Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Design, synthesis and biological evaluation of novel FXIa inhibitors with 2-phenyl-1H-imidazole-5-carboxamide moiety as P1 fragment

(2021) Yu Lei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa

(2020) Tianan Fang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design and Synthesis of Novel Proline Based Factor XIa Selective Inhibitors as Leads for Potential New Anticoagulants

(2020) Zahid Hussain et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Heart Disease and Stroke Statistics—2020 Update: A Report From the American Heart Association

(2020) Salim S. Virani et al.   CIRCULATION

Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species

(2020) Wu Yang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach

(2020) Edwige Lorthiois et al.   JOURNAL OF MEDICINAL CHEMISTRY

Studies on fragment-based design of allosteric inhibitors of human factor XIa

(2020) Rio S. Boothello et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A synthetic heparin mimetic that allosterically inhibits factor XIa and reduces thrombosis in vivo without enhanced risk of bleeding

(2019) Rami A. Al‐Horani et al.   JOURNAL OF THROMBOSIS AND HAEMOSTASIS

Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability

(2019) Charles G. Clark et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups

(2019) James R. Corte et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker

(2017) James R. Corte et al.   JOURNAL OF MEDICINAL CHEMISTRY

Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N -phenyl carbamate P2 prime group

(2016) James R. Corte et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel phenylalanine derived diamides as Factor XIa inhibitors

(2016) Leon M. Smith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pyridine and pyridinone-based factor XIa inhibitors

(2015) James R. Corte et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties

(2015) Donald J.P. Pinto et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa

(2015) Pancras C. Wong et al.   JOURNAL OF THROMBOSIS AND THROMBOLYSIS

Factor XI Antisense Oligonucleotide for Prevention of Venous Thrombosis

(2015) Harry R. Büller et al.   NEW ENGLAND JOURNAL OF MEDICINE

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2′ Moiety

(2015) Zilun Hu et al.   ACS Medicinal Chemistry Letters

Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity

(2014) Jon J. Hangeland et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors

(2014) Mimi L. Quan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Thrombosis: a major contributor to the global disease burden

(2014)   JOURNAL OF THROMBOSIS AND HAEMOSTASIS

New oral anticoagulants: A view from the laboratory

(2012) Jeffrey I. Weitz   AMERICAN JOURNAL OF HEMATOLOGY

Global and regional mortality from 235 causes of death for 20 age groups in 1990 and 2010: a systematic analysis for the Global Burden of Disease Study 2010

(2012) Rafael Lozano et al.   LANCET

A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits

(2011) Pancras C. Wong et al.   JOURNAL OF THROMBOSIS AND THROMBOLYSIS

Structure and function of factor XI

(2010) J. Emsley et al.   BLOOD

Patients with severe factor XI deficiency have a reduced incidence of deep-vein thrombosis

(2010) Ophira Salomon et al.   THROMBOSIS AND HAEMOSTASIS

C−H Bonds as Ubiquitous Functionality: A General Approach to Complex Arylated Pyrazoles via Sequential RegioselectiveC-Arylation andN-Alkylation Enabled by SEM-Group Transposition

(2009) Roman Goikhman et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Synthesis of 3-Substituted-4(3H)-quinazolinones via HATU-Mediated Coupling of 4-Hydroxyquinazolines with Amines

(2009) Zili Xiao et al.   ORGANIC LETTERS

Prevention of vascular graft occlusion and thrombus-associated thrombin generation by inhibition of factor XI

(2008) E. I. Tucker et al.   BLOOD

Reduced incidence of ischemic stroke in patients with severe factor XI deficiency

(2008) O. Salomon et al.   BLOOD