The race to an orally active Factor Xa inhibitor: recent advances.

ML Quan, JM Smallheer - Current Opinion in Drug Discovery & …, 2004 - europepmc.org
Factor Xa (fXa) is a key enzyme in the coagulation cascade and an essential component of
the prothrombinase complex, which activates prothrombin to thrombin, leading to fibrin clot …

Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors

X Hao, X Zuo, D Kang, J Zhang, Y Song… - Expert opinion on …, 2019 - Taylor & Francis
Introduction: Thrombosis is a common causal pathology for stroke, acute coronary syndrome
and venous thromboembolism disorders, which are the leading cause of death worldwide …

Novel factor Xa inhibitors: a patent review

M De Candia, G Lopopolo… - Expert opinion on …, 2009 - Taylor & Francis
Importance of the field. New oral anticoagulants with favorable safety profiles and fixed
doses are required for the management of thromboembolism and stroke prevention in …

Developments in factor Xa inhibitors for the treatment of thromboembolic disorders

YK Lee, MR Player - Medicinal Research Reviews, 2011 - Wiley Online Library
Thromboembolic diseases are the leading causes of morbidity and mortality in the
developed world. Anticoagulants provide effective treatment for venous or arterial …

Optimization of the β-Aminoester class of factor Xa inhibitors. part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant …

KR Guertin, CJ Gardner, SI Klein, AL Zulli… - Bioorganic & medicinal …, 2002 - Elsevier
Further optimization of the β-aminoester class of factor Xa (fXa) inhibitors is described
culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with …

The design and synthesis of noncovalent factor Xa inhibitors

ML Quan, RR Wexler - Current Topics in Medicinal Chemistry, 2001 - ingentaconnect.com
Thrombosis is a major cause of mortality in the industrialized world. Therefore, the control of
blood coagulation has become a major target for new therapeutic agents. One attractive …

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 …

Factor Xa inhibitors: next-generation antithrombotic agents

DJP Pinto, JM Smallheer, DL Cheney… - Journal of medicinal …, 2010 - ACS Publications
Thrombosis is the underlying cause of a host of common, debilitating, and often fatal
cardiovascular disorders. Formation of thrombi in the arterial circulation can lead to acute …

Contemporary developments in the discovery of selective factor Xa inhibitors: A review

NR Patel, DV Patel, PR Murumkar, MR Yadav - European journal of …, 2016 - Elsevier
Thrombosis is a leading cause of death in cardiovascular diseases such as myocardial
infarction (MI), unstable angina and acute coronary syndrome (ACS) in the industrialized …

Recent advances in the discovery and development of direct coagulation factor Xa inhibitors

WR Gould, RJ Leadley - Current pharmaceutical design, 2003 - ingentaconnect.com
Coronary heart disease (CHD) is the leading cause of mortality and morbidity in the United
States. Currently, there are approximately 12 million Americans with CHD, which is most …