3,4-Disubstituted azetidin-2-one derivatives useful as cysteine

Details 3,4-Disubstituted azetidin-2-one derivatives useful as cysteine 3,4-Disubstituted azetidin-2-one derivatives useful as cysteine

1997-09-22

1999-09-28

Tsang, Cecilia J.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548950, 514210, 540200, C07D20500

Patent

active

059591234

ABSTRACT:
The present invention is based on the discovery that certain 3,4-disubstituted-azetidin-2-one derivatives exhibit excellent cysteine proteinase inhibitory activity 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. In accordance to the present invention, there is provided a 3,4-disubstituted-azetidin-2-one derivatives of formula I, wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein, or a pharmaceutically acceptable salt thereof. ##STR1##

REFERENCES:
Monocyclic B-lactam antibiotics produced by bacteria, Sykes et al., vol. 291, Jun. 11, 1981, pp. 489-491 XP 002050350.
Synthesis and antibacterial activity of C4 substituted monobactams, Arnould et al., Eur. J. Med Chem (1992) 27, 131-140, XP 002050351.
4-Alkylated Monobactams- Chiral Synthesis and Antibacterial Activity, Cimarusti et al, vol. 39, No. 15. pp. 2577 to 2589, 1983 XP 002050352.

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