Novel derivates of boronic acid, process for their preparation and pharmaceutical compositions containing them

摘要

Boronic acid derivatives of formula (I), their isomers and their acid and base addition salts are new. R1, R2 = H or 1-6C alkyl; or CR1R2 = 3-8C cycloalkyl; R3 = H, 1-6C alkyl or phenyl or benzyl (both optionally substituted); R4 = heterocyclyl, amino, amidino, guanidino isothioureido iminomethylamino or mercapto (all optionally substituted); R5, R6 = H or 1-6C alkyl; or B(OR5)(OR6) = boronic ester of pinanediol; m = 0-6; n = 1-6; A1 = -CO-, -CS- or -SO2-; A = 5-10C bicycloalkyl-phenyl (optionally substituted) or -A2-N(R7)(R8), provided that m is not 0; A2 = -CO- or -CS-; R7, R8 = H, 1-6C alkyl (optionally substituted), 1-6C alkylsulphonyl, arylsulphonyl, aryl, heterocyclyl or 5-10C bicycloalkyl-phenyl (optionally substituted), indanyl or a group of formula (i) or (ii); Ra = 1-6C alkyl or phenyl (optionally substituted); Rb, Rc = H, halo, 1-6C alkyl, 1-6C alkoxy, hydroxy, optionally substituted amino or trihalomethyl.