Results 261 to 270 of about 655,147 (306)

Sulfonamidolactam inhibitors of coagulation factor Xa

Bioorganic & Medicinal Chemistry Letters, 2008
As part of an effort to identify novel backups for previously reported pyrazole-based coagulation Factor Xa inhibitors, the pyrazole 5-carboxamide moiety was replaced by 3-(sulfonylamino)-2-piperidone. This led to the identification of a structurally diverse chemotype that was further optimized to incorporate neutral or weakly basic aryl and heteroaryl
Joanne M, Smallheer, Shuaige, Wang, Mia L, Laws, Suanne, Nakajima, Zilun, Hu, Wei, Han, Irina, Jacobson, Joseph M, Luettgen, Karen A, Rossi, Alan R, Rendina, Robert M, Knabb, Ruth R, Wexler, Patrick Y S, Lam, Mimi L, Quan   +13 more
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Tetrahydro-isoquinoline-Based Factor Xa Inhibitors

Journal of Medicinal Chemistry, 1998
Derivatives 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, F, Grams, H, Leinert, K, Marzenell, R A, Engh, W, von der Saal   +5 more
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The direct factor Xa inhibitor rivaroxaban

Medical Journal of Australia, 2009
Warfarin 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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Factor Xa inhibitors

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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Epistaxis in the setting of antithrombotic therapy: A comparison between factor Xa inhibitors, warfarin, and antiplatelet agents

The Laryngoscope, 2018
To describe the characteristics and severity of epistaxis in patients taking factor Xa inhibitors novel anticoagulants.
E. Glikson, Uri Chavkin, O. Madgar, D. Sagiv, G. Nakache, A. Yakirevitch, M. Wolf, E. Alon   +7 more
semanticscholar   +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 ...
S. Kunitada, T. Nagahara, T. Hara
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Nonbenzamidine isoxazoline derivatives as factor Xa inhibitors

Bioorganic & Medicinal Chemistry Letters, 2003
Factor 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, Christopher D, Ellis, Ming Y, He, Ann Y, Liauw, Patrick Y S, Lam, Karen A, Rossi, Robert M, Knabb, Joseph M, Luettgen, Matthew R, Wright, Pancras C, Wong, Ruth R, Wexler   +10 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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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
openaire   +2 more sources