Structure-and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs

RJ Young, M Campbell, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2006 - Elsevier
Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-
ylsulfonyl) aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an …

Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with biaryl P4 motifs

RJ Young, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2008 - Elsevier
Structure and property based drug design was exploited in the synthesis of
sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups …

2‐Aminobenzamide‐Based Factor Xa Inhibitors with Novel Mono‐and Bi‐Aryls as S4 Binding Elements

NR Patel, DV Patel, AM Kanhed, SP Patel… - …, 2019 - Wiley Online Library
Factor Xa, a key serine protease in the coagulation cascade, has attracted a great deal of
attention as a target for developing new antithrombotic agents. A series of novel alkyl …

Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors incorporating substituted biphenyl P4 motifs

P Zhang, L Bao, JF Zuckett, EA Goldman, ZJ Jia… - Bioorganic & medicinal …, 2004 - Elsevier
Anthranilamides 4 and 5 were designed and synthesized as selective and orally
bioavailable factor Xa inhibitors. Structural modifications aimed at lowering their lipophilicity …

Design, synthesis and structure–activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors

Y Zhao, M Jiang, S Zhou, S Wu, X Zhang, L Ma… - European journal of …, 2015 - Elsevier
A novel series of potent and efficacious factor Xa inhibitors which possesses
pyrrole/indole/thiazole moieties as S4 binding element was identified. Compound 7b …

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 …

Indoline derivatives II: synthesis and factor Xa (FXa) inhibitory activities

T Noguchi, N Tanaka, T Nishimata, R Goto… - Chemical and …, 2007 - jstage.jst.go.jp
Factor Xa (FXa) is well known to play a pivotal role in blood coagulation, so FXa inhibitor is a
promising drug candidate for prophylaxis and treatment of thromboembolic diseases. In the …

Design, synthesis and biological activity of amidinobicyclic compounds (derivatives of DX-9065a) as factor Xa inhibitors: SAR study of S1 and aryl binding sites

S Komoriya, N Kanaya, T Nagahara… - Bioorganic & medicinal …, 2004 - Elsevier
Since factor Xa (fXa) plays a pivotal role in the blood coagulation cascade, inhibition of fXa
is thought to be an effective treatment for a variety of thrombotic events.(2S)-2-[4-[[(3S)-1 …

Advances in the development of novel factor Xa inhibitors: a patent review

AN Khadse, MK Sharma, PR Murumkar… - Mini Reviews in …, 2018 - ingentaconnect.com
Development of new anticoagulants has been in constant demand throughout the world due
to increasing rate of morbidity and mortality caused by thrombotic diseases. Factor Xa (FXa) …

Amino (methyl) pyrrolidines as novel scaffolds for factor Xa inhibitors

Y Shi, D Sitkoff, J Zhang, W Han, Z Hu, PD Stein… - Bioorganic & medicinal …, 2007 - Elsevier
The design and synthesis of a novel class of amino (methyl) pyrrolidine-based sulfonamides
as potent and selective FXa inhibitors is reported. The amino (methyl) pyrrolidine scaffolds …