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 development of new factor Xa inhibitors based on amide synthesis

DN Tarasov, DG Tovbin, DV Malakhov… - Current drug …, 2018 - ingentaconnect.com
Background: Factor Xa (FXa) is known to play a central role in blood coagulation cascade
and considered to be one of the most attractive targets for oral anticoagulants of new …

Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor

H Nishida, Y MiYAZAKI, Y Kitamura… - Chemical and …, 2001 - jstage.jst.go.jp
Intravascular clot formation is an important factor in a number of cardiovascular diseases.
Therefore, the prevention of blood coagulation has become a major target for new …

Synthesis of pyrrolo [3, 2-d] pyrimidineone derivatives as novel FXa inhibitors

J Yang, B Su, R Liao, J Wang, S Bo - Bioorganic & Medicinal Chemistry …, 2023 - Elsevier
Abstract A series of pyrrolo [3, 2-d] pyrimidineone compounds have been designed and
synthesized as novel FXa inhibitors. Bioassay of the tested compounds showed moderate to …

Advances in inhibitors of FXa

L Guo, S Ma - Current Drug Targets, 2015 - ingentaconnect.com
Thromboembolic diseases such as deep vein thrombosis (DVT), pulmonary embolism (PE),
myocardial infarction (MI) and ischemic strokes are mainly responsible for people's morbidity …

Cinnamyl derivatives: synthesis and factor Xa (FXa) inhibitory activities

T Noguchi, N Tanaka, T Nishimata, R Goto… - Chemical and …, 2008 - jstage.jst.go.jp
To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety
was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result …

Synthesis and Conformational Analysis of a Non-Amidine Factor Xa Inhibitor That Incorporates 5-Methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine as S4 Binding …

N Haginoya, S Kobayashi, S Komoriya… - Journal of medicinal …, 2004 - ACS Publications
Our exploratory study was based on the concept that a non-amidine factor Xa (fXa) inhibitor
is suitable for an orally available anticoagulant. We synthesized and evaluated a series of N …

Design, synthesis, and biological activity of non-amidine factor Xa inhibitors containing pyridine N-oxide and 2-carbamoylthiazole units

N Haginoya, S Kobayashi, S Komoriya… - Bioorganic & medicinal …, 2004 - Elsevier
Based on the both of results for X-ray studies of tetrahydrothiazolopyridine derivative 1c and
FXV673, we synthesized a series of thiazol-5-ylpyridine derivatives containing pyridine N …

Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities

H Nishida, Y Miyazaki, T Mukaihira, F Saitoh… - Chemical and …, 2002 - jstage.jst.go.jp
Intravascular clot formation is an important event in a number of cardiovascular diseases.
The prevention of blood coagulation has become a major target for new therapeutic agents …

Characterization of a novel selective factor Xa inhibitor, DJT06001, which reduces thrombus formation with low risk of bleeding

X Hu, Y Xiao, C Yu, Y Zuo, W Yang, X Wang… - European Journal of …, 2018 - Elsevier
Abstract Factor Xa (FXa) is a serine protease that plays key roles in linking the intrinsic and
extrinsic coagulation pathways to the final common pathway. DJT06001 is an oral, highly …