To obtain the subject new compound having matrix-metalloproteinase inhibiting activity and orally administratable.
This is a compound of formula I {R1 is OH, NHOH, etc.; R2 is a group of formula II [(n) is an integer of 2-4], etc.; A is a group of formula III (B is H, an allyl, etc.; R3 is NHCH3, NHtBu, etc.)} or its pharmaceutically permissible salt, e.g. N-[(2R)-2-(1'-carboxymethyl)-3-(azulen-1-yl)propionyl]-6- phenylalanine-N-methylamide. In order to obtain a compound of formula I whose R1 is OH, a compound of formula IV (R4 is an alkyl) is made to react with a compound of the formula HACOR3, and the reaction product is subjected to hydrolysis. This product can be orally administered for the treatment and/or prophylaxis of a disease attributable to the damage of extracellular matrixes caused by matrix-metalloproteinase.
TOMIYAMA ITARU
YANAGISAWA TAKASHI
NODA ATSUSHI
KOBAYASHI YOSHINORI
