The development of new low-molecular-weight factor Xa inhibitors that are potential anticoagulants

DG Tovbin, DN Tarasov, DV Malakhov… - Current Drug …, 2022 - ingentaconnect.com
Background: Despite the introduction of direct oral anticoagulants, the search for new oral
anticoagulants remains an urgent task. Objective: By using docking and scoring, based on …

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 …

Discovery of transition state factor Xa inhibitors as potential anticoagulant agents

BY Zhu, W Huang, T Su, C Marlowe… - Current Topics in …, 2001 - ingentaconnect.com
Factor Xa is an attractive biological target in the discovery and development of either
parenteral or orally active anticoagulant agents. Several strategies have been utilized at …

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 …

Discovery of a novel, potent, and specific family of factor Xa inhibitors via combinatorial chemistry

JA Ostrem, F Al-Obeidi, P Safar, A Safarova… - Biochemistry, 1998 - ACS Publications
A series of low molecular weight peptide inhibitors of factor Xa, unrelated to any previously
described, was identified by screening a combinatorial peptide library composed of l-amino …

New factor Xa inhibitors based on 1, 2, 3, 4-tetrahydroquinoline developed by molecular modelling

I Ilin, E Lipets, A Sulimov, D Kutov, K Shikhaliev… - Journal of Molecular …, 2019 - Elsevier
Factor Xa is a serine protease representing a crucial element in the coagulation process and
an attractive target for anticoagulant therapy. At the present time there are several chemical …

Patent Update: Inhibitors of Coagulation Factor Xa: From Macromolecular Beginnings to Small Molecules

RB Wallis - Current Opinion on Therapeutic Patents, 1993 - Taylor & Francis
The discovery and subsequent clinical use of coumarins, in the 1950s and of heparin in the
1970s allowed, for the first time, rational treatment of thrombotic diseases. However, in spite …

Recent advances in Factor Xa inhibitors

A Betz - Expert Opinion on Therapeutic Patents, 2001 - Taylor & Francis
Due to its critical role in the coagulation cascade Factor Xa became an important target for
antithrombotic drug development. The design of the first generation of Factor Xa inhibitors …

Synthetic inhibitors of coagulation factor Xa

U Sinha - Expert Opinion on Investigational Drugs, 1999 - Taylor & Francis
The antithrombotic efficacy of low molecular weight heparins suggest that specific inhibition
of blood coagulation factor Xa (fXa) is an appropriate target for drug discovery. Clinical …

Design, synthesis and biological activities of orally active coagulation factor Xa inhibitors

T Nagahara, S Katakura, Y Yokoyama… - European journal of …, 1995 - Elsevier
DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITIES OF ORALLY ACTIVE COAGULATION
FACTOR Xa INHIBITORS Page 1 DESIGN, SYNTHESIS AND BIOLOGICAL ACTIVITIES OF …