Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-04-11
2008-08-26
Shameem, Golam M. M. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S470000
Reexamination Certificate
active
07417063
ABSTRACT:
The present invention provides compounds of Formula (I):or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, X5, R4, and W are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
REFERENCES:
patent: 4581354 (1986-04-01), Bell
patent: 4634776 (1987-01-01), Bell
patent: 4885295 (1989-12-01), Bell
patent: 4978664 (1990-12-01), Bell
patent: 5013732 (1991-05-01), Bell
patent: 5312829 (1994-05-01), Okada et al.
patent: 5604253 (1997-02-01), Lau et al.
patent: 5639780 (1997-06-01), Lau et al.
patent: 5684034 (1997-11-01), Bach et al.
patent: 5811425 (1998-09-01), Woods et al.
patent: 6069156 (2000-05-01), Oku et al.
patent: 6100238 (2000-08-01), Gyorkos et al.
patent: 6166023 (2000-12-01), Schindler et al.
patent: 6358992 (2002-03-01), Pamukcu et al.
patent: 6653304 (2003-11-01), Leftheris et al.
patent: 6858577 (2005-02-01), Zhang et al.
patent: 2003/0203909 (2003-10-01), Ushio et al.
patent: 2004/0006123 (2004-01-01), Alkan et al.
patent: 2004/0220206 (2004-11-01), Smallheer et al.
patent: 2004/0235847 (2004-11-01), Quan et al.
patent: WO 93/02050 (1993-02-01), None
patent: WO 98/08818 (1998-03-01), None
patent: WO 99/12903 (1999-03-01), None
patent: WO 99/12935 (1999-03-01), None
patent: WO 99/43654 (1999-09-01), None
patent: WO 00/35886 (2000-06-01), None
patent: WO 01/27079 (2001-04-01), None
patent: WO01058869 (2001-08-01), None
patent: WO 03/101961 (2003-12-01), None
patent: WO 2004/050637 (2004-06-01), None
patent: WO 2004/062661 (2004-07-01), None
patent: WO 2004/080971 (2004-09-01), None
patent: WO 2004/094372 (2004-11-01), None
Walsh, P.N., “Platelets and Factor XI Bypass the Contact System of Blood Coagulation”,Thromb. and Haemostasis, 82(2), pp. 234-242, 1999.
Colman, R. Contact Activation Pathway: Inflammatory, Fibrinolytic, Anticoagulant, Antiadhesive, and Antiangiogenic Activities,Hemostasis and thrombosis: basic principles and clinical practice, Lippincott Williams & .Wilkins, 2001, pp. 103-122.
Schmaier, A.H., “Contact Activation”,Thrombosis and Hemorrhage, Williams&Wilkins, 1998, Chapter 5, pp. 105-128.
Gailani, D., “Activation of Factor IX by Factor XIa”,Trends in Cardiovascular Medicine, vol. 10, No. 5, 2000, pp. 198-204.
Bouma, B.N. et al., “Thrombin-Activatable Fibrinolysis Inhibitor (TAFI, Plasma Procarboxypeptidase B, Precarboxypeptidase R, Procarboxypeptidase U)”,Thrombosis. Research, 2001, 101, pp. 329-354.
Gailani, D., “Gene Targeting in Hemostasis. Factor XI”,Frontiers in Bioscience, 2001, 6, pp. d201-d207.
Gailani, D., et al., “A murine model of factor XI deficiency”,Blood Coagulation and Fibrinolysis, 1997, vol. 8, pp. 134-144.
Minnema, M.C., et al., “Activation of Clotting Factors XI and IX in Patients with Acute Myocardial Infarction”,Arterioscler. Thromb. Vasc. Biol., 2000, 20, pp. 2489-2493.
Murakami, T., et al., “Evaluation of Factor XIa-α1—Antitrypsin in Plasma, a Contact Phase-Activated Coagulation Factor-Inhibitor Complex, in Patients With Coronary Artery Disease”,Arterioscler. Thromb. Vasc. Biol., 1995, vol. 15, No. 8, pp. 1107-1113.
Meijers, J.C.M., et al., “High Levels of Coagulation Factor XI as a Risk Factor for Venous Thrombosis”,N. Engl. J. Med., 2000, vol. 342, No. 10, pp. 696-701.
Komoriya et al., “Design, synthesis and biological activity of amidinobicyclic compounds (derivatives of DX-9065a) as factor Xa inhibitors: SAR study of S1 and aryl binding sites”,Bioorganic&Medicinal Chemistry, vol. 12, pp. 2099-2114, 2004.
Zhang et al., “A Versatile Synthesis of 3-Substituted Indolines and Indoles”,J. Org. Chem., vol. 61, pp. 2594-2595, 1996.
Woods et al., “Thiazole Analogues of the NSAID Indomethacin as Selective COX-2 Inhibitors”,Bioorganic&Medicinal Chemistry Letters, vol. 11, pp. 1325-1328, 2001.
Jacobs, R. T. et al., “Substituted 3-(Phenylmethyl)-1H-indole-5-carboxamides and 1-(Phenylmethyl)indole-6-carboxamides as Potent, Selective, Orally Active Antagonists of the Peptidoleukotrienes”, J. Med. Chem., vol. 36, No. 3, pp. 394-409 (1993).
Corte James R.
Smallheer Joanne M.
Bristol--Myers Squibb Company
Chung Susannah
Shameem Golam M. M.
Sun Jing G.
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