Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.

[1]  V. Fuster,et al.  Redefining medical treatment in the management of unstable angina. , 2011, The American journal of medicine.

[2]  L. Weber,et al.  Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors. , 2005, Bioorganic & medicinal chemistry letters.

[3]  A. Turpie Fondaparinux: a Factor Xa inhibitor for antithrombotic therapy , 2004, Expert opinion on pharmacotherapy.

[4]  M. Crowther,et al.  Ximelagatran: the first oral direct thrombin inhibitor , 2004, Expert opinion on investigational drugs.

[5]  R. Kurumbail,et al.  Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors. , 2003, Journal of medicinal chemistry.

[6]  R. Kurumbail,et al.  Polymer-assisted solution-phase library synthesis and crystal structure of alpha-ketothiazoles as tissue factor VIIa inhibitors. , 2003, Journal of medicinal chemistry.

[7]  Yuchiao Chang,et al.  Effect of intensity of oral anticoagulation on stroke severity and mortality in atrial fibrillation. , 2003, The New England journal of medicine.

[8]  R. Kurumbail,et al.  Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors. , 2003, Journal of medicinal chemistry.

[9]  M. S. South,et al.  Pharmacological Interruption of Acute Thrombus Formation with Minimal Hemorrhagic Complications by a Small Molecule Tissue Factor/Factor VIIa Inhibitor: Comparison to Factor Xa and Thrombin Inhibition in a Nonhuman Primate Thrombosis Model , 2003, Journal of Pharmacology and Experimental Therapeutics.

[10]  R. Kurumbail,et al.  Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex. , 2003, Journal of medicinal chemistry.

[11]  E. MacLaughlin,et al.  Ximelagatran: A New Era in Oral Anticoagulation , 2003 .

[12]  H. Matter,et al.  Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors. , 2003, Bioorganic & medicinal chemistry letters.

[13]  B. Eriksson,et al.  Ximelagatran and melagatran compared with dalteparin for prevention of venous thromboembolism after total hip or knee replacement: the METHRO II randomised trial , 2002, The Lancet.

[14]  Stephen Hanessian,et al.  Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones. , 2002, Bioorganic & medicinal chemistry letters.

[15]  A. Carroll,et al.  Dysinosin A: a novel inhibitor of Factor VIIa and thrombin from a new genus and species of Australian sponge of the family Dysideidae. , 2002, Journal of the American Chemical Society.

[16]  S. Hanessian,et al.  Total synthesis and structural confirmation of the marine natural product Dysinosin A: a novel inhibitor of thrombin and Factor VIIa. , 2002, Journal of the American Chemical Society.

[17]  T. Girard,et al.  Pharmacological Intervention at Disparate Sites in the Coagulation Cascade: Comparison of Anti-thrombotic Efficacy vs. Bleeding Propensity in a Rat Model of Acute Arterial Thrombosis , 2002, Journal of Thrombosis and Thrombolysis.

[18]  E. Leahy,et al.  Optimization of a screening lead for factor VIIa/TF. , 2001, Bioorganic & medicinal chemistry letters.

[19]  D. Kirchhofer,et al.  Inhibition of Arterial Thrombosis by a Soluble Tissue Factor Mutant and Active Site-blocked Factors IXa and Xa in the Guinea Pig , 2001, Thrombosis and Haemostasis.

[20]  E. Persson,et al.  Inhibitors of the tissue factor/factor VIIa-induced coagulation: synthesis and in vitro evaluation of novel 2-aryl substituted pyrid. , 2000, Bioorganic & medicinal chemistry.

[21]  K. J. Filipski,et al.  An efficient synthesis of 2-(3-(4-amidinophenylcarbamoyl)naphthalen-2-yl)-5-((2,2-methylpropyl)carbamoyl)benzoic acid: a factor VIIa inhibitor discovered by the Ono Pharmaceutical Company , 2000 .

[22]  B. Pedersen,et al.  Inhibitors of the tissue factor/factor VIIa-induced coagulation: synthesis and in vitro evaluation of novel specific 2-aryl substituted 4H-3,1-benzoxazin-4-ones. , 2000, Bioorganic & medicinal chemistry.

[23]  J. Willerson,et al.  Thromboresistance of balloon-injured porcine carotid arteries after local gene transfer of human tissue factor pathway inhibitor. , 2000, Circulation.

[24]  M. Bradley,et al.  Inhibition of the tissue factor/factor VIIa complex — Lead optimisation using combinatorial chemistry , 1999 .

[25]  M. Condorelli,et al.  Antithrombotic effects of recombinant human, active site-blocked factor VIIa in a rabbit model of recurrent arterial thrombosis. , 1998, Circulation research.

[26]  D. Kirchhofer,et al.  Dissociation of Antithrombotic Effect and Bleeding Time Prolongation in Rabbits by Inhibiting Tissue Factor Function , 1997, Thrombosis and Haemostasis.

[27]  T. Edgington,et al.  The Structural Basis of Function of the TF●VIIa Complex in the Cellular Initiation of Coagulation , 1997, Thrombosis and Haemostasis.

[28]  Alan D. Lopez,et al.  Mortality by cause for eight regions of the world: Global Burden of Disease Study , 1997, The Lancet.

[29]  R. Kelley,et al.  A soluble tissue factor mutant is a selective anticoagulant and antithrombotic agent. , 1997, Blood.

[30]  Paul R. Gerber,et al.  MAB, a generally applicable molecular force field for structure modelling in medicinal chemistry , 1995, J. Comput. Aided Mol. Des..

[31]  J. Hirsh,et al.  Interactions of Warfarin with Drugs and Food , 1994, Annals of Internal Medicine.

[32]  Wolfgang Kabsch,et al.  Automatic processing of rotation diffraction data from crystals of initially unknown symmetry and cell constants , 1993 .

[33]  Y. Nemerson,et al.  The tissue factor pathway of blood coagulation. , 1992, Progress in hemostasis and thrombosis.

[34]  A. Brunger Free R value: a novel statistical quantity for assessing the accuracy of crystal structures. , 1992 .

[35]  L Goldman,et al.  Bleeding in outpatients treated with warfarin: relation to the prothrombin time and important remediable lesions. , 1989, The American journal of medicine.

[36]  E. Saiah,et al.  Chapter 9. Anticoagulants: Inhibitors of the factor vila/tissue factor pathway , 2002 .

[37]  M. Chiariello,et al.  A monoclonal antibody against rabbit tissue factor inhibits thrombus formation in stenotic injured rabbit carotid arteries. , 1994, Circulation research.

[38]  Axel T. Brunger,et al.  X-PLOR Version 3.1: A System for X-ray Crystallography and NMR , 1992 .