Results 261 to 270 of about 644,115 (313)
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HIP International, 2020
Introduction: Debate over the ideal agent for venous thromboembolism (VTE) prophylaxis after total hip arthroplasty (THA) has led to changes in prescribing trends of commonly used agents. We investigate variation in utilisation and the differences in VTE
Abiram Bala +6 more
semanticscholar +1 more source
Introduction: Debate over the ideal agent for venous thromboembolism (VTE) prophylaxis after total hip arthroplasty (THA) has led to changes in prescribing trends of commonly used agents. We investigate variation in utilisation and the differences in VTE
Abiram Bala +6 more
semanticscholar +1 more source
, 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. Hara, T. Nagahara
openaire +1 more source
Expert Opinion on Therapeutic Patents, 1999
The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X1 -YIR-X2, wherein X1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are
Pavel Safar +6 more
openaire +2 more sources
The invention provides compounds which specifically inhibit factor Xa activity. The compounds consist of the structure X1 -YIR-X2, wherein X1 is H, acyl, alkyl, acylalkyl, arylalkyl or one or more amino acids, and X2 is a modified C-terminal group, one or more carboxy-protecting groups or one or more amino acids or other substituent, and Y, I and R are
Pavel Safar +6 more
openaire +2 more sources
Anthranilamide inhibitors of factor Xa
Bioorganic & Medicinal Chemistry Letters, 2007SAR 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.
Jeffry Bernard Franciskovich +20 more
openaire +3 more sources
Rivaroxaban: An Oral Factor Xa Inhibitor
Clinical Therapeutics, 2013Currently available anticoagulants utilized for venous thromboembolism (VTE) treatment and prevention and stroke prevention in patients with atrial fibrillation (AF) have proven effectiveness but are not optimally utilized because of barriers such as the need for subcutaneous administration and requisite routine laboratory monitoring.
Valerie S. Ganetsky +2 more
openaire +3 more sources
Heterogeneity of Synthetic Factor Xa Inhibitors
Current Pharmaceutical Design, 2005Heparins and vitamin K antagonists are the landmarks of antithrombotic treatment. Both of them were discovered by serendipity; they are multi-targeted drugs and share several limitations. New molecules have been designed in order to be both more selective concerning their biological target and more homogeneous in their biochemical structure aiming at ...
Grigoris T. Gerotziafas +1 more
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Sulfonamidolactam inhibitors of coagulation factor Xa
Bioorganic & Medicinal Chemistry Letters, 2008As 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
Suanne Nakajima +13 more
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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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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 +2 more sources
Phenyltriazolinones as potent factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2010We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.
Steven Sheriff +12 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
Timothy A. Brighton +2 more
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