Alcohol or aldehyde derivatives and their use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514414, 514394, 548496, 548510, 5483051, A61K 3140, C07D20908

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active

056397810

ABSTRACT:
The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (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.sup.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.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.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.

REFERENCES:
Driguez et al., Canadian Journal of Chemistry, vol. 56, pp. 119-130 (1978).
Towatari et al., FEBS Letters, vol. 280, No. 2, pp. 311-315 (1991).
Aoyagi et al., The Journal of Antibiotics, vol. 22, No. 6, pp. 283-286 (1969).
Hanada et al., Agricultural and Biological Chemistry, vol. 42, No. 3, pp. 523-541 (1978).
Murata et al., FEBS Letters, vol. 280, No. 2, pp. 307-310 (1991).

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