Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2006-12-13
2009-12-01
Saeed, Kamal A (Department: 1626)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
C548S343100, C548S343500, C548S311100
Reexamination Certificate
active
07626039
ABSTRACT:
The present invention provides compounds of Formula (I):or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11are as defined herein. The compounds of Formula (I) are 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 or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
REFERENCES:
patent: 6852725 (2005-02-01), Thurieau et al.
patent: 7129264 (2006-10-01), Smallheer et al.
patent: 7138412 (2006-11-01), Quan et al.
patent: 7417063 (2008-08-01), Smallheer et al.
patent: 7429604 (2008-09-01), Corte et al.
patent: 7453002 (2008-11-01), Hangeland et al.
patent: 7459564 (2008-12-01), Corte et al.
patent: 2004/0132788 (2004-07-01), Chabrier De Lassauniere et al.
patent: 2004/0180855 (2004-09-01), Schumacher et al.
patent: 2004/0186151 (2004-09-01), Mjalli et al.
patent: 2004/0220206 (2004-11-01), Smallheer et al.
patent: 2004/0235847 (2004-11-01), Quan et al.
patent: 2005/0203143 (2005-09-01), Breslin et al.
patent: 2005/0228000 (2005-10-01), Smallheer et al.
patent: 2005/0282805 (2005-12-01), Hangeland et al.
patent: 2006/0004013 (2006-01-01), Kimura et al.
patent: 2006/0009455 (2006-01-01), Corte et al.
patent: 2006/0154915 (2006-07-01), Corte et al.
patent: WO98/27108 (1997-11-01), None
patent: WO98/57951 (1998-12-01), None
patent: WO99/64401 (1999-12-01), None
patent: WO99/65942 (1999-12-01), None
patent: WO01/02387 (2001-01-01), None
patent: WO01/27079 (2001-04-01), None
patent: WO02/10140 (2002-02-01), None
patent: WO2003/064440 (2003-08-01), None
patent: WO2004/071448 (2004-08-01), None
patent: WO 2004/071448 (2004-08-01), None
patent: WO2005/082895 (2005-09-01), None
patent: WO2006/061638 (2006-06-01), None
patent: WO2007/070816 (2007-06-01), None
patent: WO2007/070818 (2007-06-01), None
Vippagunta et al, “Crystalline Solids”, Advanced Drug Delivery Reviews, vol. 48, pp. 3-26 (2001).
Gavezzotti, “Are Crystal Structures Predictable?”, Accounts of Chemical Research, vol. 27, pp. 309-314 (1994).
U.S. Appl. No. 12/266,659, filed Nov. 7, 2008, James R. Corte.
U.S. Appl. No. 12/097,068, filed Jun. 12, 2008, Wei Han.
U.S. Appl. No. 12/097,080, filed Jun. 12, 2008, James R. Corte.
U.S. Appl. No. 12/097,068, filed Dec. 13, 2006, Wei Han.
U.S. Appl. No. 12/097,080, filed Dec. 13, 2006, James R. Corte.
Walsh, P.N.,Platelets and Factor XI Bypass the Contact System of Blood Coagulation, Thromb. Haemostasis, 1999, vol. 82, pp. 234.242.
Coleman, R.,Contact Activation Pathway, Hemostasis and Thrombosis, pp. 103-122, 2001.
Schmaier A.H.,Contact Activation, Thrombosis and Hemorrhage, pp. 105-128, 1998.
Galiani, D.Activation of Factor IX by Factor XIa, Trends Cardiovasc. Med., vol. 10, No. 5, pp. 198-204, 2000.
Bouma, B.N. et al.,Thrombin-Activatable Fibrinolysis Inhibitor, Thromb. Res. 2001, vol. 101, 329-354.
Gailani D.,Gene Targeting in Hemostasis, Factor XI, Frontiers in Bioscience, 2001, vol. 6, 201-207.
Gailani, D. et al.,A murine model of factor XI deficiency, Blood Coagulation and Fibrinolysis, 1997, vol. 8, 134-144.
Minnema, M.C. et al.,Activation of Clotting Factors XI and IX in Patients with Acute Myocardial Infarction, Arterioscler. Throb. Vasc. Biol., 2000, vol. 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, 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, pp. 696-701.
Hirsh, J. et al.,New anticoagulants, Blood, Jan. 15, 2005, vol. 105, No. 2. pp. 453-463.
Hoffman, M.,A cell-based model of coagulation and the role of factor VIIal, Blood Reviews (2003), 17, 51-55.
Shariat-Madar et al.,Blood, Jul. 1, 2006, vol. 108, No. 1, pp. 192-199.
Renne, T. et al.,Defective thrombus formation in mice lacking coagulation factorXII, J. Exp. Medicine 2005, vol. 202, pp. 271-281.
Kleinschnitz et al.,Targeting coagulation factor XII provides protection from pathological thrombosis in cerebral ischemia without interfering with hemostasis, J. Expl. Medicine, 2006, vol. 203, 513-518.
Chan et al.,The Characterization of Mice with a Targeted Combined Deficiency of Protein C and Factor XI, Amer. J. Pathology 2001, vol. 158, pp. 469-479.
Gruber et al.,Factor XI-dependence of surface- and tissue factor-initiated thrombus propagation in primates, Blood 2003, vol. 102, pp. 953-955.
Rosen et al.,FXI is Essential for Thrombus Formation Following FeCI3-induced Injury of the Carotid Artery in the Mouse, Thromb. Haemost 2002; 87; 774-776.
Wang et al.,Effects of factor IX or factor XI deficiency on ferric chloride-induced carotid artery occlusion in mice, Journal of Thrombosis and Haemostasis, 3: 695-702, (2005).
Cavallaro Cullen L.
Corte James R.
Gilligan Paul J.
Hu Zilun
Pinto Donald J. P.
Bristol--Myers Squibb Company
Rodriguez-Garcia Valerie
Saeed Kamal A
Sun Jing G.
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