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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
12
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pubmed:dateCreated |
2002-5-31
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pubmed:abstractText |
Further optimization of the beta-aminoester class of factor Xa (fXa) inhibitors is described culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with excellent in vivo anticoagulant activity. An X-ray structure of FXV673 bound to human fXa is also presented. Based on its selectivity, potent in vivo activity and favorable pre-clinical safety profile, FXV673 was selected for further development and is currently undergoing clinical trials.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BentleyRoss GRG,
pubmed-author:BrownKaren DKD,
pubmed-author:CheneyDaniel LDL,
pubmed-author:ChuValeriaV,
pubmed-author:ColussiDennis JDJ,
pubmed-author:CzekajMarkM,
pubmed-author:DunwiddieChristopher TCT,
pubmed-author:GardnerCharles JCJ,
pubmed-author:GongYongY,
pubmed-author:GuertinKevin RKR,
pubmed-author:GuilloteauJean-PierreJP,
pubmed-author:HeranChristopher LCL,
pubmed-author:KleinScott ISI,
pubmed-author:LeadleyRobert JRJ,
pubmed-author:MaignanSebastianS,
pubmed-author:MorganSuzanne RSR,
pubmed-author:PaulsHenry WHW,
pubmed-author:SpadaAlfred PAP,
pubmed-author:ZulliAllison LAL
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pubmed:issnType |
Print
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pubmed:day |
17
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1671-4
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:12039587-Anticoagulants,
pubmed-meshheading:12039587-Crystallography, X-Ray,
pubmed-meshheading:12039587-Cyclic N-Oxides,
pubmed-meshheading:12039587-Esters,
pubmed-meshheading:12039587-Factor Xa,
pubmed-meshheading:12039587-Humans,
pubmed-meshheading:12039587-Models, Molecular,
pubmed-meshheading:12039587-Molecular Structure,
pubmed-meshheading:12039587-Pyridines,
pubmed-meshheading:12039587-Serine Proteinase Inhibitors
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pubmed:year |
2002
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pubmed:articleTitle |
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
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pubmed:affiliation |
Drug Innovation and Approval, Aventis Pharmaceuticals, Route 202-206, Bridgewater, NJ 08807, USA. kevin.guertin@roche.com
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pubmed:publicationType |
Journal Article
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