CARBOXAMIDE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES, PROCESSESFOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS

摘要

The invention relates to carboxamide-substituted benzimidazol derivatives of general formula (I), wherein R1 represents an optionally substituted residue from the group C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, phenyl-C1-C4-alkyl , heterocyclyl, heterocyclyl-C1-C4-alkyl; R2 represents -C(=NH)NH2, -CH2-NH2; R3 represents an optionally substituted residue from the group C1-C6 alkyl, C1- C6 hydroxyalkyl, C1-C4 alkoxy-C1-C4-alkyl, heterocyclyl, heterocyclyl-C1-C4- alkyl, heterocyclyl-C2-C4-alkenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl-C1-C4-alkyl, naphthyl-C1-C4-alkyl, and; R4 represents hydrogen and an optionally substituted C1-C6 alkyl, optionally provided in t he form of their tautomers, racemates, enantiomers, diastereomers, mixtures thereof and pharmacologically safe acid addition salts thereof. The inventio n also relates to methods for the producing said carboxamide-substituted benzimidazol derivatives and to their use as medicaments having a tryptase- inhibiting effect. The invention additionally relates to so-called prodrugs , wherein R2 represents C(=NR7)NH2 and intermediate products, wherein R2 represents -CN.