2,3-methano-amino acid compounds for treating serine protease disorders

摘要

2,3 -methano-amino acid compounds of the formula shown, to a process for their preparation, to the pharmaceutical compositions containing them and their use as trypsin-related serine protease inhibitors. R1 represents a C3-8cycloalkyl group, an optionally substituted phenyl group or a linear or branched C1-6alkyl group optionally substituted by one or more identical or different groups selected from halogen, C3-8cycloalkyl and optionally substituted phenyl; R2 represents an amino group, an amidino group optionally substituted by one or more identical or different groups selected from linear or branched C1-6alkyl and hydroxy, a guanidino group optionally substituted by a linear or branched C1-6alkyl group, or an isothioureido group optionally substituted by a linear or branched C1-6alkyl group; Ar represents an aryl group or a monocyclic nitrogen-containing heteroaryl group; X1 represents a hydroxy group, an amino group or an -NHR3 group, R3 represents a propargyl group, an iminomethyl group, a linear or branched C1-6alkylsulphonyl group, a linear or branched arylC1-6alkylsulphonyl group, a -CONR'3R"3 group or a linear or branched C1-6alkyl group optionally substituted by a -CO2R'3 group, a -CONR'3R"3 group, a heterocyclic group, an aminosulphonyl group, an aryl group, or a heteroaryl group, * R'3 and R"3, which may be identical or different, each represents a hydrogen atom, or a linear or branched C1-6alkylsulphonyl group, an aryl group, a linear or branched C1-6alkyl group (optionally substituted by a carboxy group, a linear or branched C1-6alkoxycarbonyl group or a carbamoyl group) or form, with the nitrogen atom carrying them; a heterocyclic group;