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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.
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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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Mayo Clinic proceedings, 2019
OBJECTIVE To explore the efficacy and safety of direct oral factor Xa inhibitors in the treatment of cancer-associated acute venous thromboembolism (VTE).
H. Fuentes +6 more
semanticscholar +1 more source
OBJECTIVE To explore the efficacy and safety of direct oral factor Xa inhibitors in the treatment of cancer-associated acute venous thromboembolism (VTE).
H. Fuentes +6 more
semanticscholar +1 more source
2006
The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
Richard C. Becker, Frederick A. Spencer
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The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
Richard C. Becker, Frederick A. Spencer
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Isoxazolines and isoxazoles as factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2000AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
Ruth R. Wexler +7 more
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The Laryngoscope, 2018
To describe the characteristics and severity of epistaxis in patients taking factor Xa inhibitors novel anticoagulants.
E. Glikson +7 more
semanticscholar +1 more source
To describe the characteristics and severity of epistaxis in patients taking factor Xa inhibitors novel anticoagulants.
E. Glikson +7 more
semanticscholar +1 more source
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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Betrixaban – the next direct factor Xa inhibitor?
Expert Review of Hematology, 2016Venous thromboembolism is a major global health burden. Since the 1930s, prevention of stroke and pulmonary embolism in these patients has been achieved using conventional anticoagulants, such as heparin and warfarin. However, in recent years, four direct non-vitamin K antagonist oral anticoagulants (DOACs) have entered the market as alternative ...
Thoenes, Martin +4 more
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