Substituted biaryl compounds as factor XIa inhibitors

Details Substituted biaryl compounds as factor XIa inhibitors Substituted biaryl compounds as factor XIa inhibitors

2006-01-12

2008-12-02

Saeed, Kamal (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S361100, C546S152000, C546S165000, C544S237000, C544S283000, C514S379000, C514S403000, C514S311000, C514S248000, C514S266100

Reexamination Certificate

active

07459564

ABSTRACT:
The present invention provides compounds of Formula (I):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B 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: 6645939 (2003-11-01), Durette et al.
patent: 2004/0106621 (2004-06-01), Wu et al.
patent: 2004/0138268 (2004-07-01), Boy et al.
patent: 2004/0220206 (2004-11-01), Smallheer et al.
patent: 2004/0235847 (2004-11-01), Quan et al.
patent: 2005/0228000 (2005-10-01), Smallheer et al.
patent: 2005/0282805 (2005-12-01), Hangeland et al.
patent: 2006/0009455 (2006-01-01), Corte et al.
patent: 1258473 (2002-11-01), None
patent: 1314719 (2003-05-01), None
patent: WO00/39115 (2000-07-01), None
patent: WO 01/27079 (2001-04-01), None
patent: WO 01/49288 (2001-07-01), None
patent: WO02/76929 (2002-03-01), None
patent: WO2004/047738 (2004-06-01), None
patent: WO2004/060281 (2004-07-01), None
Deng et al., Bioorg. Med Chem Lett, 16, 2006, 3049-3054.
Arendsen et al., caplus an 1997:41540.
Bouma, B.N. et al., “Thrombin-Activatable Fibrinolysis Inhibitor (TAFI, Plasma Procarboxypeptidase B, Procarboxypeptidase R, Procarboxypeptidase U”, Thrombosis Research, vol. 101, pp. 329-354 (2001).
Colman, R.W., Chapter 6: “Contact Activation Pathway: Inflammatory, Fibrinolytic, Anticoagulant, Antiadhesive, and Antiangiogenic Activities”, Hemostasis and Thrombosis: Basic Principles and Clinical Practice, 4thEd., Lippincott Williams & Wilkins, publ., Colman, R.W. et al., eds., pp. 103-121 (2001).
Gailani, D., “Activation of Factor IX by Factor XIa”, Trends Cardiovasc. Med., vol. 10, No. 5, pp. 198-204 (2000).
Gailani, D., “Gene Targeting in Hemostasis. Factor XI”, Frontiers in Bioscience, vol. 6, pp. d201-207 (2001).
Gailani, D. et al., “A murine model of factor XI deficiency”, Blood Coagulation and Fibrinolysis, vol. 8, pp. 134-144 (1997).
Goodnight, S.H. et al., Chapter 4: “Screening Tests of Hemostasis”, Disorders of Hemostasis and Thrombosis: A Clinical Guide, The McGraw-Hill Companies, publ., pp. 41-51 (2001).
Meijers, J.C.M. et al., “High Levels of Coagulation Factor XI as a Risk Factor for Venous Thrombosis”, The New England Journal of Medicine, vol. 342, No. 10, pp. 696-701 (2000).
Minnema, M.C. et al., “Activation of Clotting Factors XI and IX in Patients With Acute Myocardial Infarction”, Arteriorscler. Thromb. Vasc. Biol., vol. 20, pp. 2489-2493 (2000).
Schmaier, A.H., Chapter 5: “Contact Activation”, Hemostasis and Thrombosis: Basic Principles and Clinical Practice, 4thEd., Lippincott Williams & Wilkins, publ., Colman, R.W. et al., eds., pp. 105-127 (2001).
Walsh, P.N., “Platelets and Factor XI Bypass the Contact System of Blood Coagulation”, Thrombosis and Haemostasis, vol. 82, No. 2, pp. 234-242 (1999).
Yong-Jin Wu et al., “Synthesis and Structure-Activity Relationship of Acrylamides as KCNQ2 Potassium Channel Openers”,J. Med. Chem., vol. 47, No. 11, pp. 2887-2896.
U.S. Appl. No. 11/610,027, Pinto et al.

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