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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514425, 548537, 548538, A61K 3140, C07D20708, C07D20709

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active

057983771

ABSTRACT:
A compound which inhibits human thrombin and where has the structure ##STR1## such as ##STR2##

REFERENCES:
patent: 2277409 (1942-03-01), Murray
patent: 4346078 (1982-08-01), Bajusz et al.
patent: 4703036 (1987-10-01), Bajusz et al.
patent: 5252566 (1993-10-01), Shuman et al.
patent: 5332726 (1994-07-01), Klein et al.
patent: 5380713 (1995-01-01), Balasubramanian et al.
patent: 5416093 (1995-05-01), Shuman et al.
patent: 5510369 (1996-04-01), Lumma et al.
Hussain et al., Peptides, "Anticoagulant Activity of a Peptide Boronic Acid Thrombin Inhibitor by Various Routes of Administration in Rats", vol. 12, pp. 1153-1154 (1991).
Vencill et al., Chemical Abstracts, vol. 103, Abstract No. 18900 (1986).
Banner et al., Perspect. Med. Chem., "Chapter 3 --Serine Proteases: 3D Structures, Mechanisms of Action and Inhibitors", pp. 29-43 (1993).
Tapparelli et al., Tips, "Synthetic low-molecular weight thrombin inhibitors: molecular design and pharmacological profile", vol. 14, pp. 366-376, (1993).
Bajusz et al., J. Med. Chem., "Highly Active and Selective Anticoagulants: D-Phe-Pro-Arg-H, a Free Tripeptide Aldehyde Prone to Spontaneous Inactivation and Its Stable N-Methyl Derivative, D-Mephe-Pro-Arg-H", vol. 33, pp. 1729-1735 (1990).
Edwards et al., J. AM. Chem. Soc., "Design, Synthesis, and Kinetic Evaluation of a Unique Class of Elastase Inhibitors, the Peptidyl . . . ", vol. 114, pp. 1854-1863 (1992).
Berndt, M.C. and David R. Phillips, Department of Biochemistry, St. Jude Children's Research Hospital, "Chapter 3 --Platelet membrane proteins: composition and receptor function", pp. 43-75 (1981).
Martin et al., Biochemistry, "Platelet Stimulation by Thrombin and Other Proteases", vol. 14, No. 6, pp. 1308-1314 (1975).
Greco et al., Blood, PPACK-Thrombin Inhibits Thrombin-Induced Platelet Aggregation and Cytoplasmic Acidification but Does Not Inhibit Platelet Shape Change, vol. 75, No. 10, pp. 1983-1990 (1990).
Bode et al., The Embo Journal, "The refined 1.9 .ANG. crystal structure of human a-thrombin: interation with D-Phe-Pro-Arg chloromethylketone and significance of the . . . ", vol. 8, No. 11, pp. 3467-3475 (1989).
Workman et al., The Journal of Biological Chemistry "Structure-Function Relationships in the Interaction of a-Thrombin with Blood Platelets", vol. 252, No. 20, pp. 7118-7123 (1992).
Hui et al., Biochemical and Biophysical Research Communications, "Minimal Sequence Requirement of Thrombin Receptor Agonist Peptide", vol. 184, No. 2, pp. 790-796 (1992).
Scarborough et al., The Journal of Biological Chemistry, "Tethered Ligand Agonist Peptides Structural Requirements for Thrombin Receptor . . . ", vol. 267, No. 19, pp. 13146-13149 (1992).
Vassallo et al., The Journal of Biological Chemistry, "Structure-Function Relationships in the Activation of Platelet Thrombin Receptors by Receptor-derived Peptides", vol. 267, No. 9, pp. 6081-6085 (1992).
Iwanowicz et al., Organic & Medicinal Chemistry Letters, "a-Hydroxy-and a-Ketoester Functionalized Thrombin Inhibitors", vol. 2, No. 12, pp. 1607-1612 (1992).
Okumura et al., The Journal of Biological Chemistry, "Platelet Glycocalicin-Interaction with Thrombin and Role as Thrombin Receptor of the Platelet Surface", vol. 263, No. 10, pp. 3435-3443 (1978).
Tollefsen et al., The Journal of Biological Chemistry, "The Binding of Thrombin to the Surface of Human Platelets", vol. 249, No. 8, pp. 2646-2651 (1974).
Vu et al., Cell, "Molecular Cloning of a Functional Thrombin Receptor Reveals a Novel Proteolytic Mechanism of Receptor Activation", vol. 64, pp. 1057-1068 (1991).
Gronke et al., The Journal of Biological Chemistry, "Thrombin Interaction with Platelets-Influence of Platelet Protease Nexin", vol. 262, No. 7, pp. 3030-3036 (1987).
Phillips, D. R., Thrombos. Diathes. Haemorrh. (STUTTG.), "Thrombin Interaction with Human Platelets Potentiation of Thrombin-induced Aggregation and Release by Inactivated Thrombin", vol. 32, p. 207 (1974).
Balasubramanian et al., J. Med. Chem., "Active Site-Directed Synthetic Thrombin Inhibitors: Synthesis, in Vitro and in Vivo Activity Profile of BMY 44621 and . . . ", vol. 36, pp. 300-303 (1993).
Kettner et al., The Journal of Biological Chemistry, "The Selective Inhibition of Thrombin by Peptides of Boroarginine", vol. 265, No. 30, pp. 18289-18297 (1990).
Shuman et al., J. Med. Chem., "Highly Selective Tripeptide Thrombin Inhibitors", vol. 36, pp. 314-319 (1993).

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