PURPOSE: To obtain a compound useful for treating rheumatoid arthritis disease, having high inhibitory activity against extracellular matrix metal protease, low toxicity, excellent oral absorbability, long duration time, high stability and stability of medicine, shown by a specific formula.
CONSTITUTION: This compound of formula I [R1 is H or AR1a (A is a lower alkylene; R1a is H, amino, phthalimide, etc.); R2 is H or a lower alkyl; R3 is H, OH, a lower alkoxy (lower alkoxy), etc.; R4 is H, a halogen, OH, a lower alkoxy, etc.; R5 is H, benzoyl, etc.; R6 is a 1-12C alkyl, a lower alkoxy lower alkyl, etc.; (n) is 1 or 2], preferably 3S-[4-(N-hydroxyamino)-2R- isobutylsuccinyl]amino-1-methyl-6,7-methylenedioxy-3,4-dihydroxycarbostyril, etc. For example, preferably a carboxylic acid of formula II is reacted with an alkylhalocarboxylic acid to give a mixed acid anhydride, which is reacted with an amine of formula III.
IMAOKA TAKESHI
MOTOYAMA MASAAKI
YAMAMOTO SAKAHITO
TAKASU HIDEKI
