Selective thrombin inhibitors

Details Selective thrombin inhibitors Selective thrombin inhibitors

1996-01-16

1998-05-05

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

514330, 514575, 514534, 514512, 514563, 514602, 514604, 514611, 514616, 546226, 558312, 562427, 562430, 562439, 562440, 562623, 564 81, 564 84, 564 91, 564140, 564150, 564157, A61K 3118, C07C31118

Patent

active

057475350

ABSTRACT:
The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,

REFERENCES:
patent: 4201863 (1980-05-01), Okamoto et al.
patent: 4258192 (1981-03-01), Okamoto et al.
Kikumoto, R., et al., Selective Inhibition of Thrombin by sulfony1-L-arginyl)!-2-piperidinecarboxylic Acid, Biochemistry 1984, vol. 23, pp. 85-90.
Banner, D., et al., Crystallographic Analysis at 3.0-A Resolution of the Binding to Human Thrombin of Four Active Site-directed Inhibitors*, The Journal of Biological Chemistry, 1991, vol. 266, No. 30, Oct. 25, pp. 20085-20093, 1991.
Hilpert, K. et al., Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors, J. Med. Chem, 1994, 37, 3889-3901.
Lottenberg, R. et al., Assay of Coagulation Proteases Using Peptide Chromogenic and Fluorogenic Substrates, vol. 80, pp. 341-361, 1981.
Hofsteenge, J. et al., Enzymatic Properties of Proteolytic Derivatives of Human .alpha.-Thrombin, Biochemistry 1988, vol. 27, pp. 2144-2151.
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