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 …

Synthesis and biological activity of novel 1, 4-diazepane derivatives as factor Xa inhibitor with potent anticoagulant and antithrombotic activity

H Koshio, F Hirayama, T Ishihara, Y Taniuchi… - Bioorganic & medicinal …, 2004 - Elsevier
Factor Xa (fXa) is a serine protease involved in the coagulation cascade, which has received
great interest as a potential target for the development of new antithrombotic drugs. Herein …

The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor

F Hirayama, H Koshio, N Katayama, H Kurihara… - Bioorganic & medicinal …, 2002 - Elsevier
Since Factor Xa (FXa) is well known to play a central role in thrombosis and hemostasis,
inhibition of FXa is an attractive target for antithrombotic strategies. As a part of our …

Novel anthranilamide-based FXa Inhibitors: Drug design, synthesis and biological evaluation

W Wang, J Yuan, X Fu, F Meng, S Zhang, W Xu, Y Xu… - Molecules, 2016 - mdpi.com
Factor Xa (FXa) plays a significant role in the blood coagulation cascade and it has become
a promising target for anticoagulation drugs. Three oral direct FXa inhibitors have been …

Design, synthesis and biological activity of YM-60828 derivatives: potent and orally-bioavailable factor Xa inhibitors based on naphthoanilide and …

F Hirayama, H Koshio, T Ishihara, S Watanuki… - Bioorganic & medicinal …, 2002 - Elsevier
Factor Xa (FXa) is a serine protease which plays a pivotal role in the coagulation cascade.
The inhibition of FXa has received great interest as a potential target for the development of …

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 …

Design, synthesis and SAR of novel ethylenediamine and phenylenediamine derivatives as factor Xa inhibitors

K Yoshikawa, T Yoshino, Y Yokomizo, K Uoto… - Bioorganic & medicinal …, 2011 - Elsevier
We previously reported on a series of cyclohexanediamine derivatives as highly potent
factor Xa inhibitors. Herein, we describe the modification of the spacer moiety to discover an …

Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors

Y Imaeda, T Miyawaki, H Sakamoto, F Itoh… - Bioorganic & medicinal …, 2008 - Elsevier
Factor Xa (FXa) is a trypsin-like serine protease involved in the coagulation cascade and
has received great interest as a potential target for the development of new antithrombotic …

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 …

Design, synthesis and biological activity of YM-60828 derivatives. Part 2: Potent and orally-bioavailable factor Xa inhibitors based on benzothiadiazine-4-one template

F Hirayama, H Koshio, N Katayama, T Ishihara… - Bioorganic & medicinal …, 2003 - Elsevier
Compound YM-60828 was previously characterized in our laboratory as a potent, selective
and orally-bioavailable Factor Xa (FXa) inhibitor. The L-shape conformation of this …