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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
8
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pubmed:dateCreated |
2011-4-21
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pubmed:abstractText |
Compound 4 (PF-04971729) belongs to a new class of potent and selective sodium-dependent glucose cotransporter 2 inhibitors incorporating a unique dioxa-bicyclo[3.2.1]octane (bridged ketal) ring system. In this paper we present the design, synthesis, preclinical evaluation, and human dose predictions related to 4. This compound demonstrated robust urinary glucose excretion in rats and an excellent preclinical safety profile. It is currently in phase 2 clinical trials and is being evaluated for the treatment of type 2 diabetes.
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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 |
Apr
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BianJianweiJ,
pubmed-author:Boustany-KariCarine MCM,
pubmed-author:BrandtThomasT,
pubmed-author:CollmanBenjamin MBM,
pubmed-author:KalgutkarAmit SAS,
pubmed-author:KlenoticMichelle KMK,
pubmed-author:LeiningerMichael TMT,
pubmed-author:LoweAndréA,
pubmed-author:MaguireRobert JRJ,
pubmed-author:MascittiVincentV,
pubmed-author:MastersonVictoria MVM,
pubmed-author:MaurerTristan STS,
pubmed-author:MiaoZhuangZ,
pubmed-author:MukaiyamaEmiE,
pubmed-author:PatelJigna DJD,
pubmed-author:PettersenJohn CJC,
pubmed-author:PrévilleCathyC,
pubmed-author:RobinsonRalph PRP,
pubmed-author:SamasBrianB,
pubmed-author:SobolZhannaZ,
pubmed-author:SteppanClaire MCM,
pubmed-author:StevensBenjamin DBD,
pubmed-author:SuppD MDM,
pubmed-author:ThumaBenjamin ABA,
pubmed-author:TugnaitMeeraM,
pubmed-author:UriAA,
pubmed-author:ZengDongxiangD
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pubmed:issnType |
Electronic
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pubmed:day |
28
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2952-60
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pubmed:meshHeading |
pubmed-meshheading:21449606-Animals,
pubmed-meshheading:21449606-Area Under Curve,
pubmed-meshheading:21449606-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:21449606-Crystallography, X-Ray,
pubmed-meshheading:21449606-Drug Discovery,
pubmed-meshheading:21449606-Drug Evaluation, Preclinical,
pubmed-meshheading:21449606-Humans,
pubmed-meshheading:21449606-Magnetic Resonance Spectroscopy,
pubmed-meshheading:21449606-Mass Spectrometry,
pubmed-meshheading:21449606-Models, Molecular,
pubmed-meshheading:21449606-Rats,
pubmed-meshheading:21449606-Sodium-Glucose Transporter 2
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pubmed:year |
2011
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pubmed:articleTitle |
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
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pubmed:affiliation |
Groton Laboratories, Pfizer Global Research & Development, Groton, Connecticut 06340, United States. vincent.mascitti@pfizer.com
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pubmed:publicationType |
Journal Article
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