Results 201 to 210 of about 38,154 (222)
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Apixaban: an Oral Direct Factor-Xa Inhibitor
Advances in Therapy, 2012Apixaban is a highly selective, reversible, direct factor Xa inhibitor that inhibits both free factor Xa and prothrombinase activity, and clot-bound factor Xa activity. A predictable pharmacokinetic profile, multiple pathways of elimination, an improved bleeding profile relative to warfarin with a lack of other significant adverse events, and no need ...
David, Jiménez +2 more
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1,2-Dibenzamidobenzene Inhibitors of Human Factor Xa
Journal of Medicinal Chemistry, 2000High-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 +22 more
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Isoxazolines and isoxazoles as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 20003,4,5-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
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Nonbenzamidine compounds as selective factor xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2000Nonbenzamidine compounds (imidazole, pyridine, pyrimidine, and thiazole derivatives) as selective serine protease factor Xa inhibitors are discussed.
W, He +6 more
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Novel factor Xa inhibitors: a patent review
Expert Opinion on Therapeutic Patents, 2009New 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 +2 more
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Fondaparinux, the first selective factor Xa inhibitor
Current Opinion in Hematology, 2003Fondaparinux (Arixtra, Sanofi-Synthelabo, Paris, France) is a pentasaccharide that selectively inhibits factor Xa; it is the first of a new class of synthetic antithrombotic agents. Fondaparinux has a linear pharmacokinetic profile allowing once-daily subcutaneous administration.
Alexander G G, Turpie +3 more
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Nonbenzamidine tetrazole derivatives as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2003Factor 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, inhibition of fXa has potential therapeutic applications in the treatments of both arterial and venous thrombosis.
Mimi L, Quan +11 more
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Factor Xa inhibitors (Berlex).
IDrugs : the investigational drugs journal, 2005Berlex Biosciences is investigating several series of Factor Xa inhibitors aimed at the prevention and treatment of thrombotic disorders [297584]. Some compounds are based on the structure of ZK-805412, a Z,Z-2,7-bis(dibenzylidene)cycloheptanone, which showed nanomolar Factor Xa inhibitor potency [301618].
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