Coagulation factor Xa inhibition: biological background and rationale

J Leadley - Current topics in medicinal chemistry, 2001 - ingentaconnect.com
Ischemic heart disease and cerebrovascular disease are the leading causes of death in the
world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due …

[HTML][HTML] Discovery and development of Factor Xa inhibitors (2015–2022)

W Zheng, X Dai, B Xu, W Tian, J Shi - Frontiers in Pharmacology, 2023 - frontiersin.org
As a pathological coagulation process, thrombus can lead to many serious diseases,
including ischemic stroke, acute myocardial infarction (AMI), acute coronary syndrome …

[HTML][HTML] Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies

PC Wong, EJ Crain, B Xin, RR Wexler, PYS Lam… - Journal of Thrombosis …, 2008 - Elsevier
Background: Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late‐
stage clinical development for the prevention and treatment of thromboembolic diseases …

[HTML][HTML] Milvexian, an orally bioavailable, small‐molecule, reversible, direct inhibitor of factor XIa: in vitro studies and in vivo evaluation in experimental thrombosis in …

PC Wong, EJ Crain, JM Bozarth, Y Wu… - Journal of Thrombosis …, 2022 - Elsevier
Abstract Background Milvexian (BMS‐986177/JNJ‐70033093) is an orally bioavailable
factor XIa (FXIa) inhibitor currently in phase 2 clinical trials. Objectives To evaluate in vitro …

Discovery of 1-(3'-Aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide …

ML Quan, PYS Lam, Q Han, DJP Pinto… - Journal of medicinal …, 2005 - ACS Publications
Modification of a series of pyrazole factor Xa inhibitors to incorporate an
aminobenzisoxazole as the P1 ligand resulted in compounds with improved selectivity for …

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

PC Wong, EJ Crain, CA Watson… - Journal of thrombosis and …, 2011 - Springer
Abstract BMS-262084 is a 4-carboxy-2-azetidinone-containing irreversible inhibitor of FXIa,
which is selective over other coagulation proteases. We evaluated the in vitro and in vivo …

Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants

PYS Lam, CG Clark, R Li, DJP Pinto… - Journal of medicinal …, 2003 - ACS Publications
As part of an ongoing effort to prepare orally active factor Xa inhibitors using structure-based
drug design techniques and molecular recognition principles, a systematic study has been …

Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a Potent …

JR Pruitt, DJP Pinto, RA Galemmo… - Journal of medicinal …, 2003 - ACS Publications
Factor Xa, a serine protease, is at the critical juncture between the intrinsic and extrinsic
pathways of the coagulation cascade. Inhibition of factor Xa has the potential to provide …

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

PC Wong, ML Quan, CA Watson, EJ Crain… - Journal of thrombosis …, 2015 - Springer
Abstract BMS-654457 ((+) 3′-(6-carbamimidoyl-4-methyl-4-phenyl-1, 2, 3, 4-tetrahydro-
quinolin-2-yl)-4-carbamoyl-5′-(3-methyl-butyrylamino)-biphenyl-2-carboxylic acid) is a …

The P2Y1 receptor antagonist MRS2500 prevents carotid artery thrombosis in cynomolgus monkeys

PC Wong, C Watson, EJ Crain - Journal of thrombosis and thrombolysis, 2016 - Springer
Adenosine diphosphate directly induces platelet aggregation via the G-protein coupled P2Y
1 and P2Y 12 receptors. P2Y 12, but not P2Y 1, receptor antagonists are available in the …