Discovery and characterization of a potent and selective non-amidine inhibitor of human factor Xa.

[1]  D. Davey,et al.  Structure-activity relationships of substituted benzothiophene-anthranilamide factor Xa inhibitors. , 2003, Bioorganic & medicinal chemistry letters.

[2]  H. Kurihara,et al.  The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor. , 2002, Bioorganic & medicinal chemistry.

[3]  D. Abendschein,et al.  Human in vitro pharmacodynamic profile of the selective Factor Xa inhibitor ZK-807834 (CI-1031). , 2002, Thrombosis research.

[4]  P. Sprengeler,et al.  Neutral inhibitors of the serine protease factor Xa. , 2001, Bioorganic & medicinal chemistry letters.

[5]  D. Abendschein,et al.  A novel synthetic inhibitor of factor Xa decreases early reocclusion and improves 24-h patency after coronary fibrinolysis in dogs. , 2001, The Journal of pharmacology and experimental therapeutics.

[6]  P. Lam,et al.  Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa. , 2001, Journal of medicinal chemistry.

[7]  C. Dominguez,et al.  Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors. , 2000, Journal of medicinal chemistry.

[8]  D. R. Holland,et al.  Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors. , 2000, Journal of medicinal chemistry.

[9]  Sung-Hou Kim,et al.  Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa. , 2000, Biochemistry.

[10]  A. Spada,et al.  Crystal structures of human factor Xa complexed with potent inhibitors. , 2000, Journal of medicinal chemistry.

[11]  C. Dunwiddie,et al.  In vitro characterization of a novel factor Xa inhibitor, RPR 130737. , 2000, Thrombosis research.

[12]  H. Demuth,et al.  Thioxo amino acid pyrrolidides and thiazolidides: new inhibitors of proline specific peptidases. , 2000, Biochimica et biophysica acta.

[13]  J. T. Metz,et al.  Non-amidine-containing 1,2-dibenzamidobenzene inhibitors of human factor Xa with potent anticoagulant and antithrombotic activity. , 2000, Journal of medicinal chemistry.

[14]  D. Abendschein,et al.  Effects of ZK-807834, a novel inhibitor of factor Xa, on arterial and venous thrombosis in rabbits. , 2000, Journal of cardiovascular pharmacology.

[15]  B. Zhu,et al.  Antithrombotic and hemostatic capacity of factor Xa versus thrombin inhibitors in models of venous and arteriovenous thrombosis. , 2000, European journal of pharmacology.

[16]  J. A. Kyle,et al.  1,2-Dibenzamidobenzene inhibitors of human factor Xa. , 2000, Journal of medicinal chemistry.

[17]  R. Bentley,et al.  Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis. , 2000, European journal of pharmacology.

[18]  J. A. Kyle,et al.  Structure-based design of potent, amidine-derived inhibitors of factor Xa: evaluation of selectivity, anticoagulant activity, and antithrombotic activity. , 2000, Journal of Medicinal Chemistry.

[19]  J. A. Kyle,et al.  N(2)-Aroylanthranilamide inhibitors of human factor Xa. , 2000, Journal of medicinal chemistry.

[20]  C. Dunwiddie,et al.  Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA. , 1999, Bioorganic & medicinal chemistry letters.

[21]  J R Pruitt,et al.  Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 1. , 1999, Journal of medicinal chemistry.

[22]  A. Beatty,et al.  Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. , 1999, Journal of medicinal chemistry.

[23]  R. Knabb,et al.  Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa. , 1999, Bioorganic & medicinal chemistry letters.

[24]  J. Stenflo Contributions of Gla and EGF-like domains to the function of vitamin K-dependent coagulation factors. , 1999, Critical reviews in eukaryotic gene expression.

[25]  R. Knabb,et al.  Preparation of meta-amidino-N,N-disubstituted anilines as potent inhibitors of coagulation factor Xa. , 1998, Bioorganic & Medicinal Chemistry Letters.

[26]  M. Whitlow,et al.  Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa. , 1998, Journal of medicinal chemistry.

[27]  M. Kayama,et al.  Biochemical and Pharmacological Characterization of YM-60828, a Newly Synthesized and Orally Active Inhibitor of Human Factor Xa , 1998, Thrombosis and Haemostasis.

[28]  Y. Matsumoto,et al.  Comparative Studies of an Orally-active Factor Xa Inhibitor, YM-60828, with other Antithrombotic Agents in a Rat Model of Arterial Thrombosis , 1998, Thrombosis and Haemostasis.

[29]  M. Bock,et al.  Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position. , 1997, Journal of medicinal chemistry.

[30]  Richard Spann,et al.  High capacity screening of pooled compounds: Identification of the active compound without re‐assay of pool members , 1996 .

[31]  H. Ishihara,et al.  DX-9065a, an Orally Active, Specific Inhibitor of Factor Xa, Inhibits Thrombosis without Affecting Bleeding Time in Rats , 1995, Thrombosis and Haemostasis.

[32]  S. Katakura,et al.  Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors. , 1994, Journal of medicinal chemistry.

[33]  H. Ishihara,et al.  DX-9065a, a New Synthetic, Potent Anticoagulant and Selective Inhibitor for Factor Xa , 1994, Thrombosis and Haemostasis.

[34]  D. Turk,et al.  The refined 1.9‐Å X‐ray crystal structure of d‐Phe‐Pro‐Arg chloromethylketone‐inhibited human α‐thrombin: Structure analysis, overall structure, electrostatic properties, detailed active‐site geometry, and structure‐function relationships , 1992, Protein science : a publication of the Protein Society.

[35]  C. Dunwiddie,et al.  Comparison of the In Vivo Anticoagulant Properties of Standard Heparin and the Highly Selective Factor Xa Inhibitors Antistasin and Tick Anticoagulant Peptide (TAP) in a Rabbit Model of Venous Thrombosis , 1991, Thrombosis and Haemostasis.

[36]  I. H. Segel Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems , 1975 .

[37]  A. Cornish-Bowden A simple graphical method for determining the inhibition constants of mixed, uncompetitive and non-competitive inhibitors. , 1974, The Biochemical journal.