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Efficacy and safety of oral factor Xa inhibitors versus vitamin-K antagonists in the early phase after acute ischemic stroke or TIA in the real-world setting: The PRODAST study. [PDF]

open access: yesEur Stroke J
Diener HC   +14 more
europepmc   +1 more source
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FACTOR XA INHIBITORS

2006
The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
ZHU BING-YAN   +5 more
openaire   +6 more sources

Anthranilamide inhibitors of factor Xa

Bioorganic & Medicinal Chemistry Letters, 2007
SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
David, Mendel   +20 more
openaire   +2 more sources

Factor Xa Inhibitors

Current Pharmaceutical Design, 1996
Thrombin occupies a central position in thrombus formation and eventually has been a target to develop anticoagulant agents. Although both heparin and warfarin have been used as anticoagulants, a more useful, ideal anticoagulant is desired at bedside.
Satoshi Kunitada, Takayasu Nagahara
openaire   +1 more source

Factor Xa inhibitors

2023
This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
openaire   +1 more source

Isoxazolines and isoxazoles as factor Xa inhibitors

Bioorganic & Medicinal Chemistry Letters, 2000
3,4,5-Trisubstituted isoxazolines (2) and isoxazoles (3) were prepared and evaluated for their in vitro and in vivo antithrombotic efficacy. They were compared to 3,5,5-trisubstituted isoxazolines (1) for Factor Xa selectivity and potency. They were also compared in an arterio-venous (A-V) shunt model of thrombosis.
J R, Pruitt   +7 more
openaire   +2 more sources

Factor Xa inhibitors

Perspectives in Drug Discovery and Design, 1994
Factor Xa is the serine protease that activates prothrombin to yield thrombin. Inhibitors of factor Xa play a crucial role in curtailing thrombin generation. Two key factor Xa inhibitors that are found in blood are antithrombin III and tissue factor pathway inhibitor.
openaire   +1 more source

Inhibitors of factor Xa

1999
Thrombin occupies a central position in thrombus formation and recently has been a target for the development of anticoagulant agents. As is well known, blood coagulation operates as a cascade or multiple enzymatic amplification process. In the classical intrinsic pathway, factor (f) IXa in the presence of fVIIIa, Ca2+ and phospholipid converts fX to ...
BRUNCK TERENCE KEVIN   +2 more
openaire   +3 more sources

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