Patent ID: 6545035
Filing Date: 2003-04-08
Classification: A61P,C07D

Abstract:
A compound of the formula wherein:X denotes an oxygen or sulphur atom, R1 denotes a hydrogen atom, a C1-4-alkoxy-carbonyl or C2-4-alkanoyl group, R2 denotes a carboxy or C1-4-alkoxy-carbonyl group or an aminocarbonyl group optionally substituted by one or two C1-3-alkyl groups, whilst the substituents may be identical or different, R3 denotes a hydrogen atom or a C1-6-alkyl group which may be substituted at the 2 position, in relation to the carbon atom of the R3-C(R4NR5)&boxH; group by a fluorine, chlorine or bromine atom, by a hydroxy, C1-3-alkoxy, C1-3-alkylsulphenyl, C1-3-alkylsulphinyl, C1-3-alkylsulphonyl, phenylsulphenyl, phenylsulphinyl, phenylsulphonyl, amino, C1-3-alkylamino, di-(C1-3-alkyl)-amino, C2-5-alkanoylamino or N-(C1-3-alkylamino)-C2-5-alkanoylamino group, R4 denotes a phenyl or naphthyl group which is substituted by a C2-3-alkoxy group which is substituted in the 2 or 3 position by a 5- membered cycloalkyleneimino group, by a carbonyl group which is substituted by a 5- membered cycloalkyleneimino group, by a C1-3-alkyl group which is substituted by a 5-membered cycloalkenyleneimino group or by a 4- to 5-membered cycloalkyleneimino group, wherein the abovementioned 5-membered cycloalkyleneimino groups may be substituted by one or two C1-3-alkyl groups, by a C5-7-cycloalkyl or phenyl group, by a C1-3-alkyl, C5-7-cycloalkyl, phenyl, carboxy or C1-4-alkoxy-carbonyl group and by a hydroxy group and in the abovementioned cycloalkyleneimino groups a methylene group adjacent to the nitrogen atom may be replaced by a carbonyl group, or by a C1-3-alkyl group which is substituted by a 5-membered cycloalkyleneimino group, whilst a phenyl group optionally mono- or disubstituted by fluorine, chlorine or bromine atoms or by methyl or methoxy groups, wherein the substituents may be identical or different, may be fused to the abovementioned 5-membered cycloalkyleneimino groups via two adjacent carbon atoms, whilst additionally the abovementioned monosubstituted phenyl groups may be substituted by a fluorine, chlorine or bromine atom or by a methyl, methoxy or nitro group, a 5-membered heteroaromatic group which contains an imino group, and R5 denotes a hydrogen atom or a C1-3-alkyl group whilst any carboxy, amino or imino groups present may be substituted by groups which can be cleaved in vivo, or a pharmaceutically acceptable salt thereof.