2,3-methano-amino acid derivatives, process for their preparation and pharmaceutical compositions containing them

摘要

2,3-methano amino acid derivatives (I), their isomers, their acid and base addition salts, their preparation, and pharmaceut compositions are new. The new compounds are of formula (I) n = 2 or 3; R1 = 3-8C cycloalkyl, phenyl (optionally substituted), 1-6c alkyl (optionally substituted by one or more halogens, 3-8C cycloalkyl, or phenyl, itself optionally substituted); R2 = amino, amidino (optionally substituted by one or more alkyl or OH groups), guanidino (optionally substituted by alkyl), or isothioureido (optionally substituted by 1-6C alkyl); Ar = aryl or nitrogen monocyclic heteroaryl; X1 = OH, amino, or -NHR3; R3 = propargyl, iminomethyl, 1-6C alkylsulfonyl, arylalkyl sulfonyl, -CONR'3R3 or 1-6C alkyl (optionally substituted by -COOR'3, -CONR'3R3, heterocycle, aminosulfonyl, aryl, or heteroaryl,; R'3 and R3 = H, 1-6C alkylsulfonyl, aryl, alkyl (optionally substituted by carboxy, alkoxycarbonyl, or carbamoyl), or together with the N atom they form a heterocycle.