Patent ID: 6441017
Filing Date: 2002-08-27
Classification: A61K,A61P,B82Y,C07D

Abstract:
A compound of the formula A: whereinX1 is (C(R1a)2)nA1(C(R1a)2)nA2; X2 is (C(R1b)2)pA3(C(R1b)2)p; X3 is (C(R1c)2)qA4(C(R1c)2)q; R1a, R1b and R1c are independentlys elected from: a) hydrogen; b) unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, unsubstituted or substituted C3-C10 cycloalkyl, R10Oâ€”, R6aS(O)m, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C2-C6 alkynyl, â€”C(O)NR6R7, R10C(O)NR10â€”, (R10)2NC(O) NR10â€”, R10C(O)â€”, â€”N(R10)2, R10OC(O)â€”, or R10OC(O)NR10â€”; and c) unsubstituted or substituted C1-C6 alkyl, wherein one or more of the substituents on the substituted C1-C6 alkyl is selected from unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, unsubstituted or substituted C3-C10 cycloalkyl, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C2-C6 alkynyl, R10Oâ€”, R6aS(O)m, R10C(O)NR10â€”, (R10)2NC(O)NR10â€”, R10C(O)â€”, â€”C(O)NR6R7, R10OC(O)â€”, â€”N(R10)2, R10OC(O)NR10â€”, and halo; A1, A3 and A4 are independently selected from a) a bond, b) â€”C(&boxH;O)â€”, c) â€”HC&boxH;CHâ€”, d) â€”Câ‰¡Câ€”, e) O, f) NR10, g) NR10C(O), h) C(O)NR10, i) OC(O)NR10, j) NR10C(O)O, k) S(&boxH;O)m, l) C(O)O, and m) OC(O); A2 is selected from a) a bond, b) â€”C(&boxH;O)â€”, c) NR10C(O), d) S(&boxH;O)m, and e) OC(O); R2 is independently selected from: a) hydrogen, b) CN, c) NO2, d) halogen, e) aryl, unsubstituted or substituted, f) heterocycle, unsubstituted or substituted: g) C1-C6 alkyl, unsubstituted or substituted, h) OR10, i) N3, j) R6aS(O)m, k) C3-C10 cycloalkyl, umsubstituted or substituted, l) C2-C6 alkenyl, unsubstituted or substituted, m) C2-C6 alkynyl, unsubstituted or substituted, n) (R10)2NC(O)NR10â€”, o) R10C(O)â€”, p) R10C(O)NR10â€”, q) R10OC(O)â€”, r) â€”N(R10)2, s) R10OC(O)NR10â€”, and t) â€”(C1-C6 alkyl)NR10C(O)R13; R3 is independently seleted from: â€ƒH, CN, NO2, halo, unsubstituted or substituted C1-C6 alkyl, N3, oxido, unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C2-C6 alkynyl, unsubstituted or substituted aralkyl, unsubstituted or substituted beterocyclylalkyl, C1-C6 perfluoroalkyl, CF3Oâ€”, CF3CH2â€”, unsubstituted or substituted C3-C10 cycioalkyl, OR10, NR6R7, OR6, â€”C(O)R10, â€”O(C1-C6 alkyl)OR10, â€”S(O)mR6a, â€”C(O)NR6R7, â€”NHC(O)R10, â€”(C1-C6 alkyl)OR10, and â€”(C1-C6 alkyl)C(O)R10; R4 and R5 are independently selected from: â€ƒH, OR10, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C8 alkenyl, unsubstitiuted or substituted C2-C8 alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocycle, â€ƒwherein the substituted group is substituted with one or more of: 1) aryl or heterocycle, unsubstituted or substituted with: a) C1-C6 alkyl, b) (CH2)nOR6, c) (CH2)nNR6R7, d) halogen, e) CN, f) aryl or heteroaryl, g) perfludro-C1-C4 alkyl, h) S(O)mR6a, 2) C3-C6 cycloalkyl, 3) OR6, 4) S(O)mR6a, 15) N3, 16) halo, and 17) perfluoro, C1-4-alkyl; or R4 and R5 are attached to the same C atom and are combined to form â€”(CH2)uâ€” wherein one of the carbon atoms is optionally replaced by a m selected from: O, S(O)m, â€”NC(O)â€”, and â€”N(COR10)â€”; and any of R4 and R5 are optionally attached to the same carbon atom; R6, R7 and R7a are independently selected from: â€ƒH, C1-C6 alkyl, C3-C6 cycloalkyl, heterocycle, aryl, aralkyl, aroyl, heteraroyl, arylsulfonyl, heteroarylsulfony, C1-C4 perfluoroalkyl, unsubstituted or substituted with one or two substituents selected from: a) C1-C6 alkoxy, b) substituted or unsubstituted aryl or substituted or unsubstituted heterocycle, c) halogen, d) HO, g) â€”S(O)mR6a, or h) N(R10)2; or R6 and R7 may be joined in a ring; R7 and R7a may be joined in a ring; R6a is selected from a) C3-6 cycloakyl, heterocycle, aryl, unsubstituted or substituted with one or more of the following: 1) C1-4 alkoxy, 2) aryl or heterocycle, 3) halogen, 4) HO, 6) SO2R6a, 7) N(R10)2; and b) C1-C6 alkyl, unsubstituted or substituted with one or more of the following: 1) â€”C(R10)2C1-4 alkoxy, 2) aryl or heterocyle, 3) â€”C(R10)2 halogen, 4) â€”C(R10)2OH, 6) â€”C(R10)2SO2R6a, and 7) â€”C(R10)2N(R10)2; R8 is independently selected from a) hydrogen, b) unsubstituted or substituted C2-C6 alkenyl, unsubstituted or substituted C2-C6 alkynyl, unsubstituted or substituted C3-C6 cycloalkyl, unsubstituted or substituted C1-C4 perfluoroalkyl, F, Cl, Br, R10Oâ€”, CN, R6aS(O)mâ€”, C(O)NR6R7, R10(C(O)NR10â€”, NO2, (R10)2NC(O)NR10â€”, R10C(O)â€”, R10OC(O)â€”, R10OC(O)NR10â€”, N3, or â€”N(R10)2, and c) C1-C6 alkyl, unsubstituted or substituted by C1-C4 perfluoroalkyl, F, Cl, Br, R10Oâ€”, R6aS(O)mâ€”, R10C(O)NR10â€”, CN, â€”C(O)NR6R7, (R10)2NC(O)NR10â€”, R10C(O)â€”, R10C(O)â€”, N3, â€”N(R10)2, and R10OC(O)NR10â€”; R9 is independently selected from 1) H, unsubstituted or substituted C1-C6 alkyl, unsubstituted or substituted C2-C8 alkenyl, unsubstituted or substituted C2-C8 alkynyl, unsubstituted or substituted aryl, and unsubstituted or substituted heterocyele, wherein the substituted group is substituted with one or more of: a) C1-C6 alkyl, unsubstituted or substituted, b) (CH2)nOR6, c) (CH2)nNR6R7, d) halogen, e) CN, f) aryl, unsubstituted or substituted, g) heterocycle, unsubstituted or substituted, h) perfluoro-C1-C4 alkyl, i) S(O)mR6a, j) N(R10)2, k) NR10C(O)R11, l) NR10OC(O)R11N(R10)2, 2) C3-C6 cycloalkyl, 3) S(O)1-2R6a, 8) â€”(C1-C6 alkyl)NR10C(O)R13; R10 is independently selected from a) hydrogen, b) unsubstituted or substituted C1-C6 alkyl, c) unsubstituted or substituted C3-C6 cycloalkyl, d) 2,2,2-trifluoroethyl, e) unsubstituted or substituted heteroaryl, f) unsubstituted or substituted aralkyl, g) unsubstituted or substituted aryl, and h) unsubstituted or substituted heterocyclylalkyl; R11 is independently selected from a) unsubstituted or substituted C1-C6 alkyl, b) unsubstituted or substituted aralkyl, c) unsubstituted or substituted heterocycle, d) unsubstituted or substituted aryl, and e) unsubstituted or substituted heterocyclylaekyl; R13 is independently selected from a) H, b) unsubstituted or substituted C1-C6 alkyl, c) unsubstituted or substituted C2-C6 alkenyl, d) unsubstituted or substituted C2-C6 alkynyl, e) unsubstituted or substituted aryl, f) unsubstituted or substituted heterocycle, g) aralkyl, unsubstituted or substituted, h) heterocyclylalkyl, unsubstituted or substituted, i) CF3, j) CF3Oâ€”, k) CF3CH2â€”, l) C3-C10 cycloalkyl, unsubstituted or substituted, m) OR10, n) â€”C(O)R10, o) â€”O(C1-C6 alkyl)OR10, p) â€”C(O)NR6R7, q) â€”(C1-C6 alkyl)OR10, and r) â€”(C1-C6 alkyl)C(O)R10; G1 and G2 are independently selected from oxygen or H2; V is aryl; W is a 5-membered heterocycle; Y1 and Y2 are independently selected from a) a bond, b) C1-C8 alkyl, c) C2-C8 alkenyl, d) C2-C8 alkynyl, e) C3-C20 cycyloalkyl, f) aryl, and g) heterocycle; Z1 and Z2 are independently selected from a) a bond, b) O, c) C(O), d) S(O)m, e) C(O)NR10, f) (C(R1a)2)n, g) (C(R1a)2)nO, h) O(C(R1a)2)n, and i) NR10; m is 0, 1 or 2; n is 0, 1, 2, 3, 4, 5 or 6; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2, 3, 4, 5 or 6; r is 0 to 5, provided that r is 0 when V is a bond; s is 0, 1, 2, 3 or 4; provided that s is 0 when W is a bond; t is 0, 1, 2, 3 or 4; provided that t is 0 when Y1 is a bond; u is 4 or 5; v is 0, 1, 2,3 or 4; and w is 0, 1, 2, 3 or 4; or a pharmaceutically acceptable salt, an optical isomer or stereoisomer thereof.