Results 191 to 200 of about 38,154 (222)
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Tetrahydro-isoquinoline-Based Factor Xa Inhibitors
Journal of Medicinal Chemistry, 1998Derivatives of (2-amidino-1,2,3, 4-tetrahydro-isoquinolin-7-yloxy)phenylacetic acid (TIPAC) were developed as inhibitors of factor Xa (fXa). The compounds are prepared using 15 synthetic steps on average. The most potent compounds (14, 17, 22-26) display inhibition constants of Ki = 21-55 nM but do not inhibit thrombin (Ki = 5->100 microM) and only ...
R, Kucznierz +5 more
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The direct factor Xa inhibitor rivaroxaban
Medical Journal of Australia, 2009Warfarin and heparin are the traditional mainstay anticoagulant therapies for treating thromboembolic disease. These drugs, with a documented history of utility, also have inherent difficulties in usage; in particular, the complicated monitoring and numerous drug-drug interactions of warfarin, and the need for parenteral administration of heparins. New
Abhishek K, Verma, Timothy A, Brighton
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Hämostaseologie, 2009
SummaryOral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase ...
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SummaryOral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase ...
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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 ...
S. Kunitada, T. Nagahara, T. Hara
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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 ...
S. Kunitada, T. Nagahara, T. Hara
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Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2003Factor Xa (fXa) is an important serine protease in the blood coagulation cascade. Inhibition of fXa has emerged as an attractive target for potential therapeutic applications in the treatments of both arterial and venous thrombosis. Herein, we describe a series of non-benzamidine isoxazoline derivatives as fXa inhibitors.
Mimi L, Quan +10 more
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Factor Xa inhibitors for acute coronary syndromes
Cochrane Database of Systematic Reviews, 2011The activation of coagulation mechanisms plays a central role in the pathogenesis of acute coronary syndromes (ACS). Administration of unfractionated heparin (UFH) and low molecular weight heparins (LMWH), agents preventing the progression of thrombus formation, is a crucial therapeutic strategy.
Viviana, Brito +2 more
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Synthetic inhibitors of coagulation factor Xa
Expert Opinion on Investigational Drugs, 1999The 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 evidence also supports the effectiveness of warfarin, an orally bioavailable non-specific anticoagulant.
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Edoxaban, a Novel Oral Factor Xa Inhibitor
Annals of Pharmacotherapy, 2015Objective: To evaluate the current literature and potential clinical role of edoxaban (Savaysa) for stroke prevention in nonvalvular atrial fibrillation (NVAF) and treatment of deep-vein thrombosis and pulmonary embolism. Data Sources: A PubMed and Cochrane Central Register of Controlled trials search was conducted in February2015 using the search ...
Chelsea, Minor +2 more
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Apixaban: an emerging oral factor Xa inhibitor
Journal of Thrombosis and Thrombolysis, 2009Apixaban, an oral direct factor Xa inhibitor, is currently in late stage clinical development for the prevention and treatment of thromboembolic diseases. In comparison with current treatment standards for venous thromboembolism (VTE) prophylaxis, apixaban has shown decreased rates of clinically significant bleeding with mixed results in terms of non ...
Christopher, Roser-Jones +1 more
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Rivaroxaban, an oral direct factor Xa inhibitor
Expert Opinion on Investigational Drugs, 2008Rivaroxaban is a small molecule, direct Factor Xa inhibitor and may be a potentially attractive alternative to vitamin K antagonists. Rivaroxaban is being investigated for the prevention and treatment of venous and arterial thrombosis. A broad search of Medline, clinicaltrials.gov and the annual proceedings of the American Society of Hematology and the
Jonathan P, Piccini +4 more
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