3-amino-2-oxo-1-piperidineacetic derivatives containing an argin

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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5142225, 5142372, 5142378, 514252, 514255, 514256, 514326, 514369, 514425, 544 8, 544129, 544162, 544309, 544310, 546208, 546209, 548184, 548185, 548544, A61K 31445, C07D40112

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active

057144990

ABSTRACT:
The present invention discloses peptide aldehydes which 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.

REFERENCES:
Skiles, J.W. et al, Biorg. Med. Chem. Lett. 1993, 3(4), pp. 773-778.
R. Freidinger, et al., "Protected Lactam-Bridged Dipeptides for Use as Conformational Constraints in Peptides," J. Org. Chem., 47:104-109, 1982.
H. Vieweg, et al., "Synthese von N-alpha-(arylsulphonylglycyl)-3-amidinophenulalaninest ern als aktive and relativ spezfische Inhibtoren von Faktor Xa," Pharmazie, vol. 42, No. 4, Apr. 1987, Berlin DD p. 268.
G. Wagner, et al., "Synthese von N-alpha-(Tosyl-beta-alanyl)-und N-alpha-(Tosyl-espsilon-aminocapronyl) amidinophenylalanylamiden als stark wirksame thrombininhititoren,"Pharmazie, vol. 39, No. 5, May 1984, Berlin DD pp. 315-317.
D. Carini, et al., "Nonpeptide Angiotensin II Receptor Antagoists:The Discovery of a Series of V-(Biphenylylmethyl) imidazoles as Potent, Orally Active Antihypertensives," J. Med. Chem., vol. 34, No. 8, pp. 2525-2547, 1991.

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