Synthesis of 3, 4-diaminobenzoyl derivatives as factor Xa inhibitors

J Yang, G Su, Y Ren, Y Chen - European Journal of Medicinal Chemistry, 2015 - Elsevier
Abstract The coagulation factor Xa (FXa) plays a central role in the blood coagulation
cascade. Recent studies have shown that FXa is a particularly attractive target for the …

Progress in the design of inhibitors of coagulation factor Xa

WR Ewing, HW Pauls, AP Spada - Drugs of the Future, 1999 - access.portico.org
Background To develop superior anticoagulant strategies requires an understanding of the
biochemical and biophysical mechanisms activating and regulating blood coagulation. The …

The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review

DJP Pinto, JX Qiao, RM Knabb - Expert Opinion on Therapeutic …, 2012 - Taylor & Francis
Introduction: Factor Xa (FXa) is a critical enzyme in the coagulation cascade responsible for
thrombin generation, the final enzyme that leads to fibrin clot formation. Significant success …

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 …

The discovery of the Factor Xa inhibitor otamixaban: from lead identification to clinical development

KR Guertin, YM Choi - Current medicinal chemistry, 2007 - ingentaconnect.com
Factor Xa (fXa) is a critical serine protease situated at the confluence of the intrinsic and
extrinsic pathways of the blood coagulation cascade. FXa catalyses the conversion of …

Engineered factor Xa variants retain procoagulant activity independent of direct factor Xa inhibitors

D Verhoef, KM Visscher, CR Vosmeer… - Nature …, 2017 - nature.com
The absence of an adequate reversal strategy to prevent and stop potential life-threatening
bleeding complications is a major drawback to the clinical use of the direct oral inhibitors of …

Surfing the blood coagulation cascade: insight into the vital factor Xa

NE Núñez-Navarro, FM Santana… - Current Medicinal …, 2019 - ingentaconnect.com
Factor Xa (FXa) plays a key role in haemostasis, it is a central part of the blood coagulation
cascade which catalyzes the production of thrombin and leads to clot formation and wound …

Recent advances in Factor Xa inhibitors

A Betz - Expert Opinion on Therapeutic Patents, 2001 - Taylor & Francis
Due to its critical role in the coagulation cascade Factor Xa became an important target for
antithrombotic drug development. The design of the first generation of Factor Xa inhibitors …

State-of-the-art review: Factor Xa versus factor IIa inhibitors

B Kaiser - Clinical and Applied Thrombosis/Hemostasis, 1997 - journals.sagepub.com
The development of specific inhibitors of blood coagulation enzymes has led to a number of
new anticoagulant/antithrombotic agents that could be useful for prophylaxis and/or …

Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa

JA Willardsen, DA Dudley, WL Cody, L Chi… - Journal of medicinal …, 2004 - ACS Publications
Factor Xa (FXa) has materialized as a key enzyme for the intervention of the blood
coagulation cascade and for the development of new antithrombotic agents. FXa is the lone …