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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Stu

Journal Article · · J. Med. Chem.
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Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1845475
Journal Information:
J. Med. Chem., Vol. 65, Issue (3)
Country of Publication:
United States
Language:
ENGLISH

References (41)

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Heart Disease and Stroke Statistics—2020 Update: A Report From the American Heart Association journal March 2020
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Feedback activation of factor XI by thrombin in plasma results in additional formation of thrombin that protects fibrin clots from fibrinolysis journal October 1995
Reduced incidence of ischemic stroke in patients with severe factor XI deficiency journal April 2008
Inherited factor XI deficiency confers no protection against acute myocardial infarction journal April 2003
Patients with severe factor XI deficiency have a reduced incidence of deep-vein thrombosis journal January 2011
Levels of intrinsic coagulation factors and the risk of myocardial infarction among men: opposite and synergistic effects of factors XI and XII journal December 2006
High Levels of Coagulation Factor XI as a Risk Factor for Venous Thrombosis journal March 2000
FXI Is Essential for Thrombus Formation Following FeCl3-Induced Injury of the Carotid Artery in the Mouse journal January 2002
Effects of factor XI deficiency on ferric chloride-induced vena cava thrombosis in mice journal September 2006
Antithrombotic and hemostatic effects of a small molecule factor XIa inhibitor in rats journal September 2007
A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits journal May 2011
In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa journal August 2015
Factor XI contributes to thrombus propagation on injured neointima of the rabbit iliac artery journal July 2006
Prevention of vascular graft occlusion and thrombus-associated thrombin generation by inhibition of factor XI journal January 2009
Factor XI–dependence of surface- and tissue factor–initiated thrombus propagation in primates journal August 2003
ISIS-FXIRx, A Novel and Specific Antisense Inhibitor of Factor XI, Caused Significant Reduction in FXI Antigen and Activity and Increased aPTT without Causing Bleeding in Healthy Volunteers journal November 2011
Factor XI Antisense Oligonucleotide for Prevention of Venous Thrombosis journal January 2015
Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors journal January 2014
Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity journal November 2014
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties journal April 2015
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1 H )-one as the P2′ Moiety journal April 2015
Pyridine and pyridinone-based factor XIa inhibitors journal February 2015
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group journal May 2016
Novel phenylalanine derived diamides as Factor XIa inhibitors journal January 2016
Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker journal January 2017
Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency journal August 2017
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability journal October 2019
Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa journal February 2020
Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups journal December 2019
Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment journal August 2021
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach journal June 2020
Design and synthesis of novel proline based factor XIa selective inhibitors as leads for potential new anticoagulants journal August 2020
Studies on fragment-based design of allosteric inhibitors of human factor XIa journal December 2020
A synthetic heparin mimetic that allosterically inhibits factor XIa and reduces thrombosis in vivo without enhanced risk of bleeding journal September 2019
Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species journal May 2020
C−H Bonds as Ubiquitous Functionality: A General Approach to Complex Arylated Pyrazoles via Sequential Regioselective C -Arylation and N -Alkylation Enabled by SEM-Group Transposition journal February 2009
Synthesis of 3-Substituted-4(3 H )-quinazolinones via HATU-Mediated Coupling of 4-Hydroxyquinazolines with Amines journal February 2009

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