Patent ID: 6239130
Filing Date: 2001-05-29
Classification: A61P,C07D

Abstract:
A compound of formula I ##STR22##wherein:A is hydrogen, C.sub.1 -C.sub.4 alkyl, OR.sup.1, hydroxy, nitro, cyano, --NH.sub.2 --, --NHR.sup.1, or --NR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 independently are C.sub.1 -C.sub.4 alkyl, cyclopropyl, cyclopropylmethyl, or NR.sup.1 R.sup.2 taken together with the nitrogen to which they are bound complete a ring having 4 or 5 carbon atoms;B is hydrogen, C.sub.1 -C.sub.4 alkyl, --CH.sub.2 OM, --CH.sub.2 OC(.dbd.O)(CH.sub.2).sub.a (CO).sub.b Y.sup.1 Y.sup.2, or--(CH.sub.2).sub.c C(.dbd.O)OM;Yl is --(VCH.sub.2 CH.sub.2).sub.c --, with V.dbd.--NH-- or --O--; or Y.sup.1 is --NHCHR.sup.A --C(.dbd.O)--;Y.sup.2 is hydrogen, hydroxy, --OCH.sub.3, or 4-morpholinyl;M is hydrogen or C.sub.1 -C.sub.4 alkyl;a=1 or 2; b=0 or 1; c=0, 1, or 2;Z is CH, then Z.sub.1 and Z.sub.2 both are CH or N; orZ is N, then Z.sub.1 and Z.sub.2 are CH;X.sub.1 and X.sub.2 independently are hydrogen, C.sub.1 -C.sub.4 alkyl, --(CH.sub.2).sub.n --OR.sup.3, halogen, cyano, ##STR23##--O--C.sub.1 -C.sub.6 alkyl, --C(.dbd.O)R.sub.3, --C(.dbd.O)OR.sub.3, --C(.dbd.O)NR.sup.4 R.sup.5, or ##STR24##R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl, phenethyl, or Q.sup.1 -Q.sup.2 ;R.sup.4 is hydrogen, or C.sub.1 -C.sub.4 alkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, --CHRA--C(.dbd.O)OMl, or --Q.sup.3 -Q.sup.4 ;R.sup.6 is hydrogen, C.sub.1 -C.sub.4 alkyl, or --Q.sup.3 -Q.sup.5 ;R.sup.A is a residue of a natural .alpha.-amino-acid, the carbon atom to which it is linked having either a S configuration, or a R configuration;Q.sup.1 is --(CH.sub.2).sub.n --(CHOH).sub.m --(CH.sub.2).sub.p --;Q.sup.2 is hydroxy, --O--C.sub.1 -C.sub.6 alkyl, --OC(.dbd.O)--C.sub.1 -C.sub.6 alkyl, or 4-morpholinyl;Q.sup.3 is --(CH.sub.2).sub.n --;Q.sup.4 is --NHM.sup.1, --NM.sup.1 M.sup.2, or 4-morpholinyl;Q.sup.5 is --M.sup.1 or --OM.sup.1 ;M.sup.1 and M.sup.2 are independently hydrogen or C.sub.1 -C.sub.4 alkyl;n is 1, 2, or 3; m is 0, 1, 2, 3, or 4; p is 0, 1, 2, or 3, provided that if m is not 0,then p is not 0;its racemic form and each of its isomers,and the pharmaceutically acceptable salts thereof.