The discovery of glycine and related amino acid-based factor Xa inhibitors

JT Kohrt, KJ Filipski, WL Cody, CF Bigge, F La… - Bioorganic & medicinal …, 2006 - Elsevier
Herein, we report on the identification of three potent glycine and related amino acid-based
series of FXa inhibitors containing a neutral P1 chlorophenyl pharmacophore. A X-ray …

[引用][C] Factor Xa Inhibitors

S Kunitada, T Nagahara - Current …, 1996 - … PUBL LTD EXECUTIVE STE Y-2 …

Parallel synthesis and structure–activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors

SM Bauer, EA Goldman, W Huang, T Su… - Bioorganic & medicinal …, 2004 - Elsevier
Parallel synthesis and structure–activity relationships of a series of highly potent, selective,
and neutral factor Xa inhibitors - ScienceDirect Skip to main contentSkip to article Elsevier logo …

FXa direct synthetic inhibitors

FC Zacconi - Anticoagulant Drugs, 2018 - books.google.com
Abstract Factor Xa (FXa) is an enzyme belonging to the serine protease family which plays a
vital role in hemostasis, being an essential part in the blood-clotting cascade by catalyzing …

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 …

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 …

Aroylguanidine-based factor Xa inhibitors: the discovery of BMS-344577

Y Shi, C Li, SP O'Connor, J Zhang, M Shi… - Bioorganic & medicinal …, 2009 - Elsevier
We report the design and synthesis of a novel class of N, N′-disubstituted aroylguanidine-
based lactam derivatives as potent and orally active FXa inhibitors. The structure–activity …

Synthesis, Characterization, and Structure− Activity Relationships of Amidine-Substituted (Bis) benzylidene-Cycloketone Olefin Isomers as Potent and Selective Factor …

WJ Guilford, KJ Shaw, JL Dallas… - Journal of medicinal …, 1999 - ACS Publications
Factor Xa (FXa) is a trypsin-like serine protease that plays a key role in blood coagulation
linking the intrinsic and extrinsic pathways to the final common pathway of the coagulation …

Design, synthesis, and SAR of cis-1, 2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part I: Exploration of 5–6 fused rings as alternative S1 moieties

K Yoshikawa, A Yokomizo, H Naito, N Haginoya… - Bioorganic & medicinal …, 2009 - Elsevier
A series of cis-1, 2-diaminocyclohexane derivatives were synthesized with the aim of
optimizing previously disclosed factor Xa (fXa) inhibitors. The exploration of 5–6 fused rings …

Clinical pharmacology of direct and indirect factor Xa inhibitors

HJ Rupprecht, R Blank - Drugs, 2010 - Springer
The limitations of conventional anticoagulants have stimulated the development of new
anticoagulants. The central position of factor Xa (FXa) at the junction of the intrinsic and …