Patent ID: 6201130
Filing Date: 2001-03-13
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula I or a stereoisomer or a pharmaceutically acceptable salt of the foregoing: ##STR25##wherein,R.sup.1 is phenyl monosubstituted by a 5 membered-ring containing 1 or 2 nitrogen atoms;R.sup.2 is selected from1) hydrogen,2) linear (C.sub.1 -C.sub.6)-alkyl, and3) phenyl;R.sup.3 is --(C.sub.1 -C.sub.4)-alkyl-C(O)--N(R.sup.6)--R.sup.7 ;where R.sup.6 and R.sup.7 together with the nitrogen to which they are bonded form a radical of formula IIa: ##STR26##whereinq is zero;Z is carbon;R.sup.8 is selected from1) hydrogen2) linear (C.sub.1 -C.sub.6)-alkyl,3) branched (C.sub.1 -C.sub.6)-alkyl,4) cyclic (C.sub.3 -C.sub.6)-alkyl,5) hydroxyl,6) (C.sub.1 -C.sub.6)-alkyl-C(O)--O--,7) (C.sub.1 -C.sub.6)-alkyl-O--,8) (C.sub.1 -C.sub.6)-alkyl-O--(C.sub.1 -C.sub.4)-alkyl-O--,9) halogen,10) CF.sub.3,11) CN,12) NO.sub.213) HO--C(O)--,14) (C.sub.1 -C.sub.6)-alkyl-O--C(O)--,15) methylenedioxo,16) R.sup.4 --(R.sup.5)N--C(O)--, and17) R.sup.4 --(R.sup.5)N--;A is a covalent bond;B is --(CH.sub.2).sub.m --,where m is selected from zero, 1, 2, 3, 4, 5, and 6;X is --CH.dbd.CH--;R.sup.4 and R.sup.5 are independently selected from1) hydrogen,2) (C.sub.1 -C.sub.6)-alkyl,3) HO--C(O)--(C.sub.1 -C.sub.6)-alkyl,4) picolyl,5) phenyl-(CH.sub.2).sub.n --, where phenyl is unsubstituted, monosubstituted, or disubstituted with at least one substituent selected from linear (C.sub.1 -C.sub.6)-alkyl, branched (C.sub.1 -C.sub.6)-alkyl, cyclic (C.sub.3 -C.sub.6)-alkyl, hydroxyl, (C.sub.1 -C.sub.6)-alkyl-C(O)--O--, (C.sub.1 -C.sub.6)-alkyl-O--, (C.sub.1 -C.sub.6)-alkyl-O--(C.sub.1 -C.sub.4)-alkyl-O, halogen, CF.sub.3, CN, NO.sub.2, HO--C(O)--, (C.sub.1 -C.sub.6)-alkyl-O--C(O), methylenedioxo, R.sup.4a --(R.sup.5a)N--C(O), and R.sup.4a --(R.sup.5a)N--;where R.sup.4a and R.sup.5a are independently selected from hydrogen, (C.sub.1 -C.sub.6)-alkyl, HO--C(O)--(C.sub.1 -C.sub.6)-alkyl, substituted or unsubstituted phenyl-(CH.sub.2).sub.n --, and picolyl;n is selected from zero, 1, and 2;or together R.sup.4 and R.sup.5, form a 4, 5, 6, or 7 membered ring with the nitrogen to which R.sup.4 and R.sup.5 are attached wherein the remaining ring atoms are carbon.