HETEROCYCLIC COMPOUNDS

摘要

Compounds of the formula I wherein A represents carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylcarbamoyl, N-hydroxycarbamoyl in free or protected form, N-(C1-C20)alkoxy-N-(C1-C20)alkylcarbamoyl, the radical -C(=N-OH)-NH2, the amidino radical -C(=NH)-NH2, the N-lower alkylamidino radical -C(=NH)-NH(lower alkyl), the radical -C(=NH)-O(lower alkyl), 1-(C1-C15-alkoxycarbonyl)-1-(lower alkoxy)-methoxycarbonyl, C3-C7-alkanoyl, 1-(N-hydroxyimino)-lower alkyl, 4,5-dihydro-2-(thia, oxa, imida)zolyl, 2-(thia, oxa)zolyl, 1-lower alkyl-4,5-dihydro-2-imidazolyl, imidazolyl, 1-acyl-imidazolyl, 2-benz(othia, oxa, imida)zolyl, 1-acyl-2-benzimidazolyl, 5-tetrazolyl in free or protected from; or A represents carboxy or a pharmaceutically acceptable ester group thereof provided that R2 is other than hydrogen, phenyl, nitro-phenyl, carboxy-phenyl and C1-C2-alkoxycarbonyl-phenyl; R1 represents carboxy or a pharmaceutically acceptable ester group thereof, and R2 represents hydrogen or a radical of the group comprising lower alkyl, cycloalkyl, aryl-lower alkyl, heteroaryl-lower alkyl and aryl each of which can be unsubstituted or substituted; and R3 represents hydrogen; or R2 and R3 together represent with the proviso that R2 is other than hydrogen, if - A represents N-hydroxycarbamoyl and R1 is methoxycarbonyl, or - A represents N-hydroxyiminomethyl and R1 is methoxycarbonyl or ethoxycarbonyl; or - A is 2-benzimidazolyl and R1 is ethoxycarbonyl; and with the proviso that R2 is other than phenyl, if -A is carbamoyl and R1 is methoxycarbonyl or ethoxycarbonyl; tautomers and salts thereof. Exhibit valuable pharmacological properties, especially as antifibrotic agents. They are prepared by methods known per se.