Results 281 to 290 of about 644,115 (313)

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).
Willy Teng, Robert M. Scarborough, Katherine Tran, Paul W. Wong, Gary Park, Lane A. Clizbe, Uma Sinha, Andrea Reed, Brian Huang, Chhaya Bhakta, Yonghong Song, Bing Yan Zhu   +11 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.
Joey Kwong, Viviana Brito, Agustín Ciapponi   +2 more
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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.
Christopher D. Ellis, Patrick Y.S. Lam, Matthew R. Wright, Robert M. Knabb, Karen A. Rossi, Mimi L. Quan, Ming Y. He, Ruth R. Wexler, Ann Y. Liauw, Joseph M. Luettgen, Pancras C. Wong   +10 more
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Synthesis a novel inhibitor of factor Xa

2011 International Conference on Remote Sensing, Environment and Transportation Engineering, 2011
Inappropriate thrombus formation in blood vessels causes cardiovascular disease (myocardial infarction, stroke, pulmonary embolism and so on) which is the most common cause of mortality at present. Fxa is an important factor in blood coagulation cascade. It is an effective and safe method to treat blood coagulation diseases by inhibiting FXa to control
Shen An Xiong, Yang Gen Sheng
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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 ...
Richard A. Engh, R. Kucznierz, Marzenell K, Leinert H, Frank Grams, von der Saal W   +5 more
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Inhibitors of Thrombin and Factor Xa

2000
In medicine today, much effort is being made to develop new protease inhibitors for use as anticoagulants in multiple disease states. Deep venous thrombosis and pulmonary embolism, in particular, are major medical problems in the developed world. Similarly, myocardial infarction, stroke, and peripheral vascular disease are arterial thromboses for which
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[Heparin, thrombin and Factor Xa inhibitors].

Hamostaseologie, 2004
Direct and indirect coagulation inhibitors are used to inhibit the activity of the serine proteases of the coagulation system. Indirect inhibitors act via antithrombin and heparin cofactor II. The main representatives are heparins, lowmolecular-weight heparins, fondaparinux, idraparinux and danaparoid.
T Fenyvesi, J Harenberg
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Clinical and Experimental Experience with Factor Xa Inhibitors

American Journal of Cardiovascular Drugs, 2004
Cardiovascular disease is the major cause of mortality in the industrial world today. We are constantly moving towards new and better ways of fighting this epidemic. Advances have been made in various fields such as patient education, imaging techniques, interventional cardiology, and novel therapeutic agents.
Valentin Fuster, Juan J. Badimon, Juan Gaztanaga, Juan F. Viles-Gonzalez, Urooj Zafar   +4 more
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Fondaparinux, the first selective factor Xa inhibitor

Current Opinion in Hematology, 2003
Fondaparinux (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.
Michael R. Lassen, Alexander G.G. Turpie, Bengt I. Eriksson, Kenneth A. Bauer   +3 more
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Nonbenzamidine tetrazole derivatives as factor Xa inhibitors

Bioorganic & Medicinal Chemistry Letters, 2003
Factor 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.
Richard S. Alexander, Ann Y. Liauw, Francis J. Woerner, Patrick Y.S. Lam, Matthew R. Wright, Robert M. Knabb, Ming Y. He, Ruth R. Wexler, Mimi L. Quan, Joseph M. Luettgen, Pancras C. Wong, Christopher D. Ellis   +11 more
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