PURPOSE: To provide an alcohol or aldehyde derivative having selective inhibitory action on cathepsin, directly acting to the bones to suppress the bone resorption and useful for the prevention and treatment of osteoporosis.
CONSTITUTION: A compound of the formula I [R1 is H or arylalkyl, heterocyclic- alkyl or lower alkyl which may have substituent; R2 and R3 are H or (substituted) hydrocarbon residue; R4 is (substituted) alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl; X is CHO or CH2OB (B is H or hydroxyl-protecting group); m and n are 0 or 1], e.g. N-(1-naphthylsulfonyl)-(L)- isoleucyl-(L)-tryptophanal. Some of the compounds of the formula I can be produced by reacting a compound of the formula II [R4' is (substituted) alkanoyl, sulfonyl or carbonyloxy] or its reactive derivative with a compound of the formula III and optionally subjecting the reaction product to oxidation reaction or hydroxyl-protection reaction.
FUJISAWA YUKIO
YASUMA TSUNEO
MIZOGUCHI JUNJI
KORI MASAKI
TAKIZAWA MASAYUKI
