Selective thrombin 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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544383, 544387, 544388, 544391, A61K 31495, C07D24104

Patent

active

059771143

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.
patent: 5518735 (1996-05-01), Sturzebecher et al.
Kikumoto, R. et al., Selective Inhibition of Thrombin by (2R, 4R)-4-Methyl-1-[N.sup.2 -(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl) sulfonyl]-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 of 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.
Stuerzebecker et al., Chemical Abstract, vol. 123 (1995) 275199.
Stuerzebecker et al., Chemical Abstract, vol. 118 (1993) 7392.
Stuerzebecker et al., Chemical Abstracts, vol. 107 (1987) 97532.
Wagner et al., Chemical Abstracts, vol. 100 (1984) 210409.
Stuerzebecker et al., Chemical Abstract, vol. 99 (1983) 18600.
Stuerzebecker et al., Chemical Abstract, vol. 96 (1982) 173930.
Stuerzebecker et al., Chemical Abstract, vol. 96 (1982) 48156.
Wagner et al., Chemical Abstracts, vol. 96, abstract 104709.

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