Source:http://linkedlifedata.com/resource/pubmed/id/20650636
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
17
|
| pubmed:dateCreated |
2010-8-16
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| pubmed:abstractText |
A series of (3R,4R)-pyrrolidine-3,4-dicarboxylic acid amides was investigated with respect to their factor Xa inhibitory activity, selectivity, pharmacokinetic properties, and ex vivo antithrombotic activity. The clinical candidate from this series, R1663, exhibits excellent selectivity against a panel of serine proteases and good pharmacokinetic properties in rats and monkeys. A Phase I clinical study with R1663 has been finalized.
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| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
1464-3405
|
| pubmed:author |
pubmed-author:AnselmLilliL,
pubmed-author:BannerDavid WDW,
pubmed-author:BenzJörgJ,
pubmed-author:HaapWolfgangW,
pubmed-author:HilpertHansH,
pubmed-author:HimberJacquesJ,
pubmed-author:HuberWalterW,
pubmed-author:KuhnBerndB,
pubmed-author:MaryJean-LucJL,
pubmed-author:OttenederMichael BMB,
pubmed-author:PandayNarendraN,
pubmed-author:RicklinFabienneF,
pubmed-author:StahlMartinM,
pubmed-author:ThomiStefanS,
pubmed-author:ZbindenKatrin GroebkeKG
|
| pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
|
| pubmed:issnType |
Electronic
|
| pubmed:day |
1
|
| pubmed:volume |
20
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
5313-9
|
| pubmed:meshHeading | |
| pubmed:year |
2010
|
| pubmed:articleTitle |
Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.
|
| pubmed:affiliation |
F. Hoffmann-La Roche Ltd, Pharma Research, Basel, Switzerland.
|
| pubmed:publicationType |
Journal Article
|