Derivatives of L-tryptophanal and their use as medicinals

Details Derivatives of L-tryptophanal and their use as medicinals Derivatives of L-tryptophanal and their use as medicinals

1994-02-04

1996-03-12

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D20914, A61K 3140

Patent

active

054987288

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:
Angliker, et al., "Inactivation of Calpain by Peptidyl Fluoromethyl Ketones", J. Med. Chem., vol. 35, No. 2, (1992), pp. 216-217.
J. Med. Chem. 33:11-13, Communications to the Editor (1989).
Fehrentz et al. Synthesis p. 676 "Communications to the Editor" (1983).
R. Thompson, Biochemistry, 12(1):47-51 (1973).
A. Ito, Biochemical and Biophysical Research Communications, 49(2):343-349 (1972).

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