Alpha protein kinase 1 inhibitors for use in treating Kawasaki disease

CROSS-REFERENCE

FIELD OF THE INVENTION

BACKGROUND OF THE INVENTION

SUMMARY OF THE INVENTION

[0008]
wherein A, p, R¹, R², R³, R⁴ and R⁵ are as defined herein

[0010]
wherein p, R¹, R², R3, R⁴,R⁵, R⁶, and R⁹ are as defined herein.

[0012]
wherein p, R¹, R², R³, R⁴, R⁵, R⁶, and R⁹ are as defined herein.

[0014]
wherein p, R², R³, R⁴, R⁵, R³, D, E, F, and G are as defined herein.

[0016]

• • [0017] wherein p, R², R³, R⁴, R⁵, R¹⁵, R¹⁶, and R¹⁷ are as defined herein.

[0019]
wherein p, m, R², R³, R⁴, R⁵, R¹⁸ are as defined herein.

DETAILED DESCRIPTION

DETAILED DESCRIPTION OF THE EMBODIMENTS

[0060]

• • [0061] wherein A, p, R¹, R², R³, R⁴ and R⁵ are as defined herein:
  • [0062] A is selected from a bond, azetidinyl, —O—, —N(R⁶)—, —CH₂—N(R⁶)—, —CHR⁹—N(R⁶)—, wherein
    • [0063] R⁶ is selected from H, —OH, optionally substituted C₁-C₆ alkyl, optionally substituted C₁-C₆ haloalkyl, optionally substituted C₁-C₆ alkenyl, optionally substituted C₁-C₆ hydroxyalkyl, optionally substituted C₁-C₆ aminoalkyl, optionally substituted C₁-C₆ alkoxyl, optionally substituted saturated or unsaturated C₃-C₆ cycloalkyl, and optionally substituted saturated or unsaturated C₃-C₆ cycloalkoxyl, wherein
      • [0064] the optionally substituted R⁶ moieties comprise 0-3 substituents independently selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, and C₁-C₆ alkoxyl;
    • [0065] R⁹ is selected from optionally substituted C₁-C₆ alkyl, C₁-C₆ haloalkyl, optionally substituted saturated or unsaturated C₃-C₆ cycloalkyl, optionally substituted saturated or unsaturated C₃-C₆ cycloalkoxyl, wherein
      • [0066] optionally substituted R⁹ moieties comprise 0-2 substituents independently selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, —CH-1R^7fR^8f, —OR^7f, —OC(O)(R^7f), —C(O)(R^7f), —C(O)N(R^7fR^8f), —C(O)O(R^7f), —S(O)₂(R^7f), —S(O)ON(R^7fR^8f) and —N(R^7fR^8f) wherein
      • [0067] each R^7f and R^8f are independently selected from H, C7-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxy;
  • [0068] R¹ is selected from H, optionally substituted C₁-C₆ alkyl, optionally substituted C₁-C₆ alkenyl, optionally substituted C₁-C₆ hydroxyalkyl, optionally substituted C₁-C₆ haloalkyl, optionally substituted C₁-C₆haloalkoxyl, optionally substituted C₁-C₆ aminoalkyl, optionally substituted C₁-C₆ alkoxyl, optionally substituted saturated or unsaturated C₃-C₆ cycloalkyl, optionally substituted saturated or unsaturated C₃-C₆ cycloalkoxyl, optionally substituted mono or bicyclic aryl, optionally substituted 5-10 membered heteroaryl containing 1-4 heteroatom ring vertices selected from N, O, and S; optionally substituted saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; optionally substituted saturated or unsaturated 7-8 membered bridged heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; optionally substituted saturated or unsaturated 7-11 membered spiroheterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; and optionally substituted saturated or unsaturated 6-11 membered bicyclic heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S;
    • [0069] wherein optionally substituted R¹ moieties comprise 0-4 substituents independently selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, —R^7a, —X¹—R^7a, CHR^7aR^8a, —OR^7a, —O—X¹—R^7a, —X¹—O—X¹—R^7a, —OC(O)(R^7a), —O—X¹—C(O)(R^7a), —C(O)(R^7a), —C(O)N(R^7aR^8a), —NR^7a(CO)R^8a, —C(O)O(R^7a), S(O)₂R^7a, —S(O)₂N(R^7aR^8a), —N(R^7aR^8a), saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, mono or bicyclic aryl, 5-10 membered heteroaryl containing 1-4 heteroatom ring vertices selected from N, O, and S, saturated or unsaturated 7-8 membered bridged heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, saturated or unsaturated 7-11 membered spiroheterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, and 6-11 membered bicyclic heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; wherein each X is independently C_1-6 alkylene;
      • [0070] each R^7a and R^8a are independently selected from H, C₁-C₆ alkyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆haloalkoxyl, saturated or unsaturated C3-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, aryl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, wherein the aryl and 3-7 membered heterocyclyl groups are substituted with 0-3 substituents selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl; and
      • [0071] the C₃-C₆ cycloalkyl, C₃-C₆ cycloalkoxyl, 3-7 membered heterocyclyl, the mono or bicyclic aryl, the 5-10 membered heteroaryl, the saturated or unsaturated 7-8 membered bridged heterocyclyl, the saturated or unsaturated 7-11 membered spiroheterocyclyl, and the 6-11 membered bicyclic heterocyclyl are each independently substituted with 0 to 3 moieties selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₁-C₆ cycloalkoxyl, —CHR^7bR^8b, —OR^7b, —OC(O)(R^7b), —C(O)(R^7b), —C(O)N(R^7bR^8b), —NR^7b(CO)R^8b, —C(O)O(R^7b), —S(O)₂N(R^7bR^8b) and —N(R^7bR^8b), wherein
      • [0072] each R^7b and R^8b are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C3-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl; or
  • [0073] R¹ and R⁶ combine to form a 3-6 membered heterocycloalkyl substituted with 0-3 moieties independently selected from the group consisting of halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, and C₁-C₆ alkoxyl;
  • [0074] R⁵ is selected from H, deuterium, halo, C₁-C₆ alkyl, C₁-C₆ deuteroalkyl, and C₁-C₆ haloalkyl;
  • [0075] R² and R³ are each independently selected from H, OH, C₁-C₆ alkyl and C₂-C₆ alkynyl, wherein C₁-C₆ alkyl and C₂-C₆ alkynyl are each substituted with 0-3 moieties independently selected from halo, —OH, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, —OC(O)(R^7c), —C(O)(R^7c), C(O)O(R^7c), S(O)₂N(R^7cR^8c), and N(R^7cR^8c), wherein
    • [0076] each R^7c and R^8c are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxy, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl;
    • [0077] provided that R² and R³ are not both H; or
  • [0078] R² and R³ combine to form a C₃-C₆ cycloalkyl ring or a 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices independently selected from N, O, and S, wherein the ring formed can be optionally substituted with 1-2 substituents independently selected from C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, halo, —OH, ═O, —CN, OC(O)(R^7d), —C(O)(R^7d), C(O)O(R^7d), S(O)₂N(R^7dR^8d) and N(R^7dR^8d), wherein
    • [0079] each R^7d and R^8d are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl;
  • [0080] each R⁴ is independently selected from halo, —OH, —NH₂, CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, CHR^7eR^8e, OR^7e, OC(O)(R^7e), C(O)(R^7e), C(O)N(R^7eR^8e), C(O)O(R^7e), S(O)₂N(R^7eR^8e) and N(R^7eR^8e) wherein
    • [0081] each R^7c and R^8c are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, and
  • [0082] the subscript p is 0, 1, 2 or 3.

[0090]
wherein p, R¹, R², R³, R⁴, R⁵, R⁶, and R are as defined above.

[0125]

• • [0126] wherein p, R², R³, R⁴ and R⁵ are as defined above; and
  • [0127] D is CR¹⁰ or N;
  • [0128] E is CR¹⁴ or N;
  • [0129] F is CR¹² or N;
  • [0130] G is CR¹¹ or N;
    • [0131] provided that no more than three of D, E, F, and i are N;
  • [0132] R¹⁰, R¹¹, R¹², R¹³ and R¹⁴, when present, are each independently selected from H, halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, —R^7a, —X¹—R^7a, X¹—O—X¹—R—^7a, —CHR^7aR^8a, —OR^7a, —O—X¹—R^7a, —OC(O)(R^7a), —O—X¹—C(O)(R^7a), —C(O)(R^7a), —C(O)N(R^7aR^8a), —C(O)O(R^7a), S(O)₂R^7a, —S(O)₂N(R^7aR^8a), —N(R^7aR^8a), saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₁-C₆ cycloalkoxyl, saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; mono or bicyclic aryl, a 9-10 membered bicyclic heteroaryl containing 1-4 heteroatom ring vertices selected from N, O, and S; saturated or unsaturated 7-8 membered bridged heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; and saturated or unsaturated 7-11 membered spiroheterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; 6-11 membered bicyclic heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; wherein
    • [0133] each X¹ is independently C_1-6 alkylene;
    • [0134] each R^7a and R^8a are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl; and
    • [0135] the 3-7 membered heterocyclyl, the mono or bicyclic aryl, the 9-10 membered bicyclic heteroaryl, the 7-8 membered bridged heterocyclyl, the 7-11 membered spiroheterocycly, and the 6-11 membered bicyclic heterocyclyl are each independently substituted with 0 to 2 moieties selected from halo, —OH, —COOH, —NH₂, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, —CHR^7gR^8g, —OR^7g, —OC(O)(R^7g), —C(O)(R^7g), —C(O)N(R^7gR^8g), —NR^7g(CO)R^8g, —C(O)O(R^7g), —S(O)₂N(R^7gR^8g) and —N(R^7gR^8g), wherein
      • [0136] each R^7g and R^8g are each independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl. C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl;

[0145]

• • [0146] wherein p, R², R³, R⁴ and R⁵ are as defined above; and
  • [0147] R⁶ and R¹⁷ are each independently selected from halo and C₁-C₆ alkyl;
  • [0148] R¹⁵ is selected from —OH, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, —CHR^7bR^8b, —C(O)(R^7b), —C(O)N(R^7bR^8b), —C(O)O(R(⁶), —S(O)₂R^7b and —S(O)N(R^7bR^8b), wherein each R^7b and R^8b are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₃-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆, aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl.

[0155]
or a pharmaceutically acceptable salt thereof

[0157]
or a pharmaceutically acceptable salt thereof, wherein R⁴ is halo.

[0159]
or a pharmaceutically acceptable salt thereof

[0162]

• • [0163] wherein R², R³, R⁴ and R⁵ are as defined above formula I; and
  • [0164] m is an integer from 0-6;
    • [0165] R¹⁸ is selected from H, halo, —OH, —COOH, —NH₂, —CN, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₆ haloalkoxyl, —R^7a, —X¹—R^7a, CHR^7aR^8a, —OR^7a, —O—X¹—R^7a, X¹—O—X¹—R^7a, —OC(O)(R^7a), —O—X¹—C(O)(R^7a), —C(O)(R^7a), —C(O)N(R^7aR^8a), —NR^7a(CO)R^8a, C(O)O(R^7a), S(O)₂R^7a, —S(O)₂N(R^7aR^8a), —N(R^7aR^8a), saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, mono or bicyclic aryl, 9-10 membered bicyclic heteroaryl containing 1-4 heteroatom ring vertices selected from N, O, and S, saturated or unsaturated 7-8 membered bridged heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, saturated or unsaturated 7-11 membered spiroheterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, and 6-11 membered bicyclic heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S; wherein
  • [0166] each X¹ is independently C_1-6 alkylene;
  • [0167] each R^7a and R^8a are independently selected from H, C₁-C₆ alkyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, C₁-C₁₆haloalkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, aryl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C:3-C₆ cycloalkoxyl, saturated or unsaturated 3-7 membered heterocyclyl containing 1-2 heteroatom ring vertices selected from N, O, and S, wherein the aryl and 3-7 membered heterocyclyl groups are substituted with 0-3 substituents selected from halo, —OH, —COOH, —NH, ═O, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl; and
  • [0168] the C₃-C₆ cycloalkyl, C₃-C₆ cycloalkoxyl, 3-7 membered heterocyclyl, the mono or bicyclic aryl, the 9-10 membered bicyclic heteroaryl, the saturated or unsaturated 7-8 membered bridged heterocyclyl, the saturated or unsaturated 7-11 membered spiroheterocycly, and the 6-11 membered bicyclic heterocyclyl are each independently substituted with 0 to 3 moieties selected from halo, —OH, —COOH, —NH₂, ==0, —CN, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, saturated or unsaturated C₃-C₆ cycloalkoxyl, —CHR^7bR^8b, —OR^7b, —OC(O)(R^7b), —C(O)(R^7b), —C(O)N(R^7bR^8b), —NR^7b(CO)R^8b, —C(O)O(R^7b), —S(O)₂N(R^7bR^8b) and —N(R^7bR^8b), wherein each R^7b and R^8a are independently selected from H, C₁-C₆ alkyl, C₁-C₆ alkenyl, C₁-C₆ hydroxyalkyl, C₁-C₆ haloalkyl, C₁-C₆ aminoalkyl, C₁-C₆ alkoxyl, saturated or unsaturated C₃-C₆ cycloalkyl, and saturated or unsaturated C₃-C₆ cycloalkoxyl;
    In some embodiments, in in formula IC is 1;
  • [0169] In some embodiments, R¹⁸ in formula IC is H.

[0175]
wherein the wavy line represents the point of attachment to the remainder of the formula.

[0177]
wherein the wavy line represents the point of attachment to the remainder of the formula.

[0179]
wherein the wavy line represents the point of attachment to the remainder of the formula.

[0181]
wherein the wavy line represents the point of attachment to the remainder of the formula.

[0187]

[0189]

Preparation of Compounds of Formula I and Exemplary Compounds

Analytical Details

[0220]

Example 1

Preparation of 4-2-(4-bromophenyl)propan-2-yl)thiazol-2-amine (Intermediate 1)

[0222]

Step 1. Preparation of compound 2-(4-bromophenyl)-2-methylpropanoyl chloride

[0223]

Step 2. Preparation of compound 2-(4-bromophenyl)-N-methoxy-N,2-dimethylpropanamide

[0225]

Step 3. Preparation of compound 3-(4-bromophenyl)-3-methylbutan-2-one

[0228]

Step 4. Preparation of compound 1-bromo-3-(4-bromophenyl)-3-methylbutan-2-one

[0231]

Step 5. Preparation of 4-(2-(4-bromophenyl)propan-2-yl)thiazol-2-amine

[0234]

4-1-(4-bromophenyl)cyclopentyl)thiazol-2-anine (Intermediate 2)

[0237]

Step 1. Preparation of compound ethyl 1-(4-bromophenyl)cyclopentane-1-carboxylate

[0238]

Step 2. Preparation of compound 1-(4-bromophenyl)cyclopentane-1-carboxylic acid

[0241]

4-(2-(5-bromopyridin-2-yl)propan-2-yl)thiazol-2-amine (Intermediate 3)

[0245]

Step 1. Preparation of compound methyl 2-(5-bromopyridin-2-yl)-2-methylpropanoate

[0246]

Step 2. Preparation of compound 2-(5-bromopyridin-2-yl)-2-methylpropanoic acid

[0248]

[0252]

TABLE 1
				LCMS
Com. ID	Structure	Name	HNMR	([M + H]+ =)
Intermediate 4		4-(2-(3-bromophenyl)propan-2- yl)thiazol-2-amine	1H NMR (400MHZ, CDCl3) δ 7.67 (t, J = 1.88 Hz, 1 H), 7.43 (d, J = 7.78 Hz, 1 H), 7.33- 7.39 (m, 1 H), 7.14-7.22 (m, 1 H), 6.48 (s, 1 H), 4.87 (br s, 2 H), 2.57 (s, 1 H), 1.91 (s, 3 H). MS (ESI) m/z (M + H)+ = 309.0.	297.0
Intermediate 5		4-(2-(3-methoxyphenyl)propan- 2-yl)thiazol-2-amine		249.1
Intermediate 6		4-(2-(4-bromo-3- methoxyphenyl)propan-2- yl)thiazol-2-amine		327.0
Intermediate 7		4-(2-(4-methoxyphenyl)propan- 2-yl)thiazol-2-amine		249.1
Intermediate 8		4-(2-(4- cyclopropylphenyl)propan-2- yl)thiazol-2-amine		259.1
Intermediate 9		4-(1-phenylethyl)thiazol-2- amine		205.0
Intermediate 10		4-(2-(4-fluorophenyl)propan-2- yl)thiazol-2-amine		237.0
Intermediate 11		4-(2-(4-chlorophenyl)propan-2- yl)thiazol-2-amine		253.0
Intermediate 12		4-(2-(4-bromo-3- fluorophenyl)propan-2- yl)thiazol-2-amine		314.9
Intermediate 13		4-(2-(4-chloro-3- fluorophenyl)propan-2- yl)thiazol-2-amine		271.0
Intermediate 14		4-(2-(4-iodophenyl)propan-2- yl)thiazol-2-amine		344.9
Intermediate 15		4-(1-(4- bromophenyl)ethyl)thiazol-2- amine		282.9
Intermediate 16		4-(2-(4-ethoxyphenyl)propan- 2-yl)thiazol-2-amine		263.1
Intermediate 17		4-(2-(4-bromophenyl)propan-2- yl)-5-methylthiazol-2-amine		311.0
Intermediate 18		4-(2-(4-bromophenyl)butan-2- yl)thiazol-2-amine		311.0
Intermediate 19		4-(2-(4-bromo-2- fluorophenyl)propan-2- yl)thiazol-2-amine		315.0
Intermediate 20		4-(2-(4- (trifluoromethoxy)phenyl) propan-2-yl)thiazol-2-amine		303.0
Intermediate 21		4-(2-(p-tolyl)propan-2- yl)thiazol-2-amine		233.1
Intermediate 22		4-(1-(4- bromophenyl)cyclobutyl) thiazol-2-amine	1H NMR (400MHz, CDCl3) δ 7.45-7.41 (m, 2H), 7.22-7.17 (m, 2H), 6.05 (s, 1H), 4.88 (s, 2H), 2.74-2.65 (m, 2H), 2.62- 2.51 (m, 2H), 2.20-2.04 (m, 1H), 1.97-1.85 (m, 1H). MS (ESI) m/z (M + H)+ = 311.0.	309.0
Intermediate 23		4-(2-(4-bromo-2- fluorophenyl)propan-2- yl)thiazol-2-amine		314.9
Intermediate 24		4-(1-(4- bromophenyl)cyclopropyl) thiazol-2-amine		294.9
Intermediate 25		4-(2-(3-bromo-4- methoxyphenyl)propan-2- yl)thiazol-2-amine		327.0
Intermediate 26		4-(2-(2-aminothiazol-4- yl)propan-2-yl)benzonitrile		244.1

[0253]

Example 2

Preparation of 4-(2-(4-chlorophenyl)but-3-In-2-yl)thiazol-2-amine (Intermediate 27)

[0255]

Step 1. Preparation of compound methyl 2-(4-chlorophenyl)-3-oxobutanoate

[0256]

Step 2. Preparation of compound methyl 2-(4-chlorophenyl)-2-methyl-3-oxobutanoate

[0259]

Step 3. Preparation of compound methyl 4-bromo-2-(4-chlorophenyl)-2-methyl-3-oxobutanoate

[0262]

Step 4. Preparation of compound methyl 2-(2-aminothiazol-4-yl)-2-(4-chlorophenyl)propanoate

[0265]

Step 5. Preparation of compound methyl 2-(2-acetamidothiazol-4-yl)-2-(4-chlorophenyl)propanoate

[0268]

Step 6. Preparation of compound N-(4-(2-(4-chlorophenyl)-1-hydroxypropan-2-yl)thiazol-2-yl)acetamide

[0271]

Step 7. Preparation of compound N-(4-(2-(4-chlorophenyl)-1-oxopropan-2-yl)thiazol-2-yl)acetamide

[0274]

Step 8. Preparation of compound N-(4-(2-(4-chlorophenyl)but-3-v-2-yl)thiazol-2-yl)acetamide

[0276]

Step 9. Preparation of compound 4-(2-(4-chlorophenyl)but-3-yn-2-yl)thiazol-2-amine

[0279]

[0283]

TABLE 2
Com. ID	Structure	Name	HNMR	LCMS
Intermediate 28		2-(2-aminothiazol-4-yl)-2-(4- methoxyphenyl)propan-1-ol		265.1
Intermediate 29		4-(2-(4-methoxyphenyl)but-3-yn- 2-yl)thiazol-2-amine		259.1
Intermediate 30		4-(2-(4-bromo-2- fluorophenyl)but-3-yn-2- yl)thiazol-2-amine	1H NMR (400 MHz, DMSO-d6) δ 7.52-7.46 (m, 1H), 7.45-7.39 (m, 2H), 6.93 (s, 2H), 6.42 (s, 1H), 3.44 (s, 1H), 1.84 (s, 3H). 19F NMR (376 MHz, DMSO-d6) δ −107.657	324.9
Intermediate 31		4-(3-(4-bromophenyl)pent-1-yn- 3-yl)thiazol-2-amine	1H NMR (400MHz, DMSO-d) δ = 7.60-7.58 (m, 2 H), 7.43-7.39 (m, 2 H), 6.74 (s, 1 H), 3.77 (s, 1 H), 2.32- 2.23 (m, 1 H), 2.18-2.11 (m, 1 H), 0.83 (t, J = 7.2 Hz, 3 H)	321.0
Intermediate 32		4-(2-(4-bromophenyl)but-3-yn-2- yl)thiazol-2-amine		306.9

Example 3

4-(2-(4-bromophenyl-1-methoxypropan-2-yl) thiazol-2-amine (Intermediate 33)

[0284]

Step 1. Preparation of compound N-(4-(2-(4-bromophenyl)-1-methoxypropan-2-yl)thiazol-2-yl)acetamide

[0285]

Step 2. Preparation of compound 4-(2-(4-bromophenyl)-1-methoxypropan-2-yl) thiazol-2-amine

[0288]

[0292]

TABLE 3
Com. ID	Structure	Name	HNMR	LCMS
Intermediate 34		4-(1-methoxy-2-(4- methoxyphenyl)propan-2- yl)thiazol-2-amine		279.1
Intermediate 35		4-(2-(4-bromo-2- fluorophenyl)-1- methoxypropan-2-yl)thiazol-2- amine		345.0
Intermediate 36		4-(1-methoxy-2-phenylpropan- 2-yl)thiazol-2-amine		248.1
Intermediate 37		4-(2-(4-chlorophenyl)-1- methoxypropan-2-yl)thiazol-2- amine		282.1

Example 4

1-(2-aminothiazol-4-yl)-1-(4-bromophenyl)ethan-1-ol (Intermediate 38)

[0293]

Step 1. Preparation of compound 1-(4-bromophenyl)propane-1,2-dione

[0294]

Step 2. Preparation of compound 3-bromo-1-(4-bromophenyl)propane-1,2-dione

[0296]

Step 3. Preparation of compound (2-aminothiazol-4-yl)(4-bromophenyl)methanone

[0298]

Step 4 Preparation of compound 1-(2-aminothiazol-4-yl)-1-(4-bromophenyl)ethan-1-ol

[0301]

General Method I

Example 5

Preparation of tert-butyl 4-(4-((3-(4-(2-(4-chloro-3-fluorophenyl)propan-2-yl)thiazol-2-yl)ureido)methyl)phenyl)piperazine-1-carboxylate

[0306]

General Method II

Example 6

Preparation of tert-butyl 4-(5-((3-(4-(2-(4-bromophenyl)propan-2-yl)thiazol-2-yl) ureido)methyl)pyrimidin-2-yl)piperazine-1-carboxylate

[0309]

General Method III

Example 7

Preparation of 1-(4-(4-((tert-butyldimethylsilyl)oxy)piperidin-1-yl)benzyl)-3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl)urea

[0315]

General Method IV

Example 8

Preparation of 1-ethyl-3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl)urea

[0319]

Example 9

Preparation of compound 1-(4-(2-(4-bromophenyl)propan-2-yl)thiazol-2-yl)-3-((6-(piperazin-1-yl)pyridin-3-yl)methyl)urea hydrochloride

[0322]

[0326]

TABLE 4
					Kinase	NFkB
					assay	assay
Com.					IC50	IC50
ID	Structure	Name	HNMR	LCMS	nM.	μM
A001		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(1-(6-(piperazin- 1-yl)pyridin-3- yl)ethyl)urea		[M + H]+ = 481	58	0.67
A002		1-(1-(2,5-difluoro-4- (piperazin-1- yl)phenyl)ethyl)-3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 516	63	0.70
A003		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (1-(3,5-difluoro-4- (piperazin-1- yl)phenyl)ethyl)urea		[M + H]+ = 564	45	1.20
A004		1-(4-(2-(4- bromophenyl)propan- 2-yl) thiazol-2-yl)-3- (pyrimidin-5- ylmethyl)urea		[M + H]+ = 432	240	2.03
A005		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-(piperazin-1- yl)benzyl)urea		[M + H]+ = 514	97	3.15
A006		1-(4-((3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido)methyl) phenyl)piperidine-4- carboxamide		[M + H]+ = 556	104
A007		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(pyrazin-2- ylmethyl)urea		[M + H]+ = 384	91	5.58
A008		4-((3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido)methyl) benzamide		[M + H]+ = 473	8	0.70
A009		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(3- hydroxypyrrolidin-1- yl)benzyl)urea		[M + H]+ = 515	154	3.15
A010		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((6-(4-(2- hydroxyethyl) piperazin-1- yl)pyridin-3- yl)methyl)urea		[M + H]+ = 559	200	3.95
A011		1-((6-(3- (dimethylamino) pyrrolidin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 495	49	1.37
A012		1-((2-(3- (dimethylamino) pyrrolidin-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 496	40	2.21
A013		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(2- (methylsulfonyl)ethyl) urea		[M + H]+ = 398	316	2.97
A014		1-((6-((2- hydroxyethyl)amino) pyridin-3-yl)methyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 442	160	0.88
A015		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- (1-methylpiperidin-4- yl)picolinamide		[M + H]+ = 523	24	0.88
A016		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-((4- methylpiperazin-1- yl)methyl)benzyl)urea		[M + H]+ = 542	27	2.34
A017		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-chloro-4- fluorobenzyl)urea		[M + H]+ = 482	204	0.97
A018		4-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- (1-methylpiperidin-4- yl)benzamide		[M + H]+ = 522	29	1.28
A019		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-((6-((1- methylpiperidin-4- yl)amino)pyridin-3- yl)methyl)urea		[M + H]+ = 495	32	1.29
A020		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2-fluoroethyl)urea	1H NMR (400 MHz, cdcl3) δ 7.40-7.35 (m, 2H), 7.15-7.10 (m, 2H), 6.42 (s, 1H), 4.54-4.49 (m, 1H), 4.41-4.37 (m, 1H), 3.55 (ddd, J = 28.1, 10.0, 5.2 Hz, 2H), 1.63 (s, 6H).	[M + H]+ = 386	144	6.79
A021		1-(2-fluoroethyl)-3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, dmso) δ 10.53 (s, 1H), 7.12-7.00 (m, 2H), 6.83-6.68 (m, 2H), 6.60 (s, 1H), 6.48 (s, 1H), 4.40 (dt, J = 47.5, 5.0 Hz, 2H), 3.72-3.58 (m, 3H), 3.37 (ddd, J = 26.8, 10.6, 5.2 Hz, 2H), 1.60-1.46 (m, 6H).	[M + H]+ = 338	104	1.39
A022		1-((6-((2- hydroxyethyl)amino) pyridin-3-yl)methyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, MeOD) δ 7.85 (dd, J = 9.3, 1.9 Hz, 1H), 7.75 (s, 1H), 7.20-7.15 (m, 2H), 7.08 (d, J = 9.3 Hz, 1H), 6.87-6.81 (m, 2H), 6.78 (s, 1H), 4.31 (s, 2H), 3.85-3.78 (m, 2H), 3.78-3.73 (m, 3H), 3.55-3.48 (m, 2H), 1.67 (s, 6H).	[M + H]+ = 442	232	0.96
A023		1-((6-((2- hydroxyetbyl)(methyl) amino)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, MeOD) δ 7.94 (dd, J = 9.5, 2.1 Hz, 1H), 7.84 (d, J = 1.6 Hz, 1H), 7.31 (d, J = 9.5 Hz, 1H), 7.21-7.16 (m, 2H), 6.88-6.85 (m, 1H), 6.85 (d, J = 2.1 Hz, 1H), 6.84 (s, 1H), 4.35 (s, 2H), 3.85 (t, J = 4.8 Hz, 2H), 3.80-3.77 (m, 2H), 3.77 (s, 3H), 3.29 (s, 3H), 1.68 (s, 6H).	[M + H]+ = 456	229	1.32
A024		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2-cyanoethyl)urea	1H NMR (400 MHz, (CD3)2SO) δ 7.40 (d, 2H), 7.25 (m, 2H), 6.75 (s, 1H), 3.47 (m, 2H), 2.55 (m, 3H), 1.92 (s, 3H).	[M + H]+ = 359	13	1.25
A025		1-(4-(2-(4- cyclopropylphenyl) propan-2-yl)thiazol-2- yl)-3-(4-(piperazin-1- yl)benzyl)urea		[M + H]+ = 476	334	8.58
A026		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- ylmethyl)benzyl)urea		[M + H]+ = 528	117	1.25
A027		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- yl)benzyl)urea		[M + H]+ = 514	46	1.45
A028		1-(4-aminobutyl)-3- (4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 411	53	2.56
A029		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(2-methylpiperazin- 1-yl)benzyl)urea		[M + H]+ = 528	73
A030		1-(4-(2-(4- bromophenyl)propan- 2-yl)-5-methylthiazol- 2-yl)-3-(4-(piperazin- 1-yl)benzyl)urea		[M + H]+ = 528	232	4.11
A031		1-(4-(2-(4-chloro-3- fluorophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- yl)benzyl)urea		[M + H]+ = 488	345	1.45
A032		1-(4-(3- aminopyrrolidin-1- yl)benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 514	291	0.58
A033		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(2-oxo-2- (piperazin-1- yl)ethoxy)benzyl)urea		[M + H]+ = 572	80	3.19
A034		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(2-(piperazin-1- yl)ethoxy )benzyl)urea		[M + H]+ = 558	114	0.73
A035		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(3-(piperazin-1- yl)propoxy )benzyl)urea		[M + H]+ = 572	52	2.03
A036		1-((5-fluoro-6- (piperazin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 485	24	0.62
A037		1-(3-fluoro-4- (piperazin-1- ylmethyl)benzyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 498	57	2.51
A038		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((5-fluoro-6- (piperazin-1- yl)pyridin-3- yl)methyl)urea		[M + H]+ = 533	30	1.66
A039		1-(4-(2-(4- bromophenyl)butan-2- yl)thiazol-2-yl)-3-(4- (piperazin-1- yl)benzyl)urea		[M + H]+ = 528	189	0.711
A040		1-(3,5-difluoro-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 502	45	0.50
A041		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(4-(piperidin-4- ylamino)benzyl)urea		[M + H]+ = 480	23	1.86
A042		4-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- (piperidin-4- yl)benzamide		[M + H]+ = 508	15
A043		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-((6-(piperazin-1- yl)pyridin-2- yl)methyl)urea		[M + H]+ = 467	165
A044		1-(4-(1-(4- bromophenyl)ethyl) thiazol-2-yl)-3-(4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, cd3od) δ 7.45 (d, J = 6.9 Hz, 2H), 7.22 (s, 2H), 7.14 (s, 2H), 6.97 (s, 3H), 4.32 (s, 2H), 4.18 (s, 1H), 3.37 (s, 4H), 3.33 (s, 4H), 1.59 (s, 3H).	[M + H]+ = 500	147	1.11
A045		1-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)-3-(4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 9.28 (s, 1H), 7.39 (d, J = 8.3 Hz, 1H), 7.19 (d, J = 8.5 Hz, 2H), 7.13 (d, J = 8.3 Hz, 2H), 6.93 (d, J = 8.5 Hz, 2H), 6.76 (s, 1H), 4.18 (d, J = 4.4 Hz, 2H), 3.31 (s, 4H), 3.16 (s, 4H), 2.41 (d, J = 12.9 Hz, 2H), 1.95 (s, 2H), 1.59 (d, J = 9.0 Hz, 4H).	[M + H]+ = 540	24	1.07
A046		1-(4-(2-(4- chlorophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 8.99 (s, 1H), 7.26 (d, J = 8.5 Hz, 2H), 7.17 (d, J = 8.4 Hz, 2H), 7.12 (d, J = 8.2 Hz, 2H), 6.91 (d, J = 8.7 Hz, 3H), 6.70 (s, 1H), 4.17 (d, J = 5.8 Hz, 2H), 3.28 (s, 4H), 3.17 (s, 4H), 1.54 (s, 6H).	[M + H]+ = 470	79	1.06
A047		1-(4-(2-(4- fluorophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 7.18 (dd, J = 8.1, 5.7 Hz, 2H), 7.12 (d, J = 8.2 Hz, 2H), 7.01 (t, J = 8.6 Hz, 2H), 6.89 (d, J = 8.1 Hz, 2H), 6.84 (s, 1H), 6.66 (s, 1H), 4.17 (d, J = 5.6 Hz, 2H), 3.24 (d, J = 5.3 Hz, 4H), 3.13 (d, J = 5.0 Hz, 4H), 1.54 (s, 6H).	[M + H]+ = 454	167	2.10
A048		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2-chloro-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 9.24 (s, 1H), 7.39 (d, J = 8.6 Hz, 2H), 7.19 (d, J = 8.6 Hz, 1H), 7.12 (d, J = 8.6 Hz, 3H), 7.01 (d, J = 2.3 Hz, 1H), 6.90 (dd, J = 8.7, 2.3 Hz, 1H), 6.70 (s, 1H), 4.25 (d, J = 5.7 Hz, 2H), 3.43-3.28 (m, 4H), 3.13 (s, 4H), 1.54 (s, 6H).	[M + H]+ = 548	138	1.53
A049		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1-yl)-3- (trifluoromethyl) benzyl)urea	1H NMR (400 MHz, dmso) δ 9.11 (s, 2H), 7.54 (d, J = 9.0 Hz, 2H), 7.46 (d, J = 8.1 Hz, 1H), 7.38 (d, J = 8.5 Hz, 2H), 7.19 (s, 1H), 7.11 (d, J = 8.5 Hz, 2H), 6.70 (s, 1H), 4.30 (d, J = 5.7 Hz, 2H), 3.10 (d, J = 17.0 Hz, SH), 3.01 (d, J = 3.9 Hz, SH), 1.56 (d, J = 22.5 Hz, 8H).	[M + H]+ = 582	119	0.8
A050		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-fluoro-4-(piperazin- 1-yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 9.31 (s, 1H), 7.31 (d, J = 44.6 Hz, 3H), 7.04 (d, J = 44.4 Hz, 5H), 6.68 (s, 1H), 4.18 (s, 2H), 3.15 (s, 8H), 1.51 (s, 6H).	[M + H]+ = 532	26	1.21
A051		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2-methyl-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 10.54-10.45 (m, 1H), 9.02 (s, 1H), 7.39 (d, J = 8.6 Hz, 2H), 7.11 (d, J = 8.6 Hz, 2H), 7.05 (d, J = 8.5 Hz, 1H), 6.78 (s, 2H), 6.74 (d, J = 8.5 Hz, 1H), 6.70 (s, 1H), 4.17 (d, J = 5.4 Hz, 2H), 3.28 (d, J = 5.5 Hz, 4H), 3.16 (s, 4H), 2.20 (s, 3H), 1.54 (s. 6H).	[M + H]+ = 528	125	0.29
A052		5-((3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido)methyl)-2- (piperazin-1- yl)benzamide	1H NMR (400 MHz, dmso) δ 9.35 (s, 1H), 8.04 (s, 1H), 7.54-7.32 (m, 3H), 7.23 (d, J = 29.5 Hz, 2H), 7.09 (d, J = 19.3 Hz, 3H), 6.70 (s, 1H), 3.13 (d, J = 46.5 Hz, 8H), 2.66 (d, J = 17.4 Hz, 2H), 1.53 (s, 6H).	[M + H]+ = 557	24	1.96
A053		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, dmso) δ 9.15 (s, 1H), 7.09 (d, J = 18.4 Hz, 4H), 6.90 (s, 2H), 6.75 (s, 2H), 6.61 (s, 1H), 4.17 (s, 2H), 3.65 (s, 3H), 3.28 (s, 4H), 3.15 (s, 4H), 1.52 (s, 6H).	[M + H]+ = 466	43	0.76
A054		1-(3-fluoro-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, cd3od) δ 10.12 (s, 2H), 8.12 (s, 1H), 7.81 (d, J = 23.1 Hz, 5H), 7.53 (s, 2H), 7.39 (s, 1H), 4.97 (s, 2H), 4.43 (s, 3H), 3.93 (s, 8H), 2.29 (s. 6H).	[M + H]+ = 484	30	0.88
A055		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-(2- methoxyethoxy)-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, cd3od) δ 7.48 (d. J = 8.4 Hz, 2H), 7.19 (d, J = 7.1 Hz, 2H), 7.11 (s, 1H), 7.00 (s, 2H), 6.93 (s, 1H), 4.38 (s, 2H), 4.19 (s, 4H), 3.77 (s, 4H), 3.43 (s, 4H), 3.40 (s, 3H), 1.69 (s, 6H).	[M + H]+ = 588	182	4.70
A056		1-(4-(1-(4- bromophenyl)-1- hydroxyethyl)thiazol- 2-yl)-3-(3-fluoro-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, cd3od) δ 7.46 (d, J = 8.4 Hz, 2H), 7.38 (d, J = 8.5 Hz, 2H), 7.04 (t, J = 9.9 Hz, 4H), 4.36 (d, J = 6.7 Hz, 2H), 3.29 (s, 8H), 1.84 (d, J = 13.6 Hz, 3H).	[M + H]+ = 534	176	1.06
A057		1-(4-(2-(5- bromopyridin-2- yl)propan-2- yl)thiazol-2-yl)-3-(3- fluoro-4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, cd3od) δ 8.48 (d, J = 2.3 Hz, 1H), 7.80-7.73 (m, 1H), 7.08 (d, J = 8.4 Hz, 1H), 7.01 (d, J = 4.2 Hz, 2H), 6.99 (s, 1H), 6.73 (s, 1H), 4.30 (s, 2H), 3.25 (s, 4H), 3.23 (s, 4H), 1.64 (s, 6H).	[M + H]+ = 533	246
A058		1-(3-(hydroxymethyl)- 4-(piperazin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, cd3od) δ 7.41 (d, J = 4.2 Hz, 2H), 7.21 (s. 1H), 7.15 (d, J = 6.7 Hz, 1H), 7.12 (d, J = 5.9 Hz, 2H), 6.88 (s, 1H), 6.85 (s, 1H), 6.82 (d, J = 5.7 Hz, 2H), 4.67 (s, 2H), 4.38 (s, 2H), 3.74 (s, 3H), 3.25-3.22 (m, 4H), 3.17-3.11 (m, 4H), 1.63 (s, 6H).	[M + H]+ = 496	130	3.10
A059		1-(4-(2-(4- ethoxyphenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, cd3od) δ 7.17 (t, J = 5.9 Hz, 2H), 7.09 (dd, J = 9.4, 2.7 Hz, 2H), 6.96 (d, J = 8.7 Hz, 2H), 6.78-6.73 (m, 2H), 6.58 (s, 1H), 4.28 (s, 2H), 3.96 (q, J = 7.0 Hz, 2H), 3.34 (d. J = 3.6 Hz, 4H), 3.33 (s, 4H), 1.57 (s, 6H), 1.37-1.29 (m, 3H).	[M + H]+ = 480	269
A060		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-2- (piperazin-1- yl)benzamide	1H NMR (400 MHz, dmso) δ 9.35 (s, 2H), 8.05 (s, 1H), 7.53 (d, J = 2.0 Hz, 1H), 7.48 (s, 1H), 7.30 (d, J = 10.1 Hz, 2H), 7.08 (t, J = 8.0 Hz, 3H), 6.78 (d, J = 8.8 Hz, 2H), 6.65 (s, 1H), 4.24 (d, J = 5.2 Hz, 2H), 3.66 (s, 3H), 3.20 (s, 4H), 3.08 (s, 4H), 1.54 (s, 6H).	[M + H]+ = 509	8	4.80
A061		1-(3-aminopropyl)-3- (4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, dmso) δ 8.08 (s, 3H), 7.49 (s, 1H), 7.40 (d. J = 8.2 Hz, 2H), 7.11 (d, J = 8.2 Hz, 2H), 6.78 (s, 1H), 4.82 (s, 5H), 2.73 (s, 2H), 1.70 (s, 2H), 1.53 (s, 6H).	[M + H]+ = 397	195	1.99
A062		1-(4-(2,5- diazabicyclo[2.2.1] heptan-2-yl)benzyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, cd3od) δ 7.22-7.15 (m, 4H), 7.09 (s, 1H), 6.89 (d, J = 8.8 Hz, 2H), 6.64 (d, J = 8.5 Hz, 2H), 4.62 (s, 1H), 4.46 (s, 1H), 4.30 (s, 2H), 3.75 (s, 3H), 3.69 (dd, J = 10.7, 2.2 Hz, 1H), 3.31-3.27 (m, 3H), 2.25 (d, J = 11.0 Hz, 1H), 2.04 (d, J = 11.2 Hz, 1H), 1.68 (s. 6H).	[M + H]+ = 478	60	1.33
A063		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-2- (3-methylpiperazin-1- yl)benzamide	1H NMR (400 MHz, MeOD) δ 7.70 (d, J = 2.0 Hz, 1H), 7.50 (dd, J = 8.3, 2.0 Hz, 1H), 7.28 (d, J = 8.3 Hz, 1H), 7.23 (s, 1H), 7.20 (s, 1H), 7.14 (s, 1H), 6.93 (d, J = 8.8 Hz, 2H), 4.47 (s, 2H), 3.79 (s, 3H), 3.56-3.48 (m, 1H), 3.46-3.41 (m, 1H), 3.38 (d, J = 11.9 Hz, 1H), 3.17 (d, J = 12.7 Hz, 1H), 3.00 (d, J = 13.9 Hz, 1H), 2.97-2.91 (m, 1H), 2.90-2.84 (m, 1H), 1.72 (s, 6H), 1.40 (d, J = 6.6 Hz, 3H).	[M + H]+ = 523	29	2.91
A064		2-(2,5- diazabicyclo[2.2.1] heptan-2-yl)-5-((3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl) benzamide	1H NMR (400 MHz, DMSO) δ 10.70 (s, 1H), 9.72 (s, 1H), 8.89 (s, 1H), 7.68 (s, 1H), 7.37 (s, 1H), 7.23 (d, J = 1.9 Hz, 1H), 7.18 (dd, J = 8.5, 1.9 Hz, 1H), 7.13 (d, J = 8.8 Hz, 2H), 6.80 (dd, J = 14.2, 8.7 Hz, 3H), 6.68 (d. J = 1.1 Hz, 1H), 5.44 (s, 5H), 4.48 (s, 1H), 4.35 (s, 1H), 4.22 (d, J = 5.1 Hz, 2H), 3.71 (s, 3H), 3.17 (s, 1H), 3.11 (d, J = 10.7 Hz, 1H), 2.04 (d, J = 10.5 Hz, 1H), 1.95-1.89 (m, 1H), 1.58 (s, 6H).	[M + H]+ = 521	41	19.73
A065		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- methyl-2-(piperazin-1- yl)benzamide	1H NMR (400 MHz, dmso) δ 9.42 (s, 1H), 8.45 (s, 1H), 7.51 (d, J = 28.5 Hz, 2H), 7.28 (d, J = 8.0 Hz, 1H), 7.07 (t, J = 10.0 Hz, 3H), 6.78 (d, J = 8.4 Hz, 2H), 6.67 (s, 1H), 4.23 (s, 2H), 3.66 (s, 3H), 3.18 (s, 4H), 3.06 (s, 4H), 2.77 (d, J = 3.7 Hz, 3H), 2.46 (s, 1H), 1.54 (s, 6H).	[M + H]+ = 523	30	4.44
A066		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2- (methylsulfonyl)ethyl) urea		[M + H]+ = 446	126	10.50
A067		1-(4-(2-(4- iodophenyl)propan-2- yl)thiazol-2-yl)-3-(4- (piperazin-1- yl)benzyl)urea		[M + H]+ = 562	28	1.11
A068		1-((2-(3- aminopyrrolidin-1- yl)pyrimidin-5-yl) methyl)-3-(4-(2-(4- chlorophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 472	269
A069		1-(4-(3- hydroxypyrrolidin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 467	269
A070		4-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)-N-(1- methylpiperidin-4- yl)butanamide		[M + H]+ = 474	140	16.91
A071		4-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)-N- (piperidin-4- yl)butanamide		[M + H]+ = 460	64
A072		1-(2-(2-(3- aminopyrrolidin-1- yl)ethoxy)ethyl)-3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 448	143	1.45
A073		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (1-(4-(piperazin-1- yl)phenyl)ethyl)urea		[M + H]+ = 528	85	2.79
A074		1-(3-hydroxy-2- oxopropyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 364	61
A075		1-(4-(piperazin-1- yl)benzyl)-3-(4-(2-(p- tolyl)propan-2- yl)thiazol-2-yl)urea		[M + H]+ = 450	25	0.267
A076		1-(4-(2-(4- methoxyphenyl)butan- 2-yl)thiazol-2-yl)-3- (1-(4-(piperazin-1- yl)phenyl)ethyl)urea		[M + H]+ = 494	147	4.48
A077		1-(4-(3- aminopyrrolidin-1- yl)butyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 432	180	2.97
A078		1-((2-(3- aminopyrrolidin-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, DMSO) δ 8.46 (br, 5H), 7.39 (d, J = 8.8 Hz, 2H), 7.32 (s, 1H), 7.10 (d, J = 8.8 Hz, 2H), 6.73 (s, 1H), 4.15 (s, 2H), 3.70-3.59 (m, 5H), 2.30-2.27 (m, 1H), 2.16-2.13 (m, 1H), 1.53 (s, 6H).	[M + H]+ = 516.1	8
A079		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(3- hydroxypyrrolidin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, CDCl3) δ 8.13 (s, 2H), 7.34 (d, J = 8.4 Hz, 2H), 7.05 (d, J = 8.4 Hz, 2H), 6.48 (s, 1H), 4.49 (br s, 1H), 4.07 (br d, J = 4.0 Hz, 2H), 3.85-3.50 (m, 4H), 2.22-1.92 (m, 3H), 1.59 (s, 6H), 1.26 (s, 1H).	[M + H]+ = 519.2	170	1.68
A080		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2- methoxypyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.72 (s, 1H), 8.49 (s, 2H), 7.39 (d, J = 8.56 Hz, 2H), 7.14-7.07 (m, 2H), 6.85-6.79 (m, 1H), 6.70 (s, 1H), 4.20 (s, 2H), 3.82-3.87 (m, 3H), 1.53 (s, 6H).	[M + H]+ = 461.9	172	13.30
A081		1-((2-((2- aminoethyl)amino) pyrimidin-5- yl)methyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, DMSO- d6) δ 8.44 (s, 2H), 8.06 (br s, 3H), 7.43 (d, J = 8.56 Hz, 2H), 7.24 (br s, 1H), 7.14 (d, J = 8.56 Hz, 2H), 6.75 (s, 1H), 4.17 (br d, J = 5.38 Hz, 2H), 3.52-3.65 (m, 2H), 2.88-3.04 (m, 2H), 1.57 (s, 6H).	[M + H]+ = 492.1	17	1.84
A082		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(4- hydroxypiperidin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.65 (s, 1H), 8.27 (s, 2H), 7.42 (d, J = 8.6 Hz, 2H), 7.14 (d, J = 8.8 Hz, 2H), 6.77-6.67 (m, 2H), 4.74-4.68 (m, 1H), 4.27-4.19 (m, 2H), 4.12-4.06 (m, 2H), 3.75-3.66 (m, 1H), 3.26-3.18 (m, 2H), 1.79-1.71 (m, 2H), 1.57 (s, 6H), 1.31-1.24 (m, 2H).	[M + H]+ = 533.0	125	6.15
A083		1-((2-(3- hydroxypyrrolidin-1- yl)pyrimidin-5-yl) methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 8.16 (s, 2H), 7.15-7.03 (m, 2H), 6.79-6.77 (m, 1H), 6.83-6.72 (m, 1H), 6.46-6.38 (m, 1H), 4.55-4.49 (m, 1H), 4.15-4.06 (m, 2H), 3.77 (s, 3H), 3.71-3.59 (m, 4H), 2.13-2.02 (m, 2H), 1.58 (s, 6H)	[M + H]+ = 469.2	111	0.68
A084		1-(4-(2-(4- chlorophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, dmso) δ 9.17 (s, 1H), 8.34 (s, 2H), 7.25 (d. J = 8.0 Hz, 2H), 7.16 (d, J = 8.0 Hz, 2H), 7.02 (s. 1H), 6.69 (s, 1H), 4.11 (s, 2H), 3.90 (s, 4H), 3.09 (s, 4H), 1.53 (s, 6H).	[M + H]+ = 472	22	0.34
A085		1-(4-(2-(4- fluorophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, dmso) δ 9.34 (s, 1H), 8.35 (s, 1H), 7.22 (d, J = 40.8 Hz, 2H), 7.01 (s, 2H), 6.69 (s, 1H), 4.11 (s, 2H), 3.91 (s, 4H), 3.08 (s, 4H), 1.54 (s, 6H).	[M + H]+ = 456	85	0.49
A086		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, cd3od) δ 8.47 (s, 2H), 7.17 (s, 2H), 7.09 (s, 1H), 6.88 (s, 2H), 4.32 (s, 2H), 4.09 (s, 3H), 3.74 (s, 4H), 3.32 (d. J = 5.5 Hz, 4H), 1.67 (s, 6H).	[M + H]+ = 468	16	0.39
A087		1-(4-(2-(4- ethoxyphenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, cd3od) δ 8.57 (s, 2H), 7.15 (d, J = 8.2 Hz, 2H), 7.11 (s, 1H), 6.87 (d, J = 8.2 Hz, 2H), 4.37 (s, 2H), 4.14 (s, 4H), 3.99 (q, J = 6.9 Hz, 2H), 3.34 (d, J = 12.6 Hz, 4H), 1.68 (s, 6H), 1.34 (t, J = 6.9 Hz, 3H)	[M + H]+ = 482	89	1.74
A088		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea compound with methane (1:1)	1H NMR (400 MHz, MeOD) δ 8.51 (s, 2H), 7.53-7.51 (m, 2H), 7.24-7.22 (m, 2H), 7.15 (s, 1H), 4.36 (s, 2H), 4.14-4.12 (m, 4H), 3.34-3.33 (m, 4H), 1.73 (s, 6H).	[M + H]+ = 518.0	13	1.45
A089		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((4-methyl-2- (piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.70 (br s, 1H), 9.37 (br s, 2H), 8.21 (s, 1H), 7.42 (d, J = 8.3 Hz, 2H), 7.34-7.26 (m.1H), 7.14 (d, J = 8.6 Hz, 2H), 6.75 (s, 1H), 4.20 (br d, J = 5.1 Hz, 2H), 4.01-3.91 (m, 4H), 3.12 (br s, 4H), 2.37 (s, 3H), 1.57 (s, 6H)	[M + H]+ = 532	26	1.19
A090		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-4- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6)) 9.45 (br s, 2H), 8.35 (d, J = 5.1 Hz, 1H), 7.41-7.47 (m, 3H). 7.24-7.34 (m, 2H), 7.11-7.21 (m, 3H), 6.75 (s, 1H), 6.67 (d, J = 5.1 Hz, 1H), 4.28 (br s, 1H), 4.27 (br s, 1H), 4.05 (s, 1H), 3.05 (s. 1H), 1.58 ppm (s, 6H)		178	1.11
A091		1-((2-(1,4-diazepan-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, DMSO- d6) δ 9.24 (br s, 2H), 8.31 (d, J = 5.0 Hz, 1H), 7.45 (s, 1H), 7.42 (d, J = 3.3 Hz, 2H), 7.29 (s, 1H), 7.17 (d, J = 1.8 Hz, 2H), 7.15-7.14 (m, 1H), 6.74 (s, 1H), 6.64 (d, J = 5.0 Hz, 1H), 4.28 (br d, J = 5.3 Hz, 2H), 4.01 (br s, 2H), 3.20 (br s, 2H), 3.16-3.08 (m, 2H), 2.09-2.01 (m, 2H), 1.58 (s, 6H), 1.26-1.19 (m, 2H).	[M + H]+ = 530.0	135	3.45
A092		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((6-(piperazin-1- yl)pyridin-3- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) ¿ 10.90 (br s, 1H), 9.66 (br s, 2H), 8.05-7.92 (m, 2H), 7.48-7.28 (m, 4H), 7.21-7.10 (m, 2H), 6.75 (s, 1H), 4.30-4.20 (m, 2H), 4.04-3.92 (m, 4H), 3.24 (br s, 4H), 1.57 (s, 6H)	[M + H]+ = 517.2	20	0.57
A093		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((5-(piperazin-1- yl)pyrazin-2- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 9.26 (s, 2H), 8.30 (s, 1H), 8.07 (s, 2H), 7.41-7.36 (m, 2H), 7.13-7.11 (m, 3H), 6.72 (s, 1H), 4.29-4.28 (m, 2H), 3.76-3.74 (m, 4H), 3.16-3.14 (m, 4H), 1.54 (s, 6H).	[M + H]+ = 516.1	9	0.32
A094		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((6-(piperazin-1- yl)pyrimidin-4- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 11.05 (br s, 1H), 9.70 (br s, 2H), 8.86 (s, 1H), 7.48-7.43 (m, 2H), 7.39-7.33 (m, 1H), 7.21-7.14 (m, 3H), 6.78 (s, 1H), 4.45 (br d, J = 6.0 Hz, 2H), 4.11 (br s, 4H), 3.25 (br s, 4H), 1.59 (s, 6H).	[M + H]+ = 518.2	73	1.29
A095		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-methyl-6- (piperazin-1- yl)pyrimidin-4- yl)methyl)urea	1H NMR (400 MHz, DMSO) δ 7.40 (d, J = 8.4 Hz, 2H), 7.13 (d. J = 8.8 Hz, 2H), 6.87 (s, 1H), 6.70 (s, 1H), 6.43 (s, 1H), 4.12 (s, 2H), 3.46-3.39 (m, 4H), 2.69-2.67 (m, 4H), 2.30 (s, 3H), 1.55 (s, 6H).	[M + H]+ = 532.1	32
A096		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-methy 1-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.61 (br s, 1H), 9.04 (br s, 2H), 7.40 (d, J = 8.8 Hz, 2H), 7.12 (d, J = 8.8 Hz, 2H), 7.07-6.99 (m, 2H), 6.95 (br d, J = 7.6 Hz. 2H), 6.71 (s, 1H), 4.18 (br d, J = 5.6 Hz, 2H), 3.17 (br s, 4H), 2.97 (br d, J = 4.4 Hz, 4H), 2.19 (s, 3H), 1.54 (s, 6H).	[M + Na]+ = 552.0	69	1.43
A097		1-(3-bromo-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, CDCl3) δ 9.18 (brs, 2H), 7.43 (d, J = 8.4 Hz, 2H), 7.57-7.29 (m, 1H), 7.18-7.13 (m, 4H), 6.75 (s, 1H), 4.24 (s, 2H), 3.23-3.14 (m, 8H), 1.58 (s, 6H).	[M + H]+ = 593.03	87	1.42
A098		1-(3-amino-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, DMSO) δ 10.76 (br, 1H), 9.22 (br, 2H), 7.42-7.39 (m, 2H), 7.26- 7.12 (m, 6H), 6.71 (s, 1H), 4.26-4.25 (m, 2H), 3.24-3.22 (m, 4H), 3.03-3.02 (m, 4H), 1.55 (s, 6H).	[M + H]+ = 530.9	31	1.07
A099		1-((2-(4- aminopiperidin-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.94-10.50 (m, 1H), 8.34 (s, 2H), 8.25-7.95 (m, 3H), 7.42 (d, J = 8.5 Hz, 2H), 7.19-6.92 (m, 3H), 6.74 (s, 1H), 4.71-4.54 (m, 2H), 4.19-4.05 (m, 2H), 3.38-3.24 (m, 1H), 3.04-2.87 (m, 2H), 2.03-1.90 (m, 2H), 1.57 (s, 6H), 1.49-1.35 (m, 2H).	[M + H]+ = 532.0	13	0.45
A100		4-((3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido)methyl)-N- (1-methylpiperidin-4- yl)cyclohexane-1- carboxamide		[M + H]+ = 576	72	1.37
A101		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2-hydroxy-1-(4- (piperazin-1- yl)phenyl)ethyl)urea		[M + H]+ = 544	50	1.65
A102		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-(piperazin-1- yl)propyl)urea		[M + H]+ = 466	90	0.71
A103		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(4-(2- hydroxyethyl) piperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 560	97	6.2
A104		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(pyrimidin-5- ylmethyl)urea		[M + H]+ = 384	223	1.69
A105		1-((5-fluoro-6-((2- hydroxyethyl)amino) pyridin-3-yl)methyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 460	144	1.02
A106		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((6-(3- (dimethylamino) pyrrolidin-1- yl)pyridin-3- yl)methyl)urea		[M + H]+ = 543	48	6.72
A107		1-(4-(2-(4- bromophenyl)propan- 2-yl) thiazol-2-yl)-3- (3-fluoro-4- methoxybenzyl)urea		[M + H]+ = 478	216
A108		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-((2- hydroxyethyl)amino) benzyl)urea		[M + H]+ = 489	244	0.82
A109		1-(4-((2- hydroxyethyl)amino) benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 441	146
A110		1-(2-methoxyethyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 350	193	0.94
A111		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3- methoxypropyl)urea		[M + H]+ = 364	127	1.24
A112		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((5-fluoro-6-(3- oxopiperazin-1- yl)pyridin-3- yl)methyl)urea		[M + H]+ = 547	334
A113		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(3-oxopiperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 530	126
A114		4-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)butanamide		[M + H]+ = 377	260
A115		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- (1-propylpiperidin-4- yl)picolinamide		[M + H]+ = 551	19	0.83
A116		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-2- (4-propylpiperazin-1- yl)benzamide		[M + H]+ = 551	72	0.72
A117		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3,5-difluoro-4-((4- methy lpiperazin-1- yl)methyl)benzyl)urea		[M + H]+ = 578	67	5.03
A118		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (1-(4-((4- methylpiperazin-1- yl)methyl)phenyl) ethyl)urea		[M + H]+ = 556	227	4.38
A119		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-((2- hydroxyethyl)amino) pyrimidin-5- yl)methyl)urea		[M + H]+ = 491	36	4.43
A120		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- (1-methylpiperidin-4- yl)picolinamide		[M + H]+ = 523	53	0.99
A121		1-((5-fluoro-6-(3- oxopiperazin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 499	209	2.02
A122		1-(4- hydroxycyclohexyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 390	219	1.70
A123		1-(3- hydroxycyclohexyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 390	354	2.40
A124		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(2-(pyridin-4- yl)ethyl)urea		[M + H]+ = 397	165	1.05
A125		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- isopropylurea	1H NMR (400 MHz, CDCl3) δ 8.57 (br s, 1H), 7.39 (d, J = 8.8 Hz, 2H), 7.13 (d, J = 8.4 Hz, 2H), 6.43 (s, 1H), 3.96-3.82 (m, 1H), 1.64 (s, 6H), 1.10 (d, J = 6.4 Hz, 2H).	[M + H]+ = 382.1	28	2.80
A126		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-hydroxypropyl)urea	1H NMR (400 MHz, CDCl3) δ 7.30-7.26 (m, 2H), 7.15-7.10 (m, 2H), 6.47 (s, 1H), 3.60-3.55 (m, 2H), 3.45-3.30 (m, 2H), 1.63 (s, 6H), 1.40-1.30 (m, 2H).	[M + H]+ = 398.1	88	2.96
A127		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-morpholinopropyl) urea	1H NMR (400 MHz, DMSO- d6) δ 10.50 (br s, 1H), 7.40 (d, J = 8.56 Hz, 2H), 7.12 (d, J = 8.56 Hz, 2H), 6.68 (s, 1H), 6.29 (br s, 1H), 3.53 (t, J = 4.52 Hz, 4H), 3.09 (q, J = 6.60 Hz, 2H), 2.27 (br s, 4H), 2.22 (t, J = 6.97 Hz, 2H) 1.54 (s, 6H), 1.53-1.47 (m, 2H),	[M + H]+ = 467.1	113	0.94
A128		1-(4-hydroxybutyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 364.1	146	0.53
A129		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-(3- hydroxypyrrolidin-1- yl)propyl)urea	1H NMR (400 MHz, CDCl3) δ 7.40-7.34 (m, 2H), 7.40-7.34 (m, 2H), 7.08 (d, J = 8.78 Hz, 2H), 6.56 (br s, 1H), 5.00-4.84 (m, 1H), 4.12-4.00 (m, 1H), 3.46-3.19 (m, 3H), 3.01--2.74 (m, 3H), 2.40-2.21 (m, 1H), 2.00-1.82 (m, 2H), 1.64-1.51 (m, 6H), 1.36-1.20 (m, 2H).	[M + H]+ = 467.2	40	0.51
A130		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-(methylsulfonyl) propyl)urea	1H NMR (400 MHz, CDCl3) δ 7.38 (d, J = 8.07 Hz, 2H), 7.10 (d, J = 8.31 Hz, 2H), 6.47 (s, 1H), 3.38 (q, J = 6.11 Hz, 2H), 2.99 (br t, J = 7.58 Hz, 2H), 2.86 (s, 3H), 2.03-1.95 (m, 2H), 1.62 (s, 6H).	[M + H]+ = 462.1	293	1.10
A131		2-(3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, METHANOL-d4) δ 7.38 (d, J = 8.31 Hz, 2H), 7.16 (d, J = 8.56 Hz, 2H), 6.66 (s, 1H), 3.67 (t, J = 6.48 Hz, 2H), 3.26 (t, J = 6.36 Hz, 2H), 1.63 (s, 6H)	[M + H]+ = 447.0	219	0.94
A132		3-(3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2- yl)ureido)propane-1- sulfonamide	1H NMR (400 MHz, CDCl3) δ 7.43-7.35 (m, 2H), 7.13-7.03 (m, 2H), 6.53 (s, 1H) 5.56-5.31 (m, 1H), 3.34 (d, J = 5.77 Hz, 2H), 3.03 (s, 2H), 1.99-1.89 (m, 2H), 1.61 (s, 6H).	[M + H]+ = 463.1	80	4.56
A133		1-(3-hydroxypropyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 350.2	57	0.60
A134		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3- morpholinopropyl) urea	1H NMR (400 MHz, DMSO- d6) 6 10.46 (br s, 1H), 7.11-7.05 (m, 2H), 6.77 (d, J = 9.05 Hz, 2H), 6.59 (s, 1H), 6.32 (br s, 1H), 3.66 (s, 3H), 3.53 (br t, J = 4.52 Hz, 4H), 3.12-3.06 (m, 2H), 2.27 (br s, 4H), 2.22 (t, J = 6.97 Hz, 2H), 1.59-1.49 (m, 8H),	[M + H]+ = 419.2	152	5.11
A135		1-(3-(3- hydroxypyrrolidin-1- yl)propyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.08 (d, J = 8.8 Hz, 2H), 6.77 (d. J = 8.8 Hz, 2H), 6.69 (s, 1H), 6.60 (s, 1H), 5.40 (s, 1H), 4.34 (s, 1H), 3.66 (s, 3H), 3.11 (s, 3H), 3.03 (s, 3H), 1.77 (s, 2H), 1.53 (s, 6H), 1.35-1.15 (m, 2H), 0.95-0.85 (m, 2H).	[M + H]+ = 419.2	112	1.24
A136		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3- (methylsulfonyl) propyl)urea	1H NMR (400 MHz, MeOD) δ 7.17 (d, J = 8.8 Hz, 2H), 6.82 (d, J = 8.8 Hz, 2H), 6.43 (s, 3H), 3.78 (s, 3H), 3.42-3.38 (m, 2H), 3.00-2.97 (m, 2H), 2.86 (s, 3H), 2.05-1.98 (m, 2H), 1.64 (s, 3H)	[M + H]+ = 412.2	209	0.64
A137		2-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, MeOD) δ 7.18 (d, J = 8.8 Hz, 2H), 7.25 (d, J = 8.4 Hz, 2H), 6.61 (s, 1H), 3.77 (s, 3H), 3.72-3.66 (m, 2H), 3.30-3.25 (m, 2H), 1.65 (s, 6H).	[M + H]+ = 399.2	42	1.96
A138		3-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)propane-1- sulfonamide	1H NMR (400 MHz, MeOD) δ 7.17 (d, J = 8.8 Hz, 2H), 6.83 (d, J = 8.0 Hz, 2H), 6.63 (s, 1H), 3.77 (s, 3H), 3.39-3.35 (m, 2H), 3.15-3.02 (m, 2H), 2.12-2.00 (m, 2H), 1.65 (s, 6H).	[M + H]+ = 413.2	97	2.38
A139		1-(4-(4- hydroxypiperidin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.48 (s, 1H), 7.09 (dd, J = 12.59, 8.68 Hz, 4H), 6.87 (d, J = 8.56 Hz, 2H), 6.79 (d, J = 9.05 Hz, 2H), 6.68 (br s, 1H), 6.63 (s, 1H), 4.67 (d, J = 4.16 Hz, 1H), 4.17 (d, J = 5.87 Hz, 2H), 3.69 (s, 3H), 3.59 (td, J = 8.80, 4.40 Hz, 1H), 3.51-3.44 (m, 2H), 2.83-2.72 (m, 2H), 1.82-1.73 (m, 2H), 1.56 (s, 6H), 1.52-1.34 (m, 2H).	[M + H]+ = 481.2	261	1.35
A140		1-(4-(hydroxymethyl) benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.25-7.22 (m, 2H), 7.18-7.10 (m, 4H), 6.83-6.73 (m, 2H), 6.45 (s, 1H), 4.57 (s, 2H), 4.31-4.29 (m, 2H), 3.76 (s, 3H), 1.59 (s, 6H).	[M + H]+ = 412.2	131	5.52
A141		1-(3-(3- (dimethylamino) pyrrolidin-1- yl)propyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.43 (s, 1H) 7.08 (d, J = 8.82 Hz, 2H) 6.77 (d, J = 8.82 Hz. 2H) 6.58 (s, 1H) 6.36 (s, 1H) 3.66 (s, 3H) 3.08 (q, J = 6.39 Hz, 2H) 2.57-2.70 (m, 2H) 2.50-2.56 (m, 1H) 2.23-2.40 (m, 3H) 2.19 (t, J = 7.06 Hz, 1H) 2.05 (s, 6H) 1.73-1.84 (m, 1H) 1.44-1.60 (m, 9H)	[M + H]+ = 446.3	228	4.22
A142		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3-(4- methylpiperazin-1- yl)propyl)urea	1H NMR (400 MHz, DMSO) δ 10.49 (br, 1H), 7.14-7.12 (m, 2H), 6.83-6.80 (m, 2H), 6.63 (s, 1H), 6.34 (br, 1H), 3.73 (s, 3H), 3.14-3.09 (m, 2H), 2.53 (s, 3H), 2.40-2.29 (m, 9H), 2.21 (s, 3H), 1.57-1.52 (m, 8H)	[M + H]+ = 432.3	180	1.33
A143		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-methylurea	1H NMR (400 MHz, MeOD) δ 7.17 (d, J = 9.2 Hz, 2H), 7.25 (d. J = 8.8 Hz, 2H), 6.60 (s, 1H), 3.77 (s, 3H), 2.78 (s, 3H), 1.64 (s, 6H).	[M + H]+ = 306.2	53
A144		1-hydroxy-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 9.26-8.43 (m, 2H), 7.12-7.04 (m, 2H), 6.80-6.74 (m, 2H), 6.67 (s, 1H), 3.66 (s, 3H), 1.54 (s. 6H).	[M + H]+ = 308.1	154	1.75
A145		1-(3-(dimethylamino) propyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CD3OD) δ 7.14 (d, J = 8.82 Hz, 2H), 6.80 (d, J = 9.04 Hz, 2H), 6.59 (s, 1H), 3.74 (s, 3H), 3.22 (t, J = 6.84 Hz, 2H), 2.35-2.30 (m, 2H), 2.21 (s, 6H), 1.71-1.64 (m, 2H). 1.62 (s, 6H).	[M + H]+ = 377.2	216	4.49
A146		1-(3-(diethylamino) propyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, MeOD) δ 7.14 (d, J = 8.8 Hz, 2H), 6.80 (d, J = 8.8 Hz, 2H), 6.59 (s, 1H), 3.74 (s, 3H), 3.21 (br t, J = 6.7 Hz, 2H), 2.68-2.24 (m, 6H), 1.97-1.39 (m, 8H), 1.03 (t, J = 7.2 Hz, 6H).	[M + H]+ = 405.2	124	3.07
A147		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(4- (phenylamino)butyl) urea	1H NMR (400 MHz, MeOD) δ 7.13 (d, J = 8.82 Hz, 2H), 7.09-7.04 (m, 3H), 6.79 (d, J = 8.82 Hz, 2H), 6.62-6.55 (m, 4H), 3.72 (s, 3H), 3.25-3.19 (m, 2H), 3.06 (br t, J = 6.50 Hz, 2H), 1.61 (s, 6H), 1.59-1.54 (m, 4H)	[M + H]+ = 439.3	235	1.91
A148		3-(3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)-N- methylpropane-1- sulfonamide	1H NMR (400 MHz, CDCl3) δ 7.16-7.14 (m, 2H), 6.84-6.82 (m, 2H), 6.46 (s, 1H), 3.78 (s, 3H), 3.38-3.34 (m, 2H), 2.97-2.93 (m, 2H), 2.68-2.67 (m, 3H), 1.96-1.89 (m, 2H), 1.63 (s, 6H).	[M + H]+ = 427.0	45	0.85
A149		rac-(1s,3s)-3-((3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-N- methylcyclobutane-1- sulfonamide	1H NMR (400 MHz, CDCl3) δ 8.67 (br s, 1H), 7.13-7.11 (m, 2H), 6.82-6.80 (m, 2H), 6.41 (s, 1H), 4.85 (br s, 1H), 3.77 (s, 3H), 3.67-3.60 (m, 1H), 3.27-3.24 (m, 2H), 2.64-2.63 (m, 3H), 2.41-2.37 (m, 1H), 2.25-2.17 (m, 2H), 2.10-2.05 (m, 2H), 1.61 (s, 6H) .	[M + H]+ = 453.2	155	9.40
A150		rac-(11,3r)-3-((3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urcido)methyl)-N- methylcyclobutane-1- sulfonamide	1H NMR (400 MHz, CDCl3) δ 9.06 (br s, 1H), 7.12-7.09 (m, 2H), 6.82-6.79 (m, 2H), 6.44 (s, 1H), 4.94 (br s, 1H), 3.77 (s, 3H), 3.75-3.64 (m, 1H), 3.31-3.28 (m, 2H), 2.68-2.67 (m, 3H), 2.51-2.47 (m, 1H), 2.43-2.36 (m, 2H), 1.99-1.91 (m, 2H), 1.60 (s, 6H) .	[M + H]+ = 453.2	25	1.41
A151		1-(3,5-difluoro-4- (piperidin-4- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea hydrochloride	1H NMR (400 MHz, DMSO- d6) δ 10.72 (br, 1H), 9.10-8.70 (m, 2H), 7.09-7.07 (m, 2H), 6.95-6.93 (m, 2H), 6.78-6.76 (m, 2H), 6.62 (s, 1H), 4.22-4.20 (m, 2H), 3.66 (s, 3H), 3.30-3.25 (m, 4H), 3.20-3.14 (m, 4H), 1.53 (s, 6H).	[M + H]+ = 502.1	43	0.95
A152		1-(1-(3,5-difluoro-4- (piperazin-1- yl)phenyl)ethyl)-3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.74 (br s, 2H), 7.27 (s, 1H), 7.13-7.10 (m, 2H), 6.99-6.97 (m, 2H), 6.82-6.79 (m, 2H), 6.68 (s, 1H), 4.26-4.24 (m, 2H), 3.70 (s, 3H), 3.47-3.40 (m, 4H), 3.28-3.25 (m, 2H), 3.16-3.08 (m, 2H), 2.80-2.79 (m, 3H), 1.57 (s, 6H) .	[M + H]+ = 516.1	55	0.35
A153		N-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-hydroxyazetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.84 (br, 1H), 7.44 (d, J = 8.4 Hz, 2H), 7.34 (d, J = 8.8 Hz, 2H), 7.28 (s, 1H), 6.80 (s, 1H), 4.72-4.68 (m, 1H), 4.29-4.25 (m, 2H), 3.95-3.91 (m, 2H), 2.58 (s, 1H), 1.93 (s, 3H).	[M + H]+ = 408.0	76	0.37
A154		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3- hydroxypropyl)urea	1H NMR (400 MHz, CDCl3) δ 7.46 (d, J = 7.6 Hz, 2H), 7.37 (d, J = 8.4 Hz, 2H), 6.76 (s, 1H), 3.64 (t, J = 5.2 Hz, 2H), 3.43 (t, J = 6.0 Hz, 2H), 2.58 (s, 1H), 1.95 (s, 3H), 1.70-1.69 (m, 2H).	[M + H]+ = 408.0	21	0.38
A155		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- morpholinoethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.48-7.42 (m, 4H), 7.00 (s, 1H), 4.11-4.08 (m, 2H), 3.82-3.67 (m, 2H), 3.66-3.63 (m, 4H), 3.35 (s, 2H), 3.33-3.21 (m, 2H), 3.00 (s, 1H), 1.94 (s, 3H).	[M + H]+ = 463.1	30	0.90
A156		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2,3- dihydroxypropyl)urea	1H NMR (400 MHz, METHANOL-d4)7.44 (s, 4H), 6.91 (d, J = 1.0 Hz, 1H), 3.66-3.75 (m, 1H), 3.51 (d, J = 5.3 Hz, 2H), 3.38-3.47 (m, 1H), 3.21 (ddd, J = 13.8, 6.9, 2.6 Hz, 1H), 2.95 (s, 1H), 1.92 ppm (s, 3H)	[M + H]+ = 424.0	22	0.38
A157		1-(4-(3-(4- bromophenyl)pent-1- yn-3-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR R (400 MHz, CDCl3) δ 7.44-7.42 (m, 2H), 7.37-7.35 (m, 2H), 6.81 (s, 1H), 3.53-3.50 (m, 2H), 3.38-3.35 (m, 2H), 2.59 (s, 1H), 2.38-2.29 (m, 1H), 2.21-2.12 (m, 1H), 0.94 (t, J = 7.6 Hz, 3H)	[M + H]+ = 408.0	22	1.36
A158		1-(4-(1-(4- bromophenyl) cyclobutyl)thiazol-2- yl)-3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.50 (s, 1H), 7.47 (br d, J = 8.28 Hz, 2H), 7.19 (br d, J = 8.28 Hz, 2H), 6.66 (s, 1H), 6.47 (br s, 1H), 4.76 (br s, 1H), 3.41 (br d, J = 5.27 Hz, 2H), 3.16 (br d, J = 5.77 Hz, 2H), 2.65 (br d, J = 13.30 Hz, 2H), 2.33 (br s, 2H), 1.91-2.03 (m, 1H), 1.83 (br s, 1H)	[M + H]+ = 398	67	2.86
A159		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, CHLOROFORM-d)7.46 (d, J = 8.5 Hz, 2H), 7.36 (d, J = 8.5 Hz, 2H), 6.72 (s, 1H), 3.62 (br d, J = 4.3 Hz, 2H), 3.36 (br d, J = 3.9 Hz, 2H), 2.67 (s, 1H), 1.96 ppm (s, 3H)	[M + H]+ 94.0	48	0.49
A160		(S)-1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.41-7.39 (m, 2H), 7.31-7.29 (m, 2H), 7.24 (s, 1H), 3.45-3.43 (m, 2H), 3.32-3.29 (m, 2H), 2.52 (s, 1H), 1.89 (s, 3H).	[M + H]+ = 394.0	10	0.17
A161		(R)-1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.37-7.35 (m, 2H), 7.26-7.24 (m, 2H), 7.19 (s, 1H), 6.69 (s, 1H), 3.38-3.37 (m, 2H), 3.25-3.24 (m, 2H), 2.47 (s, 1H), 1.84 (s, 3H).	[M + H]+ = 394.0	68	0.55
A162		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO) δ 10.60 (s, 1H), 7.53-7.50 (m, 2H), 7.39-7.37 (m, 2H), 6.90 (s, 1H), 3.50 (s, 1H), 1.85 (s, 3H).	[M + H]+ = 352.0	38	0.18
A163		(S)-1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO) δ 10.61 (s, 1H), 7.53-7.51 (m, 2H), 7.39-7.34 (m, 2H), 5.76 (s, 3H), 3.50 (s, 1H), 1.85 (s, 3H).	[M + H]+ = 349.9	4	0.35
A164		(R)-1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO) δ 10.64 (s, 1H), 7.53-7.50 (m, 2H), 7.39-7.37 (m, 2H), 6.89 (s, 1H), 3.50 (s, 1H), 1.85 (s, 3H).	[M + H]+ = 350.0	17	0.59
A165		N-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(hydroxymethyl) azetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.79 (br, 1H), 7.41-7.39 (m, 2H), 7.31-7.29 (m, 2H), 7.24 (s, 1H), 6.75 (s, 1H), 4.07 (t, J = 8.0 Hz, 2H), 3.83-3.80 (m, 2H), 3.72-3.71 (m, 2H), 2.81-2.77 (m, 1H), 2.54 (s, 1H), 1.89 (s, 3H).	[M + H]+ = 420.0	138	0.73
A166		(R)-N-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(hydroxymethyl) azetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.85 (br, 1H), 7.46-7.43 (m, 2H), 7.36-7.33 (m, 2H), 6.79 (s, 1H), 4.11-4.08 (m, 2H), 3.88-3.85 (m, 2H), 3.76-3.75 (m, 2H), 2.87-2.80 (m, 1H), 2.58 (s, 1H), 1.94 (s, 3H).	[M + H]+ = 420.0	25	5.71
A167		(S)-N-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(hydroxymethyl) azetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.85 (br, 1H), 7.45-7.43 (m, 2H), 7.36-7.33 (m, 2H), 6.79 (s, 1H), 4.11-4.09 (m, 2H), 3.87-3.85 (m, 2H), 3.77-3.75 (m, 2H), 2.85-2.81 (m, 1H), 2.58 (s, 1H), 1.93 (s, 3H).	[M + H]+ = 420.0	7	0.74
A168		1-(2-hydroxyethyl)-3- (4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.38 (d, J = 8.8 Hz. 2H), 6.87-6.84 (m, 2H), 6.73 (s, 1H), 3.80 (s, 3H), 3.45 (s, 2H), 3.35-3.33 (m, 2H), 2.54 (s, 1H), 1.94 (s, 3H).	[M + H]+ = 346.1	27	0.40
A169		(R)-1-(2- hydroxyethyl)-3-(4-(2- (4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.36 (d, J = 8.8 Hz, 2H), 6.83 (d, J = 8.8 Hz, 2H), 6.70 (s, 1H), 3.78 (s, 3H), 3.46 (br d, J = 4.8 Hz, 2H), 3.32 (br d, J = 4.8 Hz, 2H), 2.52 (s, 1H), 1.92 (s, 3H)	[M + H]+ = 346	23	1.67
A170		(S)-1-(2- hydroxyethyl)-3-(4-(2- (4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.37 (d, J = 8.8 Hz, 2H), 6.84 (d, J = 8.8 Hz, 2H), 6.70 (s, 1H), 3.78 (s, 3H), 3.49 (br d, J = 5.3 Hz, 2H), 3.34 (br d, J = 5.3 Hz, 2H), 2.52 (s, 1H), 1.92 (s, 3H)	[M + H]+ = 346	8	0.46
A171		1-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.58 (s, 1H), 7.33 (d, J = 8.8 Hz, 2H), 6.86 (d, J = 8.8 Hz, 2H), 6.81 (s, 1H), 6.22 (br s, 2H), 3.72 (s, 3H), 3.40 (s, 1H), 1.83 (s, 3H)	[M + H]+ = 302	16	0.73
A172		(R)-1-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.58 (br s, 1H), 7.33 (d, J = 8.8 Hz, 2H), 6.86 (d, J = 8.8 Hz, 2H), 6.81 (s, 1H), 6.24 (br s, 1H), 3.72 (s, 3H), 3.41 (s, 1H), 1.83 (s, 3H)	[M + H]+ = 302	36	1.28
A173		(S)-1-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.60 (br s, 1H), 7.33 (d, J = 8.8 Hz, 2H), 6.86 (d, J = 8.8 Hz, 2H), 6.80 (s, 1H), 6.23 (br s, 1H), 3.72 (s, 3H), 3.40 (s, 1H), 1.83 (s, 3H)	[M + H]+ = 302	8	0.58
A174		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.64 (s, 1H), 7.33-7.46 (m, 4H), 6.90 (s, 1H), 6.34 (br s, 1H), 4.75 (t, J = 5.14 Hz, 1H), 3.50 (s, 1H), 3.41 (q, J = 5.52 Hz, 2H), 3.16 (q, J = 5.52 Hz, 2H), 1.85 (s, 3H)	[M + H]+ = 350	34	0.31
A175		(R)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.63 (br s, 1H), 7.33-7.48 (m, 4H), 6.90 (s, 1H), 6.35 (br s, 1H), 4.75 (t, J = 5.27 Hz, 1H), 3.50 (s, 1H), 3.41 (g, J = 5.35 Hz, 2H), 3.16 (q, J = 5.52 Hz, 2H), 1.85 (s, 3H)	[M + H]+ = 350	32	1.31
A176		(S)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.64 (br s, 1H), 7.34-7.49 (m, 4H), 6.90 (s, 1H), 6.35 (br s, 1H), 4.76 (t, J = 5.14 Hz, 1H), 3.51 (s, 1H), 3.42 (q, J = 5.52 Hz, 2H), 3.16 (q, J = 5.35 Hz, 2H), 1.85 (s, 3H)	[M + H]+ = 350	5.4	0.28
A177		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (2-(piperazin-1- yl)ethyl)urea		[M + H]+ = 452	249	1.66
A178		1-(4-(2-(4- iodophenyl)propan-2- yl)thiazol-2-yl)-3-((2- (piperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 564	42	0.92
A179		1-(4-(2-(4-chloro-3- fluorophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 490	95	1.36
A180		1-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)-3-((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 542	45
A181		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyridin-4- yl)methyl)urea		[M + H]+ = 515	131	1.52
A182		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((6-(piperazin-1- yl)pyridin-2- yl)methyl)urea		[M + H]+ = 515	163	4.30
A183		1-(4-((2- aminoethyl)amino) benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 440	52	2.31
A184		1-(4-(3- aminopyrrolidin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 466	242
A185		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)- N,N-dimethyl-2- (piperazin-1- yl)benzamide		[M + H]+ = 537	56
A186		1-((6-(3- aminopyrrolidin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 467	19	1.55
A187		1-((2-(3- aminopyrrolidin-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 468	7	0.7
A188		1-(4-aminobutyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiophen- 2-yl)urea		[M + H]+ = 362	59
A189		1-((6-(3- aminopyrrolidin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 515	41	2.31
A190		1-((3- aminocyclobutyl) methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 375	458	3.02
A191		1-(4-(4- aminopiperidin-1- yl)benzyl)-3-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)urea		[M + H]+ = 554	80	6.91
A192		1-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)-3-(3,5-difluoro-4- (piperazin-1- yl)benzyl)urea		[M + H]+ = 576	106	4.34
A193		1-(4-(4- aminopiperidin-1- yl)benzyl)-3-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)urea		[M + H]+ = 556	15	6.93
A194		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(3-methylpiperazin- 1-yl)benzyl)urea		[M + H]+ = 528	172	3.71
A195		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4-(3-oxopiperazin-1- yl)benzyl)urea		[M + H]+ = 528	132	9.94
A196		1-(4-(2-(4-bromo-3- fluorophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-(piperazin-1- yl)pyrimidin-5- yl)methyl)urea		[M + H]+ = 534	76	3.34
A197		1-(4-(1,4-diazepan-1- yl)-3-fluorobenzyl)-3- (4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 546	67
A198		1-(4-((2- aminoethyl)amino)-3- fluorobenzyl)-3-(4-(2- (4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 506	18	1.32
A199		1-((6-(3- aminopyrrolidin-1- yl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 467	34	0.46
A200		1-((5-(3- aminopyrrolidin-1- yl)pyridin-2- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 467	43	0.52
A201		1-(4-(3- aminopyrrolidin-1-yl)- 3,5-difluorobenzyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 502	25	0.53
A202		1-((6-((2- aminoethyl)amino) pyridin-3-yl)methyl)- 3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 441	34	5.71
A203		N-(2-aminoethyl)-5- ((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido) methyl)picolinamide		[M + H]+ = 469	94	5.70
A204		1-(4-(4- aminopiperidin-1- yl)benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 528	9	1.89
A205		1-(4-((2- aminoethyl)amino) benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 488	59	1.48
A206		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((2-((2-(piperazin-1- yl)ethyl)amino) pyrimidin-5- yl)methyl)urea		[M + H]+ = 559	68
A207		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ((3-fluoro-2- (piperazin-1- yl)pyridin-4- yl)methyl)urea		[M + H]+ = 533	99	2.18
A208		1-((2-(4-(2- hydroxyethyl) piperazin-1- yl)pyrimidin-5- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 512	78	0.76
A209		5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl)-2- (piperazin-1- yl)nicotinamide		[M + H]+ = 510	43
A210		1-(2-aminoethyl)-3-(4- (2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 383	95	4.16
A211		1-(4-(4-(aminomethyl) piperidin-1- yl)benzyl)-3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 542	94	2.59
A212		1-(4-(2- aminoethoxy)benzyl)- 3-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)urea		[M + H]+ = 489	289	2.75
A213		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (4- (3,5- dimethylpiperazin-1- yl)benzyl)urea		[M + H]+ = 542	9	6.38
A214		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-fluoro-4-(piperazin- 1- ylmethyl)benzyl)urea		[M + H]+ = 546	40	1.56
A215		1-(5-((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl) pyrimidin-2- yl)piperidine-4- carboxamide		[M + H]+ = 510	150	2.21
A216		1-((5-fluoro-6-(4-(2- hydroxyethyl) piperazin-1- yl)pyridin-3-yl) methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 529	61	1.43
A217		1-((6-(3- aminopyrrolidine-1- carbonyl)pyridin-3- yl)methyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 495	56	32.58
A218		N-(2-aminoethyl)-4- ((3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)ureido)methyl) benzamide		[M + H]+ = 468	29	6.71
A219		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-chloro-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.76 (br s, 1H), 9.25 (br s, 2H), 7.43 (d, J = 8.56 Hz, 2H), 7.34 (d, J = 1.96 Hz, 1H), 7.24-7.20 (m, 1H), 7.15 (d, J = 8.56 Hz, 4H), 6.74 (s, 1H), 4.25 (br d, J = 5.62 Hz, 2H), 3.27-3.08 (m, 8H), 1.57 (s, 6H)	[M + H]+ = 550.0	46	2.73
A220		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-methoxy-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.67 (br s, 1H) 9.14 (br s, 2H), 7.43 (d, J = 8.56 Hz, 2H), 7.15 (d, J = 8.56 Hz, 2H), 7.12 (br s, 1H), 6.93-6.88 (m, 2H), 6.80 (br d, J = 8.07 Hz, 1H), 6.74 (s, 1H), 4.25 (br d, J = 5.38 Hz, 2H), 3.77 (s, 3H), 3.18 (br d, J = 14.18 Hz, 8H), 1.57 (s, 6H).	[M + H]+ = 544.2	44	1.32
A221		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-isopropoxy-4- (piperazin-1- yl)benzyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.79 (br s, 1H), 9.48 (br s, 2H), 7.49 (br d, J = 8.80 Hz, 1H), 7.43 (d, J = 8.56 Hz, 2H), 7.15 (d, J = 8.56 Hz, 2H), 7.03 (br d, J = 8.07 Hz, 1H), 6.94 (s, 1H), 6.81 (br d, J = 7.83 Hz, 1H), 6.77 (s, 1H), 6.01 (br s, 8H), 4.61 (dt, J = 11.98, 5.99 Hz, 1H), 4.24 (br d, J = 4.40 Hz, 2H), 1.58 (s, 6H), 1.28 (d, J = 6.11 Hz, 6H).	[M + H]+ = 574.1	144	2.38
A222		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- (3-fluoro-4-(piperidin- 4-yl)benzyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.76 (br s, 1H), 9.06 (br s, 1H), 8.88 (br d, J = 9.78 Hz, 1H), 7.43 (d, J = 8.56 Hz, 2H), 7.29-7.19 (m, 2H), 7.15 (d, J = 8.56 Hz, 2H), 7.10-7.04 (m, 2H), 6.74 (s, 1H), 4.28 (br d, J = 5.62 Hz, 2H),3.33 (br d, J = 12.47 Hz, 2H), 3.14-2.93 (m, 2H), 1.93-1.81 (m, 3H), 1.57 (s, 6H), 1.23 (br s, 2H).	[M + H]+ = 532.2	56	0.93
A223		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-((4-methyl-2- (piperazin-1- yl)pyrimidin-5- yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 9.50 (br s, 2H), 8.23 (s, 1H), 7.76-7.57 (m, 1H), 7.17-7.06 (m, 2H), 6.86-6.79 (m, 2H), 6.72 (s, 1H), 4.26-4.18 (m, 2H), 4.0-3.92 (m, 4H), 3.70 (s, 3H), 3.13 (s, 4H), 2.40 (s, 3H), 1.57 (s, 6H).	[M + H]+ = 482.4	49	0.76
A224		1-(3-fluoro-4- (piperidin-4- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.73 (br s, 1H), 8.93 (br s, 1H), 8.72 (br s, 1H), 7.26-7.20 (m, 1H), 7.16-7.02 (m, 5H), 6.81 (d, J = 8.80 Hz, 2H), 6.66 (s, 1H), 4.29 (br d, J = 5.87 Hz, 2H), 3.70 (s, 3H), 3.34 (br d, J = 12.23 Hz, 2H), 3.15-3.07 (m, 1H), 3.07-2.94 (m, 2H), 1.87 (br s, 4H), 1.57 (s, 6H).	[M + H]+ = 483.2	21	0.73
A225		1-(3-isopropoxy-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, CD3OD) δ 7.23-7.16 (m, 3H), 7.11 (s, 1H), 7.07 (s, 1H), 6.97-6.87 (m, 3H), 4.75 (dt, J = 11.49, 5.75 Hz, 1H), 4.40 (s, 2H), 3.76 (s, 3H), 3.51 (s, 8H), 1.69 (s, 6H), 1.38 (d, J = 5.87 Hz. 6H).	[M + H]+ = 524.3	108	1.05
A226		1-(3-(3- aminopyrrolidin-1- yl)propyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 11.30 (s, 1H) 10.94 (s, 1H) 8.64 (s, 1H) 8.55 (s, 1H) 7.09 (d, J = 8.82 Hz, 2H) 6.95 (s, 1H) 6.78 (d, J = 8.82 Hz, 2H) 6.64 (s, 1H) 4.00 (d, J = 13.89 Hz, 1H) 3.67 (s, 3H) 3.37-3.49 (m, 1H) 3.35 (s,2H) 3.01-3.23 (m, 5H) 2.06-2.28 (m, 1H) 1.92-2.06 (m, 1H) 1.75-1.86 (m, 2H) 1.54 (s, 6H)	[M + H]+ = 418.3	100	4.82
A227		1-(2-(3- aminopyrrolidin-1- yl)ethyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, D2O) δ 7.20-7.13 (m, 2H), 6.95 (s, 1H), 6.89-6.83 (m, 2H), 4.20-3.74 (m, 3H), 3.71 (s, 3H), 3.68-3.47 (m, 4H), 3.46-3.32 (m, 2H), 2.65-2.48 (m, 1H), 2.24-2.07 (m, 1H), 1.56 (s, 6H).	[M + H]+ = 404.3	138	3.12
A228		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3-(3- methylpiperazin-1- yl)propyl)urea	1H NMR (400 MHz, DMSO- d6) δ 11.79 (br s, 1H), 10.68 (br s, 1H), 9.97 (br s, 2H), 7.12 (d, J = 8.6 Hz, 2H), 6.88 (s, 1H), 6.81 (d, J = 8.8 Hz, 2H), 6.67 (s, 1H), 3.75-3.62 (m, 6H), 3.58-3.49 (m, 1H), 3.48-3.36 (m, 1H), 3.29-3.16 (m, 3H), 3.15-2.99 (m, 3H), 1.96-1.82 (m, 2H), 1.57 (s, 6H), 1.30 (d. J = 6.4 Hz, 2H).	[M + H]+ = 432.3	100	3.86
A229		1-(3-((3- aminopyrrolidin-1- yl)sulfonyl)propyl)-3- (4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 8.47 (br s, 3H), 7.24 (br s, 1H), 7.12 (d, J = 8.82 Hz, 2H), 6.82 (d, J = 8.60 Hz, 2H), 6.70 (s, 1H), 3.83 (br d, J = 5.07 Hz, 1H), 3.70 (s, 3H), 3.58 (br dd, J = 10.80, 6.62 Hz, 1H), 3.52-3.43 (m, 1H), 3.41-3.28 (m, 3H), 3.26-3.13 (m, 4H), 2.22 (dq, J = 13.70, 6.90 Hz, 1H), 2.05-1.92 (m, 1H), 1.84 (dt, J = 14.55, 7.06 Hz, 2H), 1.57 (s, 6H).	[M + H]+ = 482.2	169	2.27
A230		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(3-(piperazin-1- ylsulfonyl)propyl)urea	1H NMR (400 MHz, DMSO- d6) δ 7.10-7.07 (m, 2H), 6.78-6.75 (m, 2H), 6.59 (s, 1H), 3.67 (s, 3H), 3.30-3.15 (m, 2H), 3.02-2.95 (m, 6H), 2.68-2.66 (m, 4H), 1.79-1.72 (m, 2H), 1.52 (s, 6H).	[M + H]+ = 482.2	127	3.01
A231		1-(2,5-difluoro-4- (piperazin-1- yl)benzyl)-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea hydrochloride	1H NMR (400 MHz, DMSO- d6) δ 10.75 (br s, 1H), 9.33 (br s, 2H), 7.39 (br s, 1H), 7.16-7.10 (m, 3H), 6.98 (dd, J = 11.36, 7.39 Hz, 1H), 6.80 (d, J = 8.82 Hz, 2H), 6.68 (s, 1H), 4.27 (br d, J = 5.51 Hz, 2H), 3.70 (s, 3H), 3.23 (br s, 8H), 1.57 (s, 6H),	[M + H]+ = 502.2	27	3.36
A232		1-(4-(3,6- diazabicyclo[3.1.1] heptan-3-yl)-3,5- difluorobenzyl)-3-(4- (2-(4-methoxyphenyl) propan-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.85-10.72 (m, 1H), 9.80-9.68 (m, 1H), 8.16-8.08 (m, 1H), 7.12 (br d, J = 8.8 Hz, 2H), 7.05-6.93 (m, 2H), 6.86-6.76 (m, 2H), 6.71-6.64 (m, 1H), 4.27 (br d, J = 6.1 Hz, 4H), 3.88 (s, 2H), 3.70 (s, 3H), 3.54-3.49 (m, 2H), 2.86-2.76 (m, 1H), 2.14-2.06 (m, 1H), 1.57 (s, 6H).	[M + H]+ = 514.3	88	0.59
A233		N-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(4-(piperazin-1- yl)phenyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 9.25 (br s, 2H), 7.33 (s, 0.4H), 7.25-7.23 (m, 2H), 7.20-7.18 (m, 2H), 7.14-7.12 (m, 0.4H), 6.98-6.96 (m, 2H),6.82-6.80 (m, 2H), 6.66 (s, 1H), 4.38-4.36 (m, 2H), 3.94-3.91 (m, 2H), 3.76-3.72 (m, 1H), 3.72 (s, 3H), 3.39-3.38 (m, 4H), 3.37-3.20 (m, 4H), 1.60 (s, 6H).	[M + H]+ = 492.2	43	0.33
A234		1-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(4-(piperazin-1- yl)phenyl)ethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.50 (br s, 1H), 9.22 (br s, 2H), 7.31 (d, J = 8.8 Hz, 2H), 7.19 (d, J = 8.4 Hz, 3H), 6.95 (d, J = 8.4 Hz, 2H), 6.85 (dd, J = 8.4, 1.2 Hz, 2H), 6.81-6.79 (m, 1H), 4.76-4.73 (m, 1H), 3.71 (s, 3H), 3.39 (s, 1H), 3.35-3.32 (m, 4H) 3.24-3.16 (m, 4H), 1.82 (d, J = 2.4 Hz, 3H), 1.33 (d, J = 6.8 Hz, 3H)	[M + Na]+ = 512.3	36	2.67
A235		1-(4-(1-hydroxy-2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(1-(4-(piperazin- 1-yl)phenyl)ethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.47 (br s, 1H), 9.11 (br s, 2H), 7.36-7.23 (m, 1H), 7.19 (d, J = 8.8 Hz, 2H), 7.10 (d, J = 8.8 Hz, 2H), 6.95 (d, J = 8.8 Hz, 2H), 6.75 (d, J = 8.0 Hz, 2H), 6.69 (s, 1H), 4.77-4.73 (m, 1H), 3.80-3.76 (m, 1H), 3.70 (s, 3H) 3.34-3.31 (m, 4H), 3.24-3.16 (m, 4H), 2.07 (s, 1H), 1.55 (s, 3H), 1.33 (d, J = 6.8 Hz, 3H)	[M + H]+ = 496.2	61	27.01
A236		N-(4-(1-(4- bromophenyl) cyclopentyl)thiazol-2- yl)-3-(3-fluoro-4- (piperazin-1- yl)phenyl)azetidine-1- carboxamide	1H NMR (400 MHz, MeOD) δ 7.34 (d, J = 8.56 Hz, 2H) 7.21 (d, J = 8.56 Hz, 2H) 7.08-7.00 (m, 3H) 6.68 (s, 1H) 4.59 (br d, J = 16.63 Hz, 1H) 4.40 (t, J = 8.56 Hz, 2H) 3.98 (dd, J = 8.31, 6.11 Hz, 2H) 3.77-3.87 (m, 1H) 3.02 (br d, J = 6.11 Hz, 8H) 2.43-2.53 (m, 2H) 2.01-2.13 (m, 2H) 1.62-1.77 (m, 4H)	[M + H]+ = 584.3	13	4.50
A237		N-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(4-(piperazin-1- yl)phenyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.93 (s, 1H) 9.22 (s, 2H) 7.47 (d, J = 8.4 Hz, 2H) 7.30 (d, J = 8.4 Hz, 2H) 7.21 (d, J = 8.4 Hz, 2H), 6.90-6.98 (m, 3H), 4.30 (br s, 1H), 3.87-3.84 (m, 2H), 3.66-3.74 (m, 1H), 3.46 (s, 1H), 3.31-3.30 (m, 4H), 3.22-3.10 (m, 4H), 1.82 (s, 3H)	[M + H]+ = 550.1	7	0.61
A238		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((4- hydroxypiperidin-4- yl)methyl)urea	1H NMR (400 MHz, MeOD) δ 7.53-7.20 (m, 2H), 7.44-7.42 (m, 2H), 7.14 (s, 1H), 3.33-3.27 (m, 2H), 3.26-3.25 (m, 4H), 3.16 (s, 1H), 1.95 (s, 3H), 1.79-1.77 (m, 4H)	[M + H]+ = 465.1	19	27.00
A239		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2-(piperazin-1- yl)ethyl)urea	1H NMR (400 MHz,METHANOL-d4) 7.47-7.54 (m, 2H), 7.38-7.46 (m, 2H), 7.14 (s, 1H), 3.62-3.82 (m, 8H), 3.47 (br t, J = 5.6 Hz, 2H), 3.14 (s, 1H), 1.95 ppm (s, 3H)	[M + H]+ = 462.0	20	0.85
A240		1-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)-3-(1-(4-(piperazin- 1-yl)phenyl) cyclopropyl)urea		[M + H]+ = 492	97	1.88
A241		1-(4-(2-(4- bromophenyl)propan- 2-yl)thiazol-2-yl)-3- ethylurea		[M + H]+ = 368.1	98	3.41
A242		1-ethyl-3-(4-(2-(4- methoxyphenyl) propan-2-yl)thiazol-2- yl)urea		[M + H]+ = 320	42	0.98
A243		2-(3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)ureido)ethane-1- sulfonamide	1H NMR (400 MHz, CDCl3) δ 7.44-7.26 (m, 4H), 6.75 (s, 2H), 5.82 (s, 2H), 3.80-3.65 (m, 2H), 3.25-3.13 (m, 2H), 2.63 (s, 1H), 1.92 (s, 3H). MS (ESI) m/z (M+H)+ = 413.0	[M + H]+ = 413.1	23	0.59
A244		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2,3- dihydroxypropyl)urea	1H NMR (400 MHz, CDCl3) δ 9.63 (br. s, 1H), 7.39-7.35 (m, 2H), 7.25-7.19 (m, 2H), 6.65 (s, 2H), 3.72-3.62 (m, 1H), 3.52-3.33 (m, 2H), 3.29-3.09 (m, 2H), 2.56 (s, 1H), 1.86 (s, 3H). MS (ESI) m/z (M + H)+ = 380.0	[M + H]+ = 380.1	72	1.03
A245		(S)-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3-fluoro-4- (piperazin-1- yl)phenyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.95 (s, 1H), 8.97 (br s, 2H), 7.35-7.42 (m, 4H), 7.20-7.30 (m, 1H), 7.11-7.18 (m, 1H), 7.04-7.09 (m, 1H), 6.97 (s, 1H), 4.33 (br t, J = 8.11 Hz, 2H), 3.91 (br t, J = 7.03 Hz, 2H), 3.75-3.81 (m, 1H), 3.48 (s, 1H), 3.21 (br d, J = 8.94 Hz, 8H), 1.85 (s, 3H)	[M + H]+ = 524.1	16	0.68
A246		(R)-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3-fluoro-4- (piperazin-1- yl)phenyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.95 (s, 1H), 8.95 (br s, 2H), 7.35-7.42 (m, 4H), 7.18-7.30 (m, 1H), 7.10-7.17 (m, 1H), 7.02-7.09 (m, 1H), 6.97 (s, 1H), 4.33 (br t. J = 8.17 Hz, 2H), 3.86-3.97 (m, 2H), 3.75-3.81 (m, 1H), 3.48 (s, 1H), 3.23 (br s, 4H), 3.20 (br s, 4H), 1.86 (s, 3H)	[M + H]+ = 524.1	29	1.59
A247		(S)-1-(5-chloro-4-(2- (4-chlorophenyl)but- 3-yn-2-yl)thiazol-2- yl)-3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.92(1, 1H), 7.38-7.36 (m, 4H), 6.49 (s, 1H), 4.80 (s, 1H), 3.58 (s, 1H), 3.45-3.35 (m, 2H), 3.22-3.18 (m, 2H), 1.85 (s, 3H)	[M + H]+ = 429.7	408	1.85
A248		(R)-1-(5-chloro-4-(2- (4-chlorophenyl)but- 3-yn-2-yl)thiazol-2- yl)-3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.92(1, 1H), 7.40-7.30 (m, 4H), 6.50 (s, 1H), 4.77 (s, 1H), 3.55 (s, 1H), 3.43-3.35 (m, 2H), 3.20-3.15 (m, 2H), 1.87 (s, 3H)	[M + H]+ = 429.9	1294	2.73
A249		(S)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3-hydroxy-3- methylbutyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.66 (s, 1H), 7.40-7.46 (m, 2H), 7.33-7.39 (m, 2H), 6.88 (s, 1H), 6.27 (s, 1H), 4.32 (s, 1H), 3.48 (s, 1H), 3.13-3.23 (m, 2H), 1.85 (s, 3H), 1.45-1.57 (m, 2H), 1.09 ppm (s, 6H)	[M + H]+ = 392.0	128	0.67
A250		(R)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3-hydroxy-3- methylbutyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.65 (s, 1H), 7.41-7.46 (m, 2H), 7.34-7.40 (m, 2H), 6.88 (s, 1H), 6.26 (s, 1H), 4.31 (s, 1H), 3.49 (s, 1H), 3.13-3.22 (m, 2H), 1.85 (s, 3H), 1.46-1.56 (m, 2H), 1.09 ppm (s, 6H)	[M + H]+ = 392.0	417	1.18
A251		(R)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.59(1, 1H), 7.44-7.42 (m, 2H), 7.38-7.36 (m, 2H), 6.89 (s, 1H), 6.22 (s, 1H), 3.49 (s, 1H), 1.85 (s, 3H)	[M + H]+ = 305.9	81	1.67
A252		(S)-1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.60(1, 1H), 7.44-7.42 (m, 2H), 7.39-7.36 (m, 2H), 6.90 (s, 1H), 6.22 (s, 1H), 3.49 (s, 1H), 1.85 (s, 3H)	[M + H]+ = 305.9	30	0.53
A253		3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 1,1-bis(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) d: 7.36 (4H, J = 19.6 Hz, t), 6.91 (1H, s), 3.51 (4H, s), 3.45 (1H, s), 3.40 (4H, s), 1.83 (3H, s)	[M + H]+ = 394.0	172	3.05
A254		3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 1-(2-hydroxyethyl)-1- methylurea	1H NMR (400 MHz, DMSO- d6) d: 7.38-7.33 (4H, m), 6.90 (1H, s), 3.47 (2H, J = 10.4 Hz, t), 3.44 (1H, s), 3.37 (2H, J = 10.4 Hz, t), 2.91 (3H, s), 1.82 (3H, s)	[M + H]+ = 364.0	548	2.07
A255		(R)-3- (hydroxymethyl)-N- (4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.83 (s, 1H), 7.29 (d, J = 8.78 Hz, 2H), 6.87 (s, 1H), 6.85 (s, 2H), 4.78 (t, J = 5.27 Hz, 1H), 3.94 (br s, 2H), 3.71 (s, 3H), 3.68 (br s, 2H), 3.48 (t, J = 5.65 Hz, 2H), 3.38 (s, 1H), 2.56-2.70 (m, 1H), 1.83 (s, 3H).	[M + H]+ = 372.0	109
A256		(S)-3- (hydroxymethyl)-N- (4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.85 (s, 1H), 7.30 (br d, J = 8.78 Hz, 2H), 6.87 (s, 1H), 6.86 (s, 2H), 4.79 (t, J = 5.14 Hz, 1H), 3.86-4.07 (m, 2H), 3.72 (s, 3H), 3.69 (br s, 2H), 3.49 (br t, J = 5.52 Hz, 2H), 3.39 (s, 1H), 2.56-2.72 (m, 1H), 1.84 (s, 3H).	[M + H]+ = 372.1	43
A257		(R)-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(hydroxymethyl) azetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.79 (s, 1H), 7.45-7.40 (m, 2H), 7.30-7.20 (m, 2H), 6.78 (s, 1H), 4.20-4.08 (m, 2H), 3.90-3.84 (m, 2H), 3.80-3.75 (m, 2H), 2.88-2.75 (m, 1H), 2.57 (s, 1H), 2.10-2.00 (m, 1H), 1.92 (s, 3H).	[M + H]+ = 376.1	246
A258		(S)-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl) thiazol-2-yl)- 3-(hydroxymethyl) azetidine-1- carboxamide	1H NMR (400 MHz, CDCl3) δ 7.78 (s, 1H), 7.45-7.36 (m, 2H), 7.30-7.20 (m, 2H), 6.78 (s, 1H), 4.20-4.08 (m, 2H), 3.90-3.84 (m, 2H), 3.80-3.75 (m, 2H), 2.90-2.80 (m, 1H), 2.57 (s, 1H), 2.05-1.95 (m, 1H), 1.93 (s, 3H).	[M + H]+ = 376.1	57
A259		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- ylmethyl)azetidine-1- carboxamide		444.2	48	0.44
A260		(S)-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 6-(piperazin-1-yl)-3,4- dihydroisoquinoline- 2(1H)-carboxamide	1H NMR (400 MHz, DMSO- d6) δ 8.23 (s, 1H), 7.41-7.35 (m, 4H), 6.99-6.91 (m, 2H), 6.75 (d, J = 7.7 Hz, 1H), 6.67 (s, 1H), 4.47 (s, 2H), 3.63 (s, 2H), 3.05 (s, 4H), 2.90 (s, 4H), 2.70 (s, 2H), 1.81 (s, 3H).	506.2	74	1.08
A261		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- yl)azetidine-1- carboxamide		430.1	83	0.51
A262		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(3-fluoro-4- (piperazin-1- yl)benzyl)urea		498.1	13	0.67
A263		3-((4-aminopiperidin- 1-yl)methyl)-N-(4-(2- (4-chlorophenyl)but- 3-yn-2-yl)thiazol-2- yl)azetidine-1- carboxamide		458.1	39	1.44
A264		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 4-(hydroxymethyl) piperidine-1- carboxamide		404.1	1374	2.81
A265		4-amino-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)piperidine-1- carboxamide		389.1	4974	2.90
A266		3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 1-(2-hydroxyethyl)-1- metbylurea	1H NMR (400 MHz, DMSO- d6) δ 7.34 (t, J = 20.0 Hz, 4H), 6.87 (s, 1H), 3.44-3.40 (m, J = 16.0, 5H), 2.88 (s, 3H), 1.79 (s, 3H).	364.0	546	2.07
A267		3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 1,1-bis(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 7.34 (t, J = 20.0 Hz, 4H), 6.86 (s, 1H), 3.46-3.40 (m, J = 16.0, 9H), 1.78 (s, 3H).	394.0	171	3.05
A268		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2-hydroxy-2- methylpropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 7.43-7.34 (dd, J = 27.8, 7.5 Hz, 4H), 6.87 (s, 1H), 6.38 (s, 1H), 4.56 (s, 1H), 3.02 (d, J = 4.0 Hz, 2H), 1.83 (s, 3H), 1.03 (s, 6H)	378.1	218	1.31
A269		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-hydroxypyrrolidine- 1-carboxamide	1H NMR (400 MHz, DMSO- d6) δ 7.36 (s, 4H), 6.90 (s, 1H), 4.93 (s, 1H), 4.22 (s, 1H), 3.44 (s, 4H), 1.83 (s, 3H), 1.74 (s, 2H).	376.0	881	1.26
A270		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(hydroxymethyl) pyrrolidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 7.36 (s, 4H), 6.90 (s, 1H), 4.68 (s, 1H), 3.44 (s, 4H), 3.11 (s, 2H), 2.24 (s, 1H), 1.83 (s, 3H), 1.60 (s, 2H).	390.1	904	1.97
A271		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-hydroxyurea	1H NMR (400 MHz, DMSO- d6) δ 7.40-7.36 (m, J = 16.0 Hz, 4H), 6.94 (s, 1H), 3.47 (s, 1H), 1.84 (s, 3H).	322.0	493	0.73
A272		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(4-(piperazin-1- yl)phenethyl)urea		494.1	135	0.89
A273		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 2-(4-(piperazin-1- yl)phenyl)acetamide	1H NMR (400 MHz, DMSO- d6) δ 7.31 (s, 4H), 7.13-7.09 (m, 4H), 6.83 (d, J = 8.0 Hz, 1H), 3.54 (s, , 2H), 3.50 (m, 4H), 2.78 (s, 4H), 1.84 (s, 3H).	465.1	60	2.68
A274		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(piperidin-4- yl)ethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 7.41-7.34 (m, 4H), 6.86 (s, 1H), 3.16 (s, 4H), 2.67 (s, 1H), 1.82 (s, 3H), 1.66 (s, 2H), 1.49 (s, 1H), 1.25 (s, 2H), 1.01 (s, 3H).	417.1	467	2.55
A275		3-amino-N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)azetidine-1- carboxamide		361.0	503	1.59
A276		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)guanidine		305.0	475	1.58
A272				[M + H]+ = 331.0	666	NA
A273		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(4-(piperazin-1- yl)phenyl) cyclopropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.77-11.73 (m, 1H), 8.01 (br s, 1H), 7.39-7.44 (m, 2H), 7.34-7.39 (m, 2H), 7.02 (d, J = 8.70 Hz, 2H), 6.86 (s, 1H), 6.80 (br d, J = 8.82 Hz, 2H), 3.48 (s, 1H), 2.92-2.99 (m, 4H), 2.75-2.83 (m, 4H), 1.84 (s, 3H), 1.06 (br d, J = 9.06 Hz, 4H).	506.1	237	3.20
A274		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(4-(piperazin-1- yl)phenyl) cyclopropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.50 (br s, 1H), 7.40-7.47 (m, 2H), 7.34-7.40 (m, 2H), 7.02 (br d, J = 8.70 Hz, 3H), 6.91 (s, 1H), 6.82 (br d, J = 8.82 Hz, 2H), 3.50 (s, 1H), 2.92-3.04 (m, 4H), 2.75- 2.88 (m, 4H), 1.84 (s, 3H), 1.09 (br d, J = 3.58 Hz, 4H).	506.1	327	3.8
A275		N-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- ylmethyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 12.00 (br s, 1H), 11.01 (br s, 1H), 9.79 (br s, 2H), 7.40 (dd, J = 8.66, 5.40 Hz, 2H), 7.13 (t, J = 8.66 Hz, 2H), 6.93 (s, 1H), 4.09 (br s, 2H), 3.76-3.85 (m, 2H), 3.57 (br d, J = 4.77 Hz, 2H), 3.39-3.53 (m, 7H), 3.26 (br s, 2H), 3.11 (br d, J = 6.53 Hz, 1H), 1.85 (s, 3H).	428.0	246	3.38
A276		N-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- ylmethyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 12.01 (br s, 1H), 11.01 (br s, 1H), 9.79 (br s, 2H), 7.40 (dd, J = 8.41, 5.40 Hz, 2H), 7.13 (t, J = 8.78 Hz, 2H), 6.93 (s, 1H), 4.01-4.12 (m, 2H), 3.75-3.85 (m, 2H), 3.58 (br s, 2H), 3.37-3.52 (m, 7H), 3.27 (br s, 2H), 3.10 (br s, 1H), 1.85 (s, 3H).	428.1	345	0.56
A277		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.60 (br s, 1H), 7.51 (d, J = 8.53 Hz, 2H), 7.37 (d, J = 8.53 Hz, 2H), 6.90 (s, 1H), 6.33 (br s, 1H), 4.86 (br d, J = 4.77 Hz, 1H), 4.59 (t, J = 5.65 Hz, 1H), 3.50 (s, 1H), 3.42-3.49 (m, 1H), 3.34-3.37 (m, 0.5H), 3.20-3.31 (m, 2.5H), 2.90-3.04 (m, 1H), 1.85 (s, 3H).	424.0	2667	1.23
A278		1-(4-(2-(4- bromophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.62 (br s, 1H), 7.51 (d, J = 8.53 Hz, 2H), 7.37 (d, J = 8.53 Hz, 2H), 6.89 (s, 1H), 6.34 (br s, 1H), 4.86 (br d, J = 4.52 Hz, 1H), 4.60 (t, J = 5.40 Hz, 1H), 3.50 (s, 1H), 3.47 (br d, J = 4.77 Hz, 1H), 3.35 (br s, 0.5H), 3.20-3.31 (m, 2.5H), 2.90-3.03 (m, 1H), 1.84 (s, 3H).	424.0	624	0.52
A279		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)-5- fluorothiazol-2-yl)-3- (2-hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.65 (s, 1H), 7.50-7.35 (m, 4H), 6.34 (br. s, 1H), 4.76 (t, J = 4.0 Hz, 1H), 3.53 (s, 1H), 3.41 (q, J = 4.0 Hz, 1H), 3.15 (q, J = 4.0 Hz, 1H), 1.86 (s, 3H).	368.0	222	4.23
A280		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 6-(piperazin-1-yl)-3,4- dihydroisoquinoline- 2(1H)-carboxamide	1H NMR (400 MHz, DMSO- d6) δ 7.44-7.35 (m, 4H), 7.01-6.94 (m, 2H), 6.81-6.75 (m, 1H), 6.72-6.68 (m, 1H), 4.53 (s, 2H), 3.66 (t, J = 8 Hz, 2H ), 3.50 (s, 1H), 3.05-2.99 (m, 4H), 2.88-2.82 (m, 4H), 2.75 (t, J = 8 Hz, 2H ), 1.87 (s, 3H).	506.5	21	2.18
A281		N-(4-(2-(4- chlorophenyl)but-3- yn-chlorophenyl)but2- yl)thiazol-2-yl)-6- (piperazin-1-yl)-3,4- dihydroisoquinoline- 2(1H)-carboxamide	1H NMR (400 MHz, DMSO- d6) δ 7.44-7.36 (m, 4H), 7.01-6.94 (m, 2H), 6.80-6.75 (m, 1H), 6.71-6.68 (m, 1H), 4.53 (s, 2H), 3.66 (t, J = 8 Hz, 2H ), 3.50 (s, 1H), 3.04-2.98 (m, 4H), 2.86-2.80 (m, 4H), 2.75 (t, J = 8 Hz, 2H ), 1.87 (s, 3H).	506.5	38	0.86
A282		1-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6 δ 10.63 (s, 1H), 7.44 (dd, J = 8.78, 5.52 Hz, 2H), 7.13 (t, J = 8.91 Hz, 2H), 6.87 (s, 1H), 6.34 (br s, 1H), 4.75 (t, J = 5.02 Hz, 1H), 3.48 (s, 1H), 3.41 (q, J = 5.52 Hz, 2H), 3.16 (q, J = 5.60 Hz, 2H), 1.85 (s, 3H).	334.1	2153	7.72
A283		1-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.63 (s, 1H), 7.44 (dd, J = 8.78, 5.52 Hz, 2H), 7.13 (t, J = 8.91 Hz, 2H), 6.88 (s, 1H), 6.33 (br s, 1H), 4.75 (t, J = 5.14 Hz, 1H), 3.48 (s, 1H), 3.41 (q, J = 5.35 Hz, 2H), 3.16 (q, J = 5.52 Hz, 2H), 1.85 (s, 3H).	334.1	550	1.70
A284		2-(3-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, DMSO- d6) δ 10.94 (br s, 1H), 7.44 (dd, J = 8.78, 5.52 Hz, 2H), 7.13 (t, J = 8.91 Hz, 2H), 6.92 (s, 2H), 6.90 (s, 1H), 6.48 (br t, J = 5.65 Hz, 1H), 3.49-3.56 (m, 2H), 3.48 (s, 1H), 3.13 (t, J = 6.65 Hz, 2H), 1.85 (s, 3H).	397.0	666	2.60
A285		2-(3-(4-(2-(4- fluorophenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, DMSO- d6) δ 10.95 (br s, 1H), 7.37-7.50 (m, 2H), 7.13 (t, J = 8.78 Hz, 2H), 6.92 (s, 2H), 6.90 (s, 1H), 6.48 (br t, J = 5.90 Hz, 1H), 3.49-3.56 (m, 2H), 3.48 (s, 1H), 3.14 (t, J = 6.65 Hz, 2H), 1.85 (s, 3H).	397.1	350	1.36
A286		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((3-hydroxyazetidin- 3-yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.75 (br s, 1H), 9.17 (br s, 1H), 8.99 (br s, 1H), 7.46-7.41 (m, 2H), 7.40-7.36 (m, 2H), 6.93 (s, 1H), 6.82 (br s, 1H), 3.75-3.90 (m, 5H), 3.52 (s, 1H), 3.43 (d, J = 6.0 Hz, 2H), 1.85 (s, 3H)	391.1	495	15.40
A287		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((3-hydroxyazetidin- 3-yl)methyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.75 (br s, 1H), 9.10 (br s, 1H), 8.95 (br s, 1H), 7.45-7.41 (m, 2H), 7.40-7.35 (m, 2H), 6.93 (s, 1H), 6.77 (br s, 1H), 3.86 (br s, 5H), 3.51 (s, 1H) 3.43 (br d, J = 6.0 Hz, 2H), 1.85 (s, 3H)	391.1	130	4.40
A288		2-(3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, CDCl3) δ 9.48 (br s, 1H), 7.30 (s, 4H), 6.76 (s, 1H), 6.05 (br s, 3H), 3.75-3.65 (m, 2H), 3.09-2.99 (m, 2H), 2.53 (s, 1H), 1.87 (s, 3H)	413.1	270	1.21
A289		2-(3-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, CDCl3) δ 9.48 (br s, 1H), 7.30 (s, 4H), 6.76 (s, 1H), 6.06 (br s, 3H), 3.75-3.65 (m, 2H), 3.10-2.98 (m, 2H), 2.53 (s, 1H) 1.87 (s, 3H)	413.1	54	0.47
A290		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)-5- fluorothiazol-2-yl)-3- (2-hydroxyethyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.65 (s, 1H), 7.50-7.35 (m, 4H), 6.34 (br. s, 1H), 4.76 (t, J = 4.0 Hz, 1H), 3.53 (s, 1H), 3.41 (q, J = 4.0 Hz, 1H), 3.15 (q, J = 4.0 Hz, 1H), 1.86 (s, 3H).	368.0	222	4.23
A291		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- ylmethyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 7.46-7.34 (m, 4H), 6.94 (s, 1H), 4.10-3.95 (m, 2H), 4.0 (br. s, 2H), 3.58 (br. s, 2H), 3.49 (br. s. 1H), 2.81-2.70 (m, 1H), 2.64 (br. s, 4H), 2.46-2.40 (m, 3H), 2.24 (br. s, 4H), 1.85 (s, 3H).	444.0	109	1.65
A292		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(piperazin-1- ylmethyl)azetidine-1- carboxamide	1H NMR (400 MHz, DMSO- d6) δ 10.91 (br. s, 1H), 8.78 (br. s, 1H), 7.42-7.35 (m, 4H), 6.95 (s, 1H), 4.09-3.96 (m, 2H), 3.65-3.55 (br. s, 2H), 3.50 (br. s, 1H), 3.08-2.99 (m, 4H), 2.87-2.70 (m, 1H), 2.60-2.52 (m, 4H), 1.85 (s, 3H).	444.1	43	0.65
A293		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxy-2- methylpropan-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.47 (s, 1H), 7.29-7.49 (m, 4H), 6.88 (s, 1H), 6.15 (br. s, 1H), 4.93 (t, J = 5.40 Hz, 1H), 3.49 (s, 1H), 3.33 (br s, 2H), 1.84 (s, 3H), 1.19 (s, 6H).	378.1	9361	8.11
A294		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxy-2- methylpropan-2- yl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.47 (s, 1H), 7.31-7.50 (m, 4H), 6.88 (s. 1H), 6.15 (br s, 1H), 4.94 (t. J = 5.52 Hz, 1H), 3.49 (s, 1H), 3.33 (br s, 2H), 1.84 (s, 3H), 1.19 (s, 6H).	378.1	285	3.04
A295		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(hydroxymethyl) cyclopropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.46 (br s, 1H), 7.33-7.47 (m, 4H), 6.91 (s, 1H), 6.57 (br s, 1H), 4.58-4.99 (m, 1H), 3.49 (s, 1H), 3.37 (br s, 2H), 1.84 (s, 3H), 0.54-0.75 (m, 4H).	376.1	522	1.79
A296		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(hydroxymethyl) cyclopropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.45 (br s, 1H), 7.31-7.45 (m, 4H), 6.92 (s, 1H), 6.55 (br s, 1H), 4.77 (br s, 1H), 3.49 (s, 1H), 3.36-3.37 (m, 2H), 1.84 (s, 3H), 0.53-0.77 (m, 4H)	376.1	114	4.79
A297		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1,3- dihydroxypropan-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.42 (d, J = 8.3 Hz, 2H), 7.31-7.27 (m, 2H), 6.76 (s, 1H), 3.87 (s, 1H), 3.71-3.52 (m, 4H), 2.60 (s, 1H), 1.93 (s, 3H)	380.1	935	4.39
A298		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1,3- dihydroxypropan-2- yl)urea	1H NMR (400 MHz, CDCl3) δ 7.41 (d, J = 8.3 Hz, 2H), 7.32-7.26 (m, 2H), 6.75 (s, 1H), 3.86 (s, 1H), 3.69-3.52 (m, 4H), 2.60 (s, 1H), 1.92 (s, 3H)	380.1	246	1.15
A299		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.44-7.36 (m, 2H), 7.31-7.27 (m, 2H), 6.77 (s, 1H), 3.52-3.41 (m, 2H), 3.39-3.27 (m, 2H), 2.56 (s, 1H), 1.93 (s, 3H)	351.1	58	0.46
A300		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxyethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.43-7.36 (m, 2H), 7.29 (d, J = 7.3 Hz, 2H), 6.77 (s, 1H), 3.53-3.41 (m, 2H), 3.38-3.27 (m, 2H), 2.56 (s, 1H), 1.93 (s, 3H)	351.1	341	3.01
A301		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((R)-2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.64 (br s, 1H), 7.47-7.40 (m, 2H), 7.40-7.34 (m, 2H), 6.89 (s, 1H), 6.41 (s, 1H), 3.54-3.42 (m, 2H), 3.37-3.20 (m, 3H), 3.04-2.91 (m, 1H), 1.85 (s, 3H)	380.0	354	2.22
A302		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((S)-2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.64 (br s, 1H), 7.46-7.40 (m, 2H), 7.40-7.34 (m, 2H), 6.89 (s, 1H), 6.43 (s, 1H), 3.54-3.43 (m, 2H), 3.37-3.20 (m, 3H), 3.03-2.91 (m, 1H), 1.85 (s, 3H)	379.9	417	2.04
A303		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((R)-2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.64 (br s, 1H), 7.48-7.40 (m, 2H), 7.40-7.33 (m, 2H), 6.89 (s, 1H), 6.43 (s, 1H), 3.56-3.41 (m, 2H), 3.37-3.19 (m, 3H), 3.04-2.88 (m, 1H), 1.85 (s, 3H)	380.0	101	0.66
A304		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-((S)-2,3- dihydroxypropyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.67 (br s, 1H), 7.48-7.40 (m, 2H), 7.33 (m, 2H), 6.90 (s, 1H), 6.54 (s, 1H), 3.57-3.42 (m, 2H), 3.38-3.20 (m, 3H), 3.07-2.90 (m, 1H), 1.85 (s, 3H)	380.0	90	0.52
A305		1-[4-[1-(4- bromophenyl)-1- methyl-prop-2- ynyl]thiazol-2-yl]-3- (2-hydroxy-2-methyl- propyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.57 (br. s, 1H), 7.51 (d, J = 8.5 Hz, 2H), 7.38 (d, J = 8.6 Hz, 2H), 6.89 (s. 1H), 6.37 (br. s, 1H), 4.54 (s, 1H), 3.50 (s, 1H), 3.04 (d, J = 5.7 Hz, 2H), 1.85 (s, 3H), 1.05 (s, 6H).	422.0	167	2.69
A306		1-[4-[1-(4- bromophenyl)-1- methyl-prop-2- ynyl]thiazol-2-yl]-3- (2-hydroxy-2-methyl- propyl)urea	1H NMR (400 MHz, DMSO- d6) δ 10.57 (br. s, 1H), 7.51 (d, J = 8.6 Hz, 2H), 7.38 (d, J = 8.6 Hz, 2H), 6.89 (s, 1H), 6.37 (br. s, 1H), 4.54 (s, 1H), 3.50 (s, 1H), 3.04 (d, J = 5.7 Hz, 2H), 1.85 (s, 3H), 1.05 (s, 6H).	422.1	56	0.83
A307		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 4-hydroxypiperidine- 1-carboxamide		390.1	2058	3.15
A308		N-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2- yl)piperazine-1- carboxamide		375.1	1535	5.33
A309		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-(4-methylbenzyl) pyrrolidin-3-yl)urea	1H NMR (400 MHz, DMSO- d6 δ 10.44 (br s, 1H), 7.48-7.33 (m, 4H), 7.23-7.06 (m, 4H), 6.90 (s, 1H), 6.51 (br s, 1H), 4.10 (br s, 1H), 3.60-3.43 (m, 3H), 2.74-2.59 (m, 1H), 2.56-2.51 (m, 1H), 2.38-2.21 (m, 5H), 2.20-2.08 (m, 1H), 1.84 (s, 3H), 1.54-1.40 (m, 1H).	479.1	1414	4.12
A310		2-(3-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, CDCl3) δ 7.32-7.27 (m, 2H), 6.89-6.79 (m, 2H), 6.74 (s, 1H), 6.02 (br s, 3H), 3.80 (s, 3H), 3.74-3.59 (m, 2H), 3.15-2.95 (m, 2H), 2.54 (s, 1H), 1.87 (s, 3H).	409.0	223	0.98
A311		2-(3-(4-(2-(4- methoxyphenyl)but-3- yn-2-yl)thiazol-2- yl)ureido) ethanesulfonamide	1H NMR (400 MHz, CDCl3) δ 7.27-7.23 (m, 2H), 6.88-6.80 (m, 2H), 6.75 (s, 1H), 6.07 (br s, 3H), 3.80 (s, 3H), 3.74-3.62 (m, 2H), 3.10-2.93 (m, 2H), 2.51 (s, 1H), 1.86 (s, 3H).	409.0	95	0.66
A312		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxypropan- 2-yl)urea	1H NMR (400 MHz, CD3OD) δ 7.54-7.46 (m, 2H), 7.32-7.25 (m, 2H), 6.91 (s, 1H), 3.93-3.76 (m, 1H), 3.60-3.41 (m, 2H), 2.96 (s, 1H), 1.92 (s, 3H), 1.16 (d, J = 6.4 Hz, 3H).	365.6	545	2.12
A313		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxypropan- 2-yl)urea	1H NMR (400 MHz, CD3OD) δ 7.55-7.43 (m, 2H), 7.37-7.24 (m, 2H), 6.90 (s, 1H), 3.91-3.76 (m, 1H), 3.56-3.44 (m, 2H), 2.96 (s, 1H), 1.92 (s, 3H), 1.16 (d, J = 6.4 Hz, 3H).	365.5	614	2.82
A314		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxypropan- 2-yl)urea	1H NMR (400 MHz, CD3OD) δ 7.58-7.39 (m, 2H), 7.36-7.18 (m, 2H), 6.90 (s, 1H), 3.97-3.75 (m, 1H), 3.62-3.37 (m, 2H), 2.96 (s, 1H), 1.92 (s, 3H), 1.16 (d, J = 6.4 Hz, 3H).	365.5	261	0.80
A315		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(1-hydroxypropan- 2-yl)urea	1H NMR (400 MHz, CD3OD) δ 7.57-7.46 (m, 2H), 7.35-7.21 (m, 2H), 6.91 (s, 1H), 4.00-3.73 (m, 1H), 3.56-3.41 (m, 2H), 2.96 (m, 1H), 1.92 (s, 3H), 1.16 (d, J = 6.4 Hz. 3H).	365.6	81	0.65
A316		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxypropyl)urea	1H NMR (400 MHz, CD3OD) δ 7.54-7.44 (m, 2H), 7.32-7.25 (m, 2H), 6.91 (s, 1H), 3.90-3.76 (m, 1H), 3.28 (s, 1H), 3.16-3.04 (m, 1H), 2.95 (s, 1H), 1.92 (s, 3H), 1.15 (d, J = 6.4 Hz, 3H).	365.6	421	1.81
A317		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxypropyl)urea	1H NMR (400 MHz, CD3OD) δ 7.52-7.44 (m, 2H), 7.32-7.26 (m, 2H), 6.91 (s, 1H), 3.89-3.78 (m, 1H), 3.30-3.25 (m, 1H), 3.15-3.06 (m, 1H), 2.95 (s, 1H), 1.92 (s, 3H), 1.15 (d. J = 6.4 Hz, 3H).	365.6	85	0.97
A318		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxypropyl)urea	1H NMR (400 MHz, CD3OD) δ 7.56-7.43 (m, 2H), 7.34-7.22 (m, 2H), 6.91 (s, 1H), 3.92-3.70 (m, 1H), 3.30-3.25 (m, 1H), 3.15-3.06 (m, 1H), 2.95 (s, 1H), 1.92 (s, 3H), 1.15 (d, J = 6.4 Hz, 3H).	365.6	534	2.24
A319		1-(4-(2-(4- chlorophenyl)but-3- yn-2-yl)thiazol-2-yl)- 3-(2- hydroxypropyl)urea	1H NMR (400 MHz, CD3OD) δ 7.59-7.43 (m, 2H), 7.35-7.14 (m, 2H), 6.91 (s, 1H), 3.89-3.75 (m, 1H), 3.30-3.24 (m, 1H), 3.14-3.05 (m, 1H), 2.95 (s, 1H), 1.92 (s, 3H), 1.15 (d. J = 6.4 Hz, 3H).	365.6	156	0.67
A320		1-14-[1-(4- chlorophenyl)-1- methyl-prop-2- ynyl]thiazol-2-yl]-3- (2,2-dideuterio-2- hydroxy-ethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.34-7.28 (m, 2H), 7.22-7.19 (m, 2H), 6.69 (s, 1H), 3.23 (d, J = 5.5 Hz, 2H), 2.48 (s, 1H), 1.84 (s, 3H)	352.1	44
A321		1-14-11-(4- chlorophenyl)-1- methyl-prop-2- ynyl]thiazol-2-yl]-3- (2,2-dideuterio-2- hydroxy-ethyl)urea	1H NMR (400 MHz, CDCl3) δ 7.43-7.35 (m, 2H), 7.31-7.27 (m, 2H), 6.76 (s, 1H), 3.31 (d, J = 5.5 Hz, 2H), 2.55 (s, 1H), 1.92 (s, 3H)	352.1	28	0.30

Example 10

Preparation of tert-butyl 4-(4-((3(4-(1-(4-bromo phenyl)ethyl)thiazol-2-yl)ureido)methyl)phenyl)piperazine-1-carboxylate

[0327]

Example 11

Preparation of tert-butyl 4-(5-((3-(4-(2-(4-bromophenyl)propan-2-yl)thiazol-2-yl)ureido methyl-3-fluoropyridin-2-yl)piperazine-1-carboxylate

[0329]

Example 12

Preparation of 5-((3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl ureido methyl)-2-(3-methylpiperazin-1-yl)benzamide

[0331]

Step 1 Preparation of 2-(4-(tert-butoxycarbonyl)-3-methylpiperazin-1-yl)-5-((3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl)ureido)methyl)benzoic acid

[0332]

Step 2: Preparation of tert-butyl 4-(2-carbamoyl-4-((3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl)ureido)methyl)phenyl)-2-methylpiperazine-1-carboxylate

[0334]

Example 13

Preparation of 1-((6-((2-hydroxyethyl)amino)pyridin-3-yl)methyl)-3-(4-(2-(4-methoxyphenyl)propan-2-yl)thiazol-2-yl)urea

[0336]

Example 14

Preparation of 1-(4-(2-(4-methoxyphenyl)but-3-yn-2-yl)thiazol-2-yl)-3-(1-(4-(piperazin-1-yl)phenyl)ethyl)urea

[0338]

Step 1. Preparation of methyl 2-(4-methoxyphenyl)acetate

[0339]

Step 2. Preparation of compound methyl 2-(4-methoxyphenyl)-3-oxobutanoate

[0342]

Step 3. Preparation of compound methyl 2-(4-methoxyphenyl)-2-methyl-3-oxobutanoate

[0345]

Step 4. Preparation of compound methyl 4-bromo-2-(4-methoxyphenyl)-2-methyl-3-oxobutanoate

[0348]

Step 5. Preparation of compound methyl 2-(2-aminothiazol-4-yl)-2-(4-methoxyphenyl)propanoate

[0351]

Step 6. Preparation of compound methyl 2-(4-methoxyphenyl)-2-(2-((phenoxycarbonyl)amino)thiazol-4-yl)propanoate

[0354]