Patent ID: 6326499
Filing Date: 2001-12-04
Classification: A61P,C07C,Y10S

Abstract:
A compound of formula I: ##STR11##wherein:R.sup.1 is CO.sub.2 R, CONR.sup.2 R.sup.3, CH.sub.2 OR.sup.4, CH.sub.2 NR.sup.5 R.sup.6, CH.sub.2 N.sub.3, CH.sub.2 Hal, CH.sub.2 NO.sub.2, CH.sub.2 SR.sup.20, COSR.sup.21, or 2,3,4,5-tetrazol-1-yl, where:R is H or a pharmaceutically acceptable cation, or CO.sub.2 R forms a pharmaceutically acceptable ester moiety;NR.sup.2 R.sup.3, NR.sup.5 R.sup.6 are the same or different and comprise a free or functionally modified amino group;OR.sup.4 comprises a free or functionally modified hydroxy group; Hal is F, Cl, Br, or I;SR.sup.20 comprises a free or functionally modified thiol group;R.sup.21 is H or a pharmaceutically acceptable cation, or COSR.sup.21 forms a pharmaceutically acceptable thioester moiety;A, B, C, D are the same or different and are C.sub.1 -C.sub.5 alkyl, C.sub.2 -C.sub.5 alkenyl, C.sub.1-5 cyclopropyl, C.sub.2 -C.sub.5 alkynyl, or a C.sub.3 -C.sub.5 allenyl group;E is ##STR12##where OR.sup.7 comprises a free or functionally modified hydroxy group;X=(CH.sub.2).sub.m or (CH.sub.2).sub.m O, where m=1-6; andY=a phenyl ring optionally substituted with alkyl, halo, trihalomethyl, acyl, or a free or functionally modified hydroxy, amino, or thiol group; orX--Y (CH.sub.2).sub.p Y.sup.1 ; where p=0-6; and ##STR13##wherein:W=CH.sub.2, O, S(O).sub.q, NR.sup.8, CH.sub.2 CH.sub.2, CH.dbd.CH, CH.sub.2 O, CH.sub.2 S(O)q, CH.dbd.N, or CH.sub.2 NR.sup.8 ; where q=0-2, and R.sup.8 =H, alkyl, or acyl;Z=H, alkyl, acyl, halo, trihalomethyl, or a free or functionally modified amino, thiol, or hydroxy group; and----=single or double bond;or X--Y=cyclohexyl.