Patent ID: 6525076
Filing Date: 2003-02-25
Classification: A61K,C07D,C07F,C07K

Abstract:
A compound having the formula: wherein:R2 is H, C1-6alkyl, C3-6cycloalkyl, C1-3alkylaryl, C1-3alkyl-C3-8cycloalkyl or aryl and R3is H, C1-6alkyl, or R2 and R3 are taken together to form a carbocyclic ring; R13 is H, C1-3alkyl, C1-3alkylaryl, aryl, or â€”CF3; X is CR1; where R1 is H, C1-3alkyl, C1-3alkylaryl, aryl, or â€”CF3; Z is CR14; where R14 is H, C1-3alkyl, C1-3alkylaryl, aryl, or â€”CF3; m is an integer from 0-3; n is an integer from 0-6; p is an integer from 0-4; s is an integer from 0-2; A is selected from the group consisting of: R4; â€”NR4R5; where R4, R5, R17 and R18 are independently selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; R19 is selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; and R20 is selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; W is C1-6alkyl, C3-8cycloalkyl, C1-6alkenyl, or aryl; K is selected from the group consisting of a direct link, C3-8cycloalkyl, aryl; E is selected from the group consisting of R26, â€”NR26R27, where R26, R27, R28 and R29 are independently selected from the group consisting of H, â€”OH, C1-6alkyl, aryl and C1-4alkylaryl; R30 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl; and R31 is selected from the group consisting of H, C1-6alkyl, aryl and C1-4alkylaryl;Y is where G is H, â€”COOR21, â€”CONR21R22, â€”CF3, â€”CF2CF3 or a group having the formula: where:R23 is selected from the group consisting of H, C1-6alkyl, C2-6 alkenyl, C0-6alkylaryl, C2-6alkenylaryl, â€”CF3 and â€”CF2CF3; J is â€”Sâ€”, â€”SOâ€”, â€”SO2â€”, â€”Oâ€” or â€”NR6â€”, where R6 is H, C1-6alkyl or benzyl; and L is selected from the group consisting of: where r is an integer from 0-2; R7 and R8 are independently selected from the group consisting of H, C1-6alkyl, aryl, C1-6alkylaryl, â€”COOR11, â€”CONR11R12, â€”CN and â€”CF3; R9 and R10 are independently selected from the group consisting of H, C1-6alkyl, aryl, C1-6alkylaryl, C1-4alkyloxy, halogen, â€”NO2, â€”NR11R12, â€”NR11COR12, â€”Oâ€”R11, â€”Oâ€”COR11, â€”COOR11, â€”CONR11R12, â€”CN, â€”CF3, â€”SO2NR11R12 and C1-6alkyl-Oâ€”R11; and R11 and R12 are independently selected from the group consisting of H, C1-6alkyl, C1-3alkylaryl and aryl; U is â€”Oâ€”, â€”Sâ€”, â€”Nâ€” or â€”N(H)â€”; V is â€”Oâ€”, â€”Sâ€”, â€”Nâ€” or â€”N(H)â€”; with the proviso that at least one of U or V is â€”Nâ€” or â€”N(H)â€”; and all optical isomers thereof.