4.36-4.28 (m, 1 H), 2.59 (s, 3 H), 2.35 (s, 3 H), 1.71-1.65 (m, 1 H), 1.35-1.27 (m, 1 H), 0.92-0.83 (m, 1 H).	560	U
2006		B	1H NMR (400 MHz, D6-dmso), δ, 9.23 (d, 1 H, J = 5.6 Hz), 8.45 (d, 1 H, J = 4.8 Hz), 8.13 (d, 1 H, J = 8.0 Hz), 8.07 (t, 1 H, J = 6.4 Hz), 7.38-7.35 (m, 1 H), 4.72 (t, 1 H, J = 5.2 Hz), 4.52-4.21 (m, 2 H), 4.35-4.12 (m, 3 H), 3.48 (t, 2 H, J = 5.6 Hz), 2.64 (s, 3 H), 2.40-2.33 (m, 1 H), 2.17-2.12 (m, 1 H), 1.65-1.57 (m, 1 H), 1.39 (s, 3H), 1.22 (b. 1 H), 1.20 (s, 3 H).	495	Z
2007		A		477	Z
2008		B		455	Z
2009		A		593	Z
2010		A		553	Z
2011		C		589	Z
2012		A		549	Z
2013		B	1H NMR (400 MHz, CD3OD), δ, 8.15 (d, 1 H, J = 8.0 Hz), 8.10 (d, 1 H, J = 8.0 Hz), 7.62 (d, 1 H, J = 7.6 Hz), 7.55 (t, 1 H, J = 7.6 Hz), 4.52-4.47 (m, 2 H), 3.94 (t, 1 H, J = 5.2 Hz), 3.89 (t, 1 H, J = 4.8 Hz), 3.57 (d, 2H, J = 4.8 Hz), 2.61 (s, 3 H), 2.45-2.37 (m, 1 H), 2.19- 2.11 (m, 1 H), 1.43-1.27 (m, 2 H), 0.89-0.66 (m, 3 H), 0.55-0.49 (m, 1 H).	510	U

Assays
Cell-Based HCV Replicon Assay