Alcohol or aldehyde derivatives and their use

Details Alcohol or aldehyde derivatives and their use Alcohol or aldehyde derivatives and their use

1995-06-27

1998-02-10

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514588, 514586, 514602, 514604, 514605, 514616, 548496, 564 28, 564 47, 564 59, 564 91, 564 98, 564 99, 564158, A61K 3140, C07D20920

Patent

active

057169802

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.

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J. Med. Chem., 33:11-13, Communications to the Editor (1989).
Fehrentz, et al., Synthesis p. 676 "Communications to the Editor" (1983).
Driguez et al., Canadian Journal of Chemistry, vol. 56, pp. 119-130 (1978).
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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. 523-528, 529-536, 537-541 (1978).
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