Patent ID: 6300342
Filing Date: 2001-10-09
Classification: A61P,C07D

Abstract:
A compound of the formula I ##STR17##wherein:R.sub.a is a hydrogen atom, a carboxy, C.sub.1-3 -alkoxycarbonyl, benzoyl, phenylsulphonyl, nitro, R.sub.1 NR.sub.2, R.sub.1 NR.sub.2 --X--, or (R.sub.3 X)NR.sub.1 -- group, wherein:R.sub.1 is a hydrogen atom, a C.sub.1-5 -alkyl group optionally substituted by a phenyl, carboxy, C.sub.1-4 -alkoxycarbonyl, or aminocarbonyl group, wherein the amino group of the aminocarbonyl group is optionally additionally mono- or disubstituted by C.sub.1-4 -alkyl, phenyl-C.sub.1-3 -alkyl, phenyl, carboxy-C.sub.1-3 -alkyl-, or C.sub.1-3 -alkoxycarbonyl-C.sub.1-3 -alkyl groups wherein the substituents are identical or different, or a straight-chained C.sub.2-3 -alkyl group terminally substituted by an amino, C.sub.1-3 -alkylamino, di-(C.sub.1-3 -alkyl)amino, C.sub.1-4 -alkanoylamino, phenylamino, N-benzyloxycarbonyl-phenylamino, pyrrolidino, piperidino, or morpholino group,R.sub.2 is a hydrogen atom, a C.sub.1-3 -alkyl group optionally substituted by one or two phenyl groups or by a naphthyl group, or a phenyl group optionally substituted by a fluorine, chlorine, or bromine atom or by a straight-chained C.sub.2-3 -alkyl group terminally substituted by an amino, C.sub.1-3 -alkylamino, C.sub.1-3 -alkanoylamino, di-(C.sub.1-3 -alkyl)amino, pyrrolidino, piperidino, or morpholino group, orR.sub.1 and R.sub.2 together with the nitrogen atom between them are a pyrrolidino or piperidino group optionally substituted by a C.sub.1-3 -alkyl, carboxy, or C.sub.1-3 -alkoxycarbonyl group, a pyrrolidino or piperidino group substituted by two C.sub.1-3 -alkyl groups, or a morpholino group,R.sub.3 is a straight-chained or branched C.sub.1-7 -alkyl group optionally substituted in the 1, 2, or 3 position by a phenyl group or in the 2 to 7 position by a fluorine, chlorine, or bromine atom, by a carboxy, or C.sub.1-3 -alkoxycarbonyl group, a trifluoromethyl group, a phenyl, naphthyl, or chromanyl group optionally substituted in each case by a fluorine, chlorine, or bromine atom, by a trifluoromethyl, C.sub.1-3 -alkyl, C.sub.1-3 -alkoxy, amino, C.sub.1-3 -alkylamino, di-(C.sub.1-3 -alkyl)amino, or aminocarbonyl group, wherein the abovementioned phenyl, naphthyl, or chromanyl groups are optionally additionally substituted by one to three methyl groups, a phenyl or aminophenyl group substituted by two chlorine or bromine atoms, a thienyl group optionally substituted by a chlorine or bromine atom or by a methyl group, a C.sub.3-8 -cycloalkyl, C.sub.8-12 -bicycloalkanone, quinolyl, isoquinolyl, or benzimidazolyl group, orR.sub.1 and R.sub.3 together are an n-alkylene group with 3 to 5 carbon atoms, wherein an ethylene group linked to the SO.sub.2 -- or CO-- group is optionally replaced by a 1,2-phenylene group, andX is a carbonyl or sulphonyl group, orR.sub.a is a C.sub.2-3 -alkanoyl group substituted in the alkyl moiety by a carboxy-C.sub.1-3 -alkyl or C.sub.1-3 -alkoxycarbonyl-C.sub.1-3 -alkyl group and a benzoyl, naphthoyl, phenylsulphonyl, or naphthylsulphonyl group;R.sub.b is an amidino group optionally substituted by a C.sub.1-10 -alkoxycarbonyl or phenyl-C.sub.1-3 -alkoxycarbonyl group, or a cyano or aminomethyl group,R.sub.c and R.sub.d, which are identical or different, are each a hydrogen, fluorine, chlorine, bromine, or iodine atom, a methyl, methoxy, nitro, amino, or aminocarbonyl group, or an amino group optionally substituted by a straight-chained C.sub.2-4 -alkanoyl group, wherein the alkanoyl moiety is optionally terminally substituted by a carboxy or C.sub.1-3 -alkoxycarbonyl group,A is an n-propylene group optionally substituted by one or two C.sub.1-3 -alkyl groups, wherein in the n-propylene group of A,a methylene group, if linked to the nitrogen atom, is optionally replaced by a carbonyl group, ora methylene group, if linked to the phenyl nucleus, is optionally replaced by an oxygen or sulfur atom, by a sulphinyl or sulphonyl group, or by an imino group optionally substituted by a C.sub.1-3 -alkyl group,B is a bond, or a methylene, ethylene, ethenylene or n-propylene group optionally substituted by one or two C.sub.1-3 -alkyl groups, whereinin the methylene, ethylene, or n-propylene group of B, if Y is a carbonyl or thiocarbonyl group, a methylene group is optionally replaced by an oxygen atom or by an imino group optionally substituted by a C.sub.1-3 -alkyl group, orin the ethylene or n-propylene group of B, if Y is a methylene group, a methylene group in the 3 or 4 position relative to the nitrogen atom is optionally replaced by an oxygen atom or by an imino group optionally substituted by a C.sub.1-3 -alkyl group;W is a methane group or a nitrogen atom; andY is a methylene, carbonyl; or thiocarbonyl group,or a tautomer or a pharmaceutically acceptable salt thereof.