Patent ID: 6121258
Filing Date: 2000-09-19
Classification: A61P,C07D

Abstract:
A compound having a structure according to Formula (I) ##STR19## wherein R.sub.1 is H;R.sub.2 is hydrogen, alkyl, or acyl;Ar is COR.sub.3 or SO.sub.2 R.sub.4 ; andR.sub.3 is selected from alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino;R.sub.4 is selected from alkyl, heteroalkyl, aryl, and heteroaryl, substituted or unsubstituted;X is NR.sub.5, wherein R.sub.5 is independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO.sub.2 R.sub.6, COR.sub.7, CSR.sub.8, and PO(R.sub.9).sub.2, or may optionally form a ring with W or Y; andR.sub.6 is selected from alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino;R.sub.7 is selected from hydrogen, alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino;R.sub.8 is selected from alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino;R.sub.9 is selected from alkyl, aryl, heteroaryl, and heteroalkyl;W is hydrogen or one or more lower alkyl moieties, or is an alkylene, arylene or heteroarylene bridge between two adjacent or nonadjacent carbons (thus forming a fused ring);Y is independently selected from one or more of hydrogen, hydroxy, SR.sub.10, SOR.sub.4, SO.sub.2 R.sub.4, alkoxy, and amino, wherein amino is of formula NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 are independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO.sub.2 R.sub.6, COR.sub.7, CSR.sub.8, and PO(R.sub.9).sub.2 ; andR.sub.10 is selected from hydrogen, alkyl, aryl, and heteroaryl;Z is nil, a spiro moiety or an oxo group substituted on the heterocyclic ring; andn is 2;or an optical isomer, diastereomer or enantiomer for Formula (I), or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof.