4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin

Details 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin

1999-04-01

2000-03-07

Criares, Theodore J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

A61K 31395

Patent

active

060340770

ABSTRACT:
In accordance with the present invention, there are provided 4-substituted-3-(2-amino-2-cycloalkyl methyl)-acetamido azetidin-2-one derivatives of the formula: ##STR1## wherein n is 1, 2 or 3; in which R.sub.1, R.sub.2 and R.sub.3 are as defined herein, and salts thereof, which exhibit excellent cysteine proteinase inhibitory activity and which can be used for treatment of different diseases such as muscular dystrophy, myocardial infarction, bone resorption, arthritis, cancer metastasis, pulmonary emphysema, septic shock, cerebral ischemia, memory function, Alzheimer and cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections, and viral infections.

REFERENCES:
Bartholomew et al., "Peptide Aldehyde Inhibitors of Cathepsin K Inhibit Bone Resorption Both In Vitro and In Vivo", Journal of Bone and Mineral Research, vol. 12, No. 9, pp. 1396-1406 (1997).
Navab et al., "Inhibition of carcinoma cell invasion and liver metastases formation by the cysteine proteinase inhibitor E-64", Clinical & Experimental Metastasis, vol. 15, No. 2, pp. 121-129 (1997).
Millest et al., "Effects of an Inhibitor of Cathepsin L on Bone Resorption in Thyroparathyroidectomized and Ovariectomized Rats", Bone vol. 20, No. 5 May 1997:465-471.

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