Patent ID: 6344483
Filing Date: 2002-02-05
Classification: A61P,C07C,C07D

Abstract:
A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H, C1-C10 alkyl, C2-C10 alkenyl, and C2-C10 alkynyl; R2 is selected from the group consisting of H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, and either R or S alpha-amino acid; R3 and R4 are independently selected from the group consisting of H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, and NO2; wherein R1, R2, R3 and R4 are optionally substituted from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, hydroxy, lower alkoxy, aryloxy, thiol, lower thioalkoxy, halogen, cyano, nitro, amino, carboxy, carboxyalkyl, carboxyaryl, amidino, and guanidino; R11 is selected from the group consisting of hydroxyl and R or S alpha-amino acid; G is selected from the group consisting of C1-C10 alkylene, C2-C10 alkenediyl, and C2-C10 alkanediyl, each of which is optionally substituted with one or more selected from the group consisting of halogen, hydroxy, trifluoromethyl, nitro, cyano, amino, C1-C10 alkyl, &boxH;CH2, C2-C10 alkenyl, C2-C10 alkynyl, and C1-C10 alkoxy, each of which are optionally substituted from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, hydroxy, lower alkoxy, aryloxy, thiol, lower thioalkoxy, halogen, cyano, nitro, amino, carboxy, carboxyalkyl, carboxyaryl, amidino, guanidino, trifluoromethyl, and nitro; G is selected from the formula (CH2)pâ€”(CX1X2)râ€”(CH2)sâ€”Qâ€”(CH2)tâ€”(CX3X4)uâ€”(CH2)v where p, r, s, t, u, v are independently 0 to 3 and Q is oxygen, C&boxH;O, S(O)a wherein a is 0 to 2, with the proviso that when a is 1 or 2, G must contain halogen, or NR12 wherein R12 is selected from the group consisting of H and C1-C10 alkyl which are optionally substituted with one or more selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, hydroxy, trifluoromethyl, nitro, cyano, amino, and halogen; G is selected from the formula â€”(CH2)wâ€”(CX5X6)yâ€”(CH2)zâ€”Aâ€”(CH2)kâ€”(CX7X8)jâ€”(CH2)h wherein w, y, z, k, j, h are independently 0 to 3 and A is a 3 to 6 membered carbocyclic radical which are optionally substituted with one or more selected from the group consisting of halogen, C1-C10 alkyl, C1-C10 alkoxy, hydroxy, trifluoromethyl, nitro, cyano, and amino, each of which are optionally substituted with halogen or C1-C10 alkyl, with the proviso that when G is selected from the formula â€”(CH2)wâ€”(CX5X6)yâ€”(CH2)zâ€”Aâ€”(CH2)kâ€”(CX7X8)jâ€”(CH2)h, Y must contain halogen; X1, X2, X3, X4, X5, X6, X7, X8 are independently not present, H, halogen, C1-C10 alkyl, &boxH;CH2, C2-C10 alkenyl, or C2-C10 alkynyl, wherein C1-C10 alkyl, &boxH;CH2, C2-C10 alkenyl, and C2-C10 alkynyl which is optionally substituted from one or more of the group consisting of lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, hydroxy, lower alkoxy, aryloxy, thiol, lower thioalkoxy, halogen, cyano, nitro, amino, carboxy, carboxyalkyl, carboxyaryl, amidino, guanidino, trifluoromethyl, and nitro; Y is selected from the group consisting of, C1-C10 haloalkyl, C1-C10 dihaloalkyl, C1-C10 trihaloalkyl, C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, and C2-C10 alkynyl, each of which is optionally substituted with one or more selected from the group consisting of halogen, hydroxy, trifluoromethyl, nitro, cyano, amino, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, and C1-C10 alkoxy; or Y is NR9R10 wherein R9 and R10 are independently selected from the group consisting of H, C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C2-C10 alkynyl, nitro, amino, aryl, and C1-C10 alkaryl; with the proviso that at least one of G or Y contains a halogen.