New N-sulfonylated pipecolic acid derivatives, are matrix metalloprotease inhibitors useful e.g. for treating rheumatism, tumor progression, arteriosclerosis or inflammatory bowel disease

摘要

4-Substituted N-sulfonylated pipecolic acid derivatives (I) are new. Pipecolic acid derivatives of formula (I) and their salts are new. R1 + R2 = =O or =NOR9; or one of R1, R2 = H and the other = -R5-R6; R9 = H, alkyl or benzyl; R5 = O, NH, NHCO or NHSO2; R6 = H, alkyl, Ph', -(CH2)n-OPh', indolyl, N-oxido-pyridyl, phthalimido, thienyl or pyridyl; n = 1-6; Ph' = phenyl (optionally substituted by OH, alkyl, alkoxy, halo, NO2 or pyridyloxy); R3 = COOH, COOEt, COOMe, CH2N(OH)(CHO) or CONHOH; R4 = alkyl or thienyl; or phenyl substituted by OH, alkyl, alkoxy, NO2, halo, pyridyloxy or phenyl (itself optionally monosubstituted by alkyl, alkoxy, OH or halo); all alkyl moieties are 'lower', i.e. have 1-6C. An Independent claim is included for the preparation of (I).