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Factor XIa inhibitors: A review of the patent literature
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journal
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February 2016 |
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Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups
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journal
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December 2019 |
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Practical application of ligand efficiency metrics in lead optimisation
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journal
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July 2018 |
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Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D
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journal
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April 2018 |
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Net Clinical Benefit of Warfarin in Patients With Atrial Fibrillation: A Report From the Swedish Atrial Fibrillation Cohort Study
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journal
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May 2012 |
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Coagulation Assays
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journal
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July 2005 |
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The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations
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journal
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November 2013 |
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Ligand efficiency indices as guideposts for drug discovery
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journal
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April 2005 |
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Exploiting Subsite S1 of Trypsin-Like Serine Proteases for Selectivity: Potent and Selective Inhibitors of Urokinase-Type Plasminogen Activator
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journal
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October 2001 |
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Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs
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journal
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October 2017 |
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Discovery of the Novel Antithrombotic Agent 5-Chloro- N -({(5 S )-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): An Oral, Direct Factor Xa Inhibitor
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journal
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September 2005 |
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Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors
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journal
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February 2017 |
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Complement factor D, a novel serine protease: Complement factor D
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journal
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April 1996 |
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Discovery of Potent, Selective, Orally Active, Nonpeptide Inhibitors of Human Mast Cell Chymase
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journal
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March 2007 |
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Congenital Factor XI Deficiency: An Update
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journal
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August 2013 |
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Factor XI as a target for antithrombotic therapy
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journal
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September 2014 |
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When to Start a Statin Is a Preference-Sensitive Decision
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journal
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September 2017 |
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Structure-based design, synthesis, and profiling of a β-tryptase inhibitor with a spiro-piperidineamide scaffold, benzylamine P1 group, and a substituted indole P4 group
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journal
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January 2011 |
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The story of the discovery of heparin and warfarin
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journal
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June 2008 |
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Two-year outcomes of patients with newly diagnosed atrial fibrillation: results from GARFIELD-AF
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journal
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June 2016 |
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Evaluation of the GastroPlus™ Advanced Compartmental and Transit (ACAT) Model in Early Discovery
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journal
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June 2016 |
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Congenital prekallikrein deficiency
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journal
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December 2010 |
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Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl- N -[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1 H -pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor
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journal
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March 2005 |
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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties
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journal
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April 2015 |
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Oral Anticoagulant Therapy
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journal
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February 2012 |
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Recent evolutionary divergence of plasma prekallikrein and factor XI
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journal
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July 1986 |
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National Trends in Oral Anticoagulant Use in the United States, 2007 to 2011
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journal
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September 2012 |
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Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1 H -pyrazolo[3,4- c ]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa
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journal
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November 2007 |
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Factor XI and contact activation as targets for antithrombotic therapy
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journal
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June 2015 |
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Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212)
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journal
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November 2017 |
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Inhibition of Factor XI activity as a promising antithrombotic strategy
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journal
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September 2014 |
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Factor XI Antisense Oligonucleotide for Prevention of Venous Thrombosis
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journal
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January 2015 |
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Interaction with the S1$beta;-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors
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journal
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June 2004 |
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The influence of drug-like concepts on decision-making in medicinal chemistry
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journal
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November 2007 |
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P450-Mediated Metabolism of 1-[3-(Aminomethyl)phenyl]- N -[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1 H -pyrazole- 5-carboxamide (DPC 423) and Its Analogues to Aldoximes. Characterization of Glutathione Conjugates of Postulated Intermediates Derived from Aldoximes
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journal
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December 2001 |
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The role of molecular size in ligand efficiency
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journal
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August 2007 |
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An Analysis of the Binding Efficiencies of Drugs and Their Leads in Successful Drug Discovery Programs
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journal
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April 2010 |
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Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis
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journal
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August 2009 |
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Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)
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journal
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October 2009 |
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Scope of the Two-Step, One-Pot Palladium-Catalyzed Borylation/Suzuki Cross-Coupling Reaction Utilizing Bis-Boronic Acid
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journal
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September 2012 |
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Ligand efficiency: a useful metric for lead selection
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journal
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May 2004 |
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MAA868, a novel FXI antibody with a unique binding mode, shows durable effects on markers of anticoagulation in humans
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journal
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March 2019 |
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Structure-Based Design of Novel Potent Nonpeptide Thrombin Inhibitors
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journal
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April 2002 |
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Contact system revisited: an interface between inflammation, coagulation, and innate immunity
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journal
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February 2016 |
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Effectiveness and Safety of Dabigatran, Rivaroxaban, and Apixaban Versus Warfarin in Nonvalvular Atrial Fibrillation
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journal
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June 2016 |
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The maximal affinity of ligands
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journal
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August 1999 |
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Real-world clinical evidence on rivaroxaban, dabigatran, and apixaban compared with vitamin K antagonists in patients with nonvalvular atrial fibrillation: a systematic literature review
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journal
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September 2018 |
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Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway
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journal
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April 2019 |
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The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex
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journal
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November 2005 |
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First-in-human study to assess the safety, pharmacokinetics and pharmacodynamics of BMS-962212, a direct, reversible, small molecule factor XIa inhibitor in non-Japanese and Japanese healthy subjects: First-in-human study of BMS-962212 a first-in-class small molecule factor XIa inhibitor
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journal
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March 2018 |
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Factor XIa Inhibitors as New Anticoagulants
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journal
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May 2018 |
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Engineering inhibitors highly selective for the S1 sites of Ser190 trypsin-like serine protease drug targets
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journal
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November 2001 |
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Bioactivation of Benzylamine to Reactive Intermediates in Rodents: Formation of Glutathione, Glutamate, and Peptide Conjugates
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journal
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August 2002 |