Patent ID: 6294529
Filing Date: 2001-09-25
Classification: A61P,C07D

Abstract:
A compound represented by formula I: ##STR179##as well as pharmaceutically acceptable salts thereof, wherein all compounds which have one or more cations are balanced with one or more, as necessary, of a charge balancing group X- or carboxylate anion:R.sup.1 represents H or methyl; CO.sub.2 M represents a carboxylic acid, a carboxylate anion, or a pharmaceutically acceptable ester group;P represents hydrogen, hydroxyl, or F;A-Q-L-B represents a side chain wherein:A is a C.sub.1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of --O--, --S--, NR.sup.a --, --C(O)-- and --CH.dbd.CH--;Q represents ##STR180##in which:b is 2 or 3;and X- is a charge balancing group;L represents a C.sub.1-8 alkylene group, unsubstituted or substituted with 1-3 R.sup.c groups, and is interrupted or terminated by 1-3 of --CH.dbd.CH--, --C(O)--, --C(O)NR.sub.d --, --Het(R.sup.e)--, --C(O)--Het(R.sup.e)--, --C(O)NR.sup.a --Het(R.sup.e)--, --O--, --S--, --S(O)--, --SO.sub.2 --, --CO.sub.2 --, --NR.sup.a, --N.sup.+ (R.sup.a).sub.2 --, ##STR181##Het is a heteroaryl group;B represents ##STR182##wherein ##STR183##represents a 5-10 membered mono- or bicyclic, N-containing heteroarylium group, optionally containing 1-4 additional heteroatoms selected from O, S and N;R.sup.a is H or C.sub.1-6 alkyl;R.sup.b is NH.sub.2 or C.sub.1-6 alkyl unsubstituted or substituted with 1-3 groups selected from halo, OH, CN and C(O)NH.sub.2 ;R.sup.c is independently selected from halo, OR.sub.a, SR.sup.a, OC(O)R.sup.a, CO.sub.2 R.sup.a, CN, C(O)N(R.sup.a).sub.2 and C(O)R.sup.a,R.sub.d is H or C.sub.1-3 alkyl, or R.sup.c and R.sub.d taken together with any intervening atoms and additional carbon atoms; represent a 4-6 membered heterocyclic ring;R.sup.e is H; R.sup.c ; NO.sub.2 ; N(R.sup.a).sub.2 ; SO.sub.2 N(R.sup.a).sub.2 or C.sub.1-4 alkyl, unsubstituted or substituted with 1-3 groups selected from halo, OH and C(O)NH.sub.2 ;R.sup.f, R.sup.g and R.sup.h are independently selected from H; C.sub.1-6 straight or branched chain alkyl, unsubstituted or substituted with 1-3 R.sup.c groups; C.sub.3-6 cycloalkyl, unsubstituted or substituted with 1-3 R.sup.c groups; phenyl, unsubstituted or substituted with 1-3 R.sup.e groups and Het, unsubstituted or substituted with 1-3 R.sup.e groups,orR.sup.f and Rg taken together with the intervening N atom and additional carbon atoms represent a 4-6 membered heterocyclic ring, optionally interrupted by 1-2 of O, S, C(O) or NR.sup.h, and optionally substituted by 1-3 R.sup.c groups;and each R independently represents H; NO.sub.2 ; N(R.sup.a).sub.2 ; SO.sub.2 N(R.sup.a).sub.2 ; R.sup.c or C.sub.1-4 alkyl, unsubstituted or substituted with 1-3 groups selected from halo, OH, C(O)NH.sub.2.