Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-09-02
1996-03-05
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514411, 514419, 514459, 514461, 546164, 546283, 546268, 546275, 548440, 548441, 548444, 548467, 549419, 549475, A61K 3144, A61K 3140, A61K 3135
Patent
active
054968348
ABSTRACT:
The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.
The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.
REFERENCES:
Alves, R. J., et al., J. Carbohydrate Chemistry 10(6):1049-1057 (1991).
Can. J. of Chemistry, 60, 558 (1982).
Can. J. of Chemistry, 56, 119 (1978).
Tet. Lett., 30, 5421 (1989).
Chem. Pharm. Bull., 16, 1881 (1968).
Eur. J. Med. Chem. 12, 317 (1977).
Biochem. Biophys. Res. Comm., 49, 343 (1972).
JO 2304-085-A (May 18, 1989).
Fujisawa Yukio
Mizoguchi Junji
Oi Satoru
Sohda Takashi
Conlin David G.
Eisenstein Ronald I.
Ivy C. Warren
Owens Amelia
Takeda Chemical Industries Ltd.
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