Patent ID: 6127423
Filing Date: 2000-10-03
Classification: A61P,C07C,C07D,Y10S

Abstract:
A compound of general formula I ##STR61## wherein A denotes X.sub.1 --C.sub.m H.sub.2m --X.sub.2, in which m is an integer 2, 3, 4, 5 or 6 or ##STR62## and X.sub.1 denotes O, NH or NCH.sub.3 ;X.sub.2 denotes O, NH, NCH.sub.3 or ##STR63## X.sub.3 denotes X.sub.1 --C.sub.n H.sub.2n in which n is the integer 1 or 2;X.sub.4 denotes C.sub.n H.sub.2n --X.sub.1, wherein n is the integer 1 or 2;R.sub.1 denotes C.sub.5-7 -cycloalkyl, Ar.sub.1, OAr.sub.1, CH.sub.2 --Ar.sub.2 ; CR.sub.4 R.sub.5 Ar.sub.3, or C(CH.sub.3).sub.2 R.sub.6 ;R.sub.2 denotes H, C.sub.1-6 -alkyl, OH, halogen, O--(C.sub.1-6 -alkyl);R.sub.3 denotes H, C.sub.1-6 -alkyl;R.sub.4 denotes C.sub.1-4 -alkyl, CF.sub.3, CH.sub.2 OH, COOH, or COO(C.sub.1-4 -alkyl);R.sub.5 denotes H, C.sub.1-4 -alkyl, CF.sub.3, CH.sub.2 OH andR.sub.4 and R.sub.5 may also together form a C.sub.4-6 -alkylene group;R.sub.6 denotes CH.sub.2 OH, COOH, COO(C.sub.1-4 -alkyl), CONR.sub.9 R.sub.10, CH.sub.2 N.sub.9 R.sub.10 ;R.sub.7 denotes H, halogen, OH, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;R.sub.8 denotes H, halogen, OH, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;R.sub.9 denotes H, C.sub.1-6 -alkyl, phenyl, phenyl-(C.sub.1-6 -alkyl), COR.sub.11, COOR.sub.11, CHO, CONH.sub.2, CONHR.sub.11, SO.sub.2 --(C.sub.1-6 -alkyl), SO.sub.2 -phenyl, wherein the phenyl ring may be mono- or polysubstituted by halogen, CF.sub.3, C.sub.1-4 -alkyl, OH, C.sub.1-4 -alkoxy;R.sub.10 denotes H or C.sub.1-6 -alkyl andR.sub.9 and R.sub.10 together may represent a C.sub.4-6 -alkylene group;R.sub.11 denotes C.sub.1-6 -alkyl, C.sub.5-7 -cycloalkyl, aryl, heteroaryl, aralkyl or heteroaryl-(C.sub.1-6 -alkyl), wherein the aryl or heteroaryl groups may be mono- or polysubstituted by Cl, F, CF.sub.3, C.sub.1-4 -alkyl, OH or C.sub.1-4 -alkoxy;Ar.sub.1 denotes an optionally mono- or polysubstituted aryl group, with the exception of the unsubstituted phenyl group and the phenyl group which is monosubstituted by halogen, C.sub.1-4 -alkyl or monosubstituted by C.sub.1-4 -alkoxy;Ar.sub.2 denotes an optionally mono- or polysubstituted aryl group, with the exception of an unsubstituted phenyl group;Ar.sub.3 denotes an optionally mono- or polysubstituted aryl groupwith the proviso thatR.sub.1 cannot represent an unsubstituted phenyl group bound via a C.sub.1-4 -alkylene unit;optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates and in the form of the free bases or the corresponding acid addition salts with pharmacologically acceptable acids.