Results 201 to 210 of about 18,017 (247)

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.
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Synthetic inhibitors of coagulation factor Xa

Expert Opinion on Investigational Drugs, 1999
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 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, 2015
Objective: 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, Katie B, Tellor, Anastasia L, Armbruster   +2 more
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Design and synthesis of factor Xa inhibitors and their prodrugs

Bioorganic & Medicinal Chemistry Letters, 2003
In addition to our previously reported fluoro acrylamides Xa inhibitors 2 and 3, a series of potent and novel cyclic diimide amidine compounds has been identified. In efforts to improve their oral bioavailability, replacement of the amidine group with methyl amidrazone gives compounds of moderate potency (14, IC(50)=0.028 microM).
Yonghong, Song, Lane, Clizbe, Chhaya, Bhakta, Willy, Teng, Paul, Wong, Brian, Huang, Katherine, Tran, Uma, Sinha, Gary, Park, Andrea, Reed, Robert M, Scarborough, Bing Yan, Zhu   +11 more
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Nonbenzamidine compounds as selective factor xa inhibitors

Bioorganic & Medicinal Chemistry Letters, 2000
Nonbenzamidine compounds (imidazole, pyridine, pyrimidine, and thiazole derivatives) as selective serine protease factor Xa inhibitors are discussed.
W, He, B, Hanney, M R, Myers, A P, Spada, K, Brown, D, Colussi, V, Chu   +6 more
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1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa

Journal of Medicinal Chemistry, 2000
High-throughput screening of a combinatorial library of diamidophenols yielded lead compounds with the ability to inhibit human factor Xa (fXa) at micromolar concentrations (e.g. compound 4, fXa apparent K(ass) = 0.64 x 10(6) L/mol). SAR studies in this novel structural series of fXa inhibitors showed that the phenolic hydroxyl group was not essential ...
D K, Herron, T, Goodson, M R, Wiley, L C, Weir, J A, Kyle, Y K, Yee, A L, Tebbe, J M, Tinsley, D, Mendel, J J, Masters, J B, Franciskovich, J S, Sawyer, D W, Beight, A M, Ratz, G, Milot, S E, Hall, V J, Klimkowski, J H, Wikel, B J, Eastwood, R D, Towner, D S, Gifford-Moore, T J, Craft, G F, Smith   +22 more
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Apixaban: an emerging oral factor Xa inhibitor

Journal of Thrombosis and Thrombolysis, 2009
Apixaban, 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, Richard C, Becker   +1 more
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Rivaroxaban, an oral direct factor Xa inhibitor

Expert Opinion on Investigational Drugs, 2008
Rivaroxaban 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, Manesh R, Patel, Kenneth W, Mahaffey, Keith A A, Fox, Robert M, Califf   +4 more
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Novel factor Xa inhibitors: a patent review

Expert Opinion on Therapeutic Patents, 2009
New oral anticoagulants with favorable safety profiles and fixed doses are required for the management of thromboembolism and stroke prevention in patients with atrial fibrillation. Among them, fXa inhibitors (the so-called xabans) are attractive options that can overcome limitations (e.g., bleeding) of the current oral antithrombotic therapy.
DE CANDIA, MODESTO, ALTOMARE, Cosimo Damiano, LOPOPOLO G   +2 more
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Factor Xa inhibitors for acute coronary syndromes

Cochrane Database of Systematic Reviews, 2011
The 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, Agustín, Ciapponi, Joey, Kwong   +2 more
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