Arginine mimic derivatives as enzyme inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514316, 514318, 514326, 514423, 546133, 546191, 546193, 546208, 546210, 548538, A61K 31435, A61K 31445, C07D40112, C07D45302

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active

058831070

ABSTRACT:
The present invention provides peptide aldehydes having an azetidinyl, prolyl or pipecolyl group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described.

REFERENCES:
patent: 5492895 (1996-02-01), Vlasuk et al.
Banner, D.A. et al, Perspect. Med. Chem. 1993, pp. 27-43.
G. Wagner et al., Pharmazie, 39:5 pp. 315-317 (May 1984).

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