Patent ID: 6288277
Filing Date: 2001-09-11
Classification: A61P,C07C,C07D

Abstract:
A compound of formula I ##STR41##whereinX denotes O, NH, N(CH.sub.3), or CH.sub.2 ;Y denotes O, NH, N(CH.sub.3), or CH.sub.2 ;R.sub.1 denotes H, F, Cl, Br, I, C.sub.1-6 -alkyl, OH, O--C.sub.1-6 -alkyl, or CF.sub.3 ;R.sub.2 denotes H, F, Cl, Br, I, C.sub.1-6 -alkyl, OH, O--C.sub.1-6 -alkyl, or CF.sub.3 ;R.sub.3 denotes H, NH.sub.2, or NHCOR.sub.5 ;R.sub.4 denotes H, CH.sub.2 NH.sub.2, or CH.sub.2 NHCOR.sub.5 ;R.sub.5 denotes H, C.sub.1-6 -alkyl, phenyl, O--(C.sub.1-6 -alkyl), wherein the phenyl ring is optionally mono- or di-substituted by: F, Cl, Br, I, R.sub.a, OR.sub.a, or CF.sub.3,R.sub.a denotes H, or C.sub.1-6 -alkyl;A denotes CR.sub.6 R.sub.7, CO, SO.sub.x, or O;x denotes 0, 1, or 2;R.sub.6 denotes H, C.sub.1-4 -alkyl, C.sub.3-6 -cycloalkyl, --(CH.sub.2).sub.y COOR.sub.8, CF.sub.3, --(CH.sub.2).sub.y OR.sub.8, or OR.sub.8 ;y denotes 0, 1, 2, 3, or 4;R.sub.7 denotes H, C.sub.1-4 -alkyl, C.sub.3-6 -cycloalkyl, --(CH.sub.2).sub.z COOR.sub.8, --(CH.sub.2).sub.z OR.sub.8, or CF.sub.3 ;z denotes 0, 1, 2, 3, or 4, wherein R.sub.6 and R.sub.7 together optionally form a C.sub.3-6 -cycloalkyl ring;R.sub.8 denotes H, or C.sub.1-6 -alkyl;B denotes C.sub.1-6 -alkyl, Ar, or CONR.sub.9 R.sub.10, and, if A represents --C(CH.sub.3).sub.2 : CH.sub.2 NR.sub.9 R.sub.10, or CH.sub.2 NR.sub.9 COR.sub.11 ;Ar denotes phenyl, naphthyl, thienyl, or pyridyl--optionally mono- or di-substituted with R.sub.12,R.sub.9 denotes H, or C.sub.1-6 -alkyl;R.sub.10 denotes H, or C.sub.1-6 -alkyl, wherein R.sub.9 and R.sub.10 together with the nitrogen atom optionally form a ring having 3 to 7 carbon atoms;R.sub.11 denotes H, C.sub.1-6 -alkyl, --O--(C.sub.1-6 -alkyl), or phenyl;R.sub.12 denotes H, C.sub.1-6 -alkyl, O--(C.sub.1-6 -alkyl), F, Cl, Br, I, R.sub.a, CF.sub.3, CHF.sub.2, C(CH.sub.3).sub.2 -phenylene-OH, COOR.sub.a, CONR.sub.a R.sub.b, or OR.sub.c ;R.sub.a denotes H, or C.sub.1-6 -alkyl;R.sub.b denotes H, or C.sub.1-6 -alkyl, wherein R.sub.a and R.sub.b together with the nitrogen atom optionally form a ring having 3 to 7 carbon atoms;R.sub.c denotes H, C.sub.1-6 -alkyl, COOR.sub.d, COR.sub.d, or a group of formula ##STR42##wherein l, m, n each denote 0, 1, 2, 3 or 4 with the proviso that l+m+n.ltoreq.4;R.sub.d denotes C.sub.1-6 -alkyl, or phenyl,the individual optical isomers thereof, a mixture of the individual enantiomers, a free base thereof such or an acid addition salt thereof with pharmacologically acceptable acids, with the proviso that R.sub.3 and R.sub.4 together cannot denote hydrogen.