Novel factor Xa inhibitors for prevention and treatment of thromboembolic diseases

D Kubitza, S Haas - Expert opinion on investigational drugs, 2006 - Taylor & Francis
Novel anticoagulants to replace unfractionated heparins, low molecular weight heparins and
vitamin K antagonists, are needed urgently. Coagulation factor Xa is an attractive target for …

Direct Factor Xa and direct thrombin inhibitors: a clinical trial update.

AG Turpie - Current Opinion in Drug Discovery & Development, 2009 - europepmc.org
Anticoagulant use is recommended for the prevention and treatment of several
thromboembolic disorders including venous thromboembolism. However, anticoagulants …

Nonbenzamidine tetrazole derivatives as factor Xa inhibitors

ML Quan, CD Ellis, MY He, AY Liauw… - Bioorganic & medicinal …, 2003 - Elsevier
Factor Xa (fXa) is an important serine protease that holds the central position linking the
intrinsic and extrinsic activation mechanisms in the blood coagulation cascade. Therefore …

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 …

Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a Potent …

JR Pruitt, DJP Pinto, RA Galemmo… - Journal of medicinal …, 2003 - ACS Publications
Factor Xa, a serine protease, is at the critical juncture between the intrinsic and extrinsic
pathways of the coagulation cascade. Inhibition of factor Xa has the potential to provide …

Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors

T Su, Y Wu, B Doughan, ZJ Jia, J Woolfrey… - Bioorganic & medicinal …, 2001 - Elsevier
Design, Synthesis, and SAR of Amino Acid Derivatives as Factor Xa Inhibitors -
ScienceDirect Skip to main contentSkip to article Elsevier logo Journals & Books Help …

Design, synthesis, and biological activity of non-basic compounds as factor Xa inhibitors: SAR study of S1 and aryl binding sites

S Komoriya, N Haginoya, S Kobayashi… - Bioorganic & medicinal …, 2005 - Elsevier
Compound 7 was identified as the active metabolite of 6 by HPLC and mass spectral
analysis. Modification of lead compound 7 by transformation of its N-oxide 6–6 biaryl ring …

Rational design, synthesis, and biological activity of benzoxazinones as novel factor Xa inhibitors

DA Dudley, AM Bunker, L Chi, WL Cody… - Journal of medicinal …, 2000 - ACS Publications
Inappropriate thrombus formation within blood vessels is the leading cause of mortality in
the industrialized world. Factor Xa (FXa) is a trypsin-like serine protease that plays a key role …

Arylsulfonamidopiperidone derivatives as a novel class of factor Xa inhibitors

Y Shi, SP O'Connor, D Sitkoff, J Zhang, M Shi… - Bioorganic & medicinal …, 2011 - Elsevier
The design, synthesis and SAR of a novel class of valerolactam-based arylsulfonamides as
potent and selective FXa inhibitors is reported. The arylsulfonamide–valerolactam scaffold …

2-Aminomethylphenylamine as a novel scaffold for factor Xa inhibitor

A Mochizuki, T Nagata, H Kanno, M Suzuki… - Bioorganic & medicinal …, 2011 - Elsevier
We have been researching orally active factor Xa inhibitor for a long time. We explored the
new diamine linker using effective ligands to obtain a new attractive original scaffold 2 …