Patent ID: 6476020
Filing Date: 2002-11-05
Classification: A61P,C07D

Abstract:
A compound having the structure: wherein:(a) the bond between C&agr; and N&bgr; is a single bond, or a double bond whereby R2 (and H on C&agr;) are nil; (b) the bond between C5 and C6 is a single bond, or a double bond whereby R13 and R15 are nil; the bond between C6 and C7 is a single bond, or a double bond whereby R11 and R13 are nil; but the C5-C6 and C6-C7 bonds are not both double bonds; (c) R1 is selected from the group consisting of hydrogen, alkyl, aryl, and heterocycle; (d) R2, if not nil, is selected from the group consisting of hydrogen, alkyl, alkylacyl, and arylacyl; (e) R3, R4 and R5 are each independently selected from the group consisting of hydrogen, halo, alkyl, aryl, alkylaryl, alkylacyl, heterocycle, nitro, and cyano; or unsubstituted or alkyl- or aryl- or heterocycle-substituted hydroxy, thio, amino, amide, formyl, carboxy and carboxamide; or R3 and R4 together are alkylene or heteroalkylene attached to adjacent carbons of the phenyl to which R3 and R4 are attached thereby forming a ring fused to the phenyl ring of carbons 1â€²-6â€², and R5 is as specified above; (f) R6, R7 and R8 are each independently selected from the group consisting of hydrogen, halo, alkyl, aryl, heterocycle, nitro, and cyano; or alkyl- or aryl- or heterocycle-substituted hydroxy, thio, amino, amide, sulfonamide, formyl, carboxy, and carboxamide; or R6 and R7 together are alkylene or heteroalkylene attached to adjacent carbons of the phenyl to which R6 and R7 are attached thereby forming a ring fused to the phenyl ring of carbons 8-11, and R8 is as specified above; (g) R9 is selected from the group consisting of hydrogen, halo, alkyl, aryl, heterocycle, and carboxy and its alkyl and aryl esters and amides; (h) R10, R12 and R14 and R11, R13 and R15 if not nil, are each independently selected from the group consisting of hydrogen, alkyl, and aryl; and an optical isomer, diastereomer or enantiomer thereof; and a pharmaceutically acceptable salt or hydrate thereof.