Patent ID: 6294528
Filing Date: 2001-09-25
Classification: A61P,C07D

Abstract:
A compound represented by formula I: ##STR59##including pharmaceutically acceptable salts thereof, wherein:R.sup.1 represents H or methyl;CO.sub.2 M represents a carboxylic acid, or carboxylate anion, provided that when CO.sub.2 M represents a carboxylate anion it is balanced by Q;P represents hydrogen, hydroxyl or F;each R independently represents R.sup.b, ##STR60##C.sub.2-6 alkenyl, or a group L--Q--R.sup.q with the proviso that only one R group of the type L--Q--R.sup.q can be present;L is C.sub.1-4 straight or branched alkylene, uninterrupted, or interrupted by 1-2 of O, S, NR.sup.a, C(O), CO.sub.2 and C(O)NR.sup.a ;Q represents: ##STR61##Y.sup.- is a charge balancing group;n is a value from 1 to 2 selected to maintain overall charge neutrality;R.sup.a is H or C1-6 alkyl;R.sup.q is C.sub.1-6 alkyl, straight or branched, uninterrupted or interrupted by 1-2 of O, S, NR.sup.a, C(O), C(O)O, C(O)NR.sup.a, --CH.dbd.CH--, --Het(R.sup.b).sub.3 --, --C(O)Het(R.sup.b).sub.3 --,--C(O)NR.sup.a Het(R.sup.b).sub.3 --, ##STR62##said R.sup.q being unsubstituted or substituted with 1-3 R.sup.c groups;Het is a heteroaryl group;each R.sup.b is independently selected from H, halo, OR.sup.a, OC(O)R.sup.a, C(O)R.sup.a, CN, C(O)NR.sup.a R.sup.d, NO.sub.2, NR.sup.a R.sup.d, SO.sub.2 NR.sup.a R.sup.d and C.sub.1-4 alkyl unsubstituted or substituted with 1-3 groups selected from R.sup.e ;each R.sup.c is independently selected from halo, OR.sup.f, OC(O)R.sup.f, SR.sup.f, S(O)R.sup.f, SO.sub.2 R.sup.f, CN, C(O)R.sup.f, CO.sub.2 R.sup.f, NR.sup.f R.sup.g, N.sup.+ R.sup.a R.sup.f R.sup.g Z.sup.-, C(O)NR.sup.a R.sup.f, -Het(R.sup.b).sub.3, C(.dbd.N.sup.+ R.sup.a R.sup.f)R.sup.a Z.sup.-, C(.dbd.N.sup.+ R.sup.a R.sup.f)NR.sup.a R.sup.f Z.sup.-, NR.sup.a C(.dbd.N.sup.+ R.sup.a R.sup.f)R.sup.a Z.sup.-, NR.sup.a C(.dbd.N.sup.+ R.sup.a R.sup.f)NR.sup.a R.sup.f Z.sup.-, heteroarylium(R.sup.b).sub.3 Z.sup.-, SO.sub.2 NR.sup.a R.sup.f, OC(O)NR.sup.a R.sup.f, NR.sup.a C(O)R.sup.f, NR.sup.a C(O)NR.sup.a R.sup.f, and ##STR63##or in the alternative, when 2 or more R.sup.c groups are present, 2 R.sup.c groups may be taken together with any intervening atoms to form a 3-6 membered carbocyclic ring, optionally interrupted with 1-3 of O, S, NR.sup.g, and C(O), said ring being unsubstituted or substituted with 1-3 R.sup.e groups;R.sup.d is H or C.sub.1-4 alkyl, oreach R.sup.e is independently selected from halo, OR.sup.a, NR.sup.a R.sup.d and CONR.sup.a R.sup.d ;R.sup.f is H; C.sub.1-6 straight or branched chain alkyl, unsubstituted or substituted with 1-3 R.sup.e groups; --Het(R.sup.b).sub.3 ; C.sub.3-6 cycloallkyl, unsubstituted or substituted with 1-3 R.sup.e groups, and ##STR64##R.sup.g is H, C.sub.1-6 alkyl, unsubstituted or substituted with 1-3 R.sup.e groups; C.sub.3-6 cycloalkyl, unsubstituted or substituted with 1-3 R.sup.e groups; C(.dbd.N.sup.+ R.sup.a R.sup.f)R.sup.a Z.sup.- or C(.dbd.N.sup.+ R.sup.a R.sup.f)NR.sup.a R.sup.f Z.sup.-, andZ is a charge balancing group selected from Y.sup.-.