Pipecolinic acid derivatives, methods of manufacturing the same and therapeutic agents containing these compounds

摘要

A compound of formula (I) EMI ID=1.1 HE=24 WI=73 LX=742 LY=1077 TI=CF PCwherein:BR one of RSP1/SP and RSP2/SP is hydrogen, and the other is -RSP5/SP-RSP6/SP (wherein RSP5/SP is -O-, -NH-, -NHCO-, or -NHSOSB2/SB- and RSP6/SP is hydrogen, lower alkyl, indolyl, N-oxidepyridyl, phthalimide, thienyl, pyridyl, -Ph-RSP7/SP or -(CHSB2/SB)SBn/SB-O-Ph-RSP7/SP (wherein n = 1-6 and RSP7/SP is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or pyridyloxy)), or RSP1/SP and RSP2/SP together represent =O or N-ORSP9/SP (wherein RSP9/SP is hydrogen, lower alkyl, or benzyl);BR RSP3/SP is -COOH, -COOEt, -COOMe, -CHSB2/SB N(OH)CHO, or -CONHOH;BR RSP4/SP is lower alkyl, thienyl, -Ph-RSP8/SP (wherein RSP8/SP is hydroxyl, lower alkyl, lower alkoxy, nitro, halogen, pyridyloxy, unsubstituted phenyl group or phenyl group substituted with lower alkyl, lower alkoxy, hydroxy, or halogen),BR or a pharmaceutically acceptable salt thereof. The components have biological activity as inhibitors of Matrix Metalloproteinases (MMP) and find use against diseases such as rheumatoid and osteoarthritis, corneal ulceration, tumour growth, arteriosclerosis, restenosis and inflammatory bowel disease.