Patent ID: 6469000
Filing Date: 2002-10-22
Classification: A61P,C07D

Abstract:
A compound having a structure according to Formula (I) whereinR1 is H; R2 is hydrogen, alkyl, or acyl; Ar is COR3 or SO2R4; and R3 is alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino; R4 is alkyl, heteroalkyl, aryl, or heteroaryl, substituted or unsubstituted; X is O, S, SO, SO2, or NR5, wherein R5 is independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO2R6, COR7, CSR8, PO(R9)2 or may optionally form a ring with Y or W; and wherein the heterocyclic rings have at least one of the following heteroatoms: sulfur, oxygen or nitrogen: R6 is alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino; R7 is hydrogen, alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino; R8 is alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino; R9 is alkyl, aryl, heteroaryl, heteroalkyl; W is hydrogen or one or more lower alkyl moieties, or a heterocycle, or is an alkylene, arylene or heteroarylene bridge between two adjacent or nonadjacent carbons (thus forming a fused ring); Y is independently one or more of hydrogen, hydroxy, SR10, SOR4, SO2R4, alkoxy, amino, wherein amino is of formula NR11, R12, wherein R11 and R12 are independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO2R6, COR7, CSR8, PO(R9)2; and R10 is hydrogen, alkyl, aryl, heteroaryl; Z is nil, a spiro moiety or an oxo group substituted on the heterocyclic ring; n is 1-4, except where X&boxH;NR5, n is 2-4; or an optical isomer, diastereomer or enantiomer for Formula (I), or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof.