Alcohol or aldehyde derivatives as cathepsin L inhibitor and bone resorption inhibitor.

摘要

The present invention provides a cathepsin L inhibitor containing a compound of the formula: wherein R<1> is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R<2> and R<3> independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R<4> is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: -CHO or -CH2OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R<4> is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R<1> is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R<2> and R<3> independently are a lower alkyl or arylalkyl, X is -CHO, m is 1 and n is 0 or 1, or a salt thereof. Compound (I) is useful as a prophylactic/therapeutic agent for osteoporosis.