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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2010-2-3
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pubmed:abstractText |
The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The basic pyrrolidine amine was intentionally converted to a sulfonamide, carbamate, or amide to address these liabilities. The evaluation of the degree of partial agonism for these non-basic pyrrolidine derivatives and demonstration of their efficacy in an in vivo model of endometriosis is disclosed herein.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AzzaranoLeonard MLM,
pubmed-author:BartonLinda SLS,
pubmed-author:BrayJeffrey DJD,
pubmed-author:DuraiswamiChayaC,
pubmed-author:FrazeeJames SJS,
pubmed-author:GrygielkoEugene TET,
pubmed-author:HammondMarlysM,
pubmed-author:HoangTram HTH,
pubmed-author:JohnsonLatishaL,
pubmed-author:KallanderLara SLS,
pubmed-author:LapingNicholas JNJ,
pubmed-author:LuQingQ,
pubmed-author:MadaussKevin PKP,
pubmed-author:NagillaRakeshR,
pubmed-author:PattersonJaclyn RJR,
pubmed-author:StewartEugene LEL,
pubmed-author:StoyPatrickP,
pubmed-author:ThompsonScott KSK,
pubmed-author:WashburnDavid GDG,
pubmed-author:WilliamsShawn PSP,
pubmed-author:XuXiaopingX
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
371-4
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pubmed:meshHeading |
pubmed-meshheading:19926282-Animals,
pubmed-meshheading:19926282-Binding Sites,
pubmed-meshheading:19926282-Carbamates,
pubmed-meshheading:19926282-Crystallography, X-Ray,
pubmed-meshheading:19926282-Endometriosis,
pubmed-meshheading:19926282-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:19926282-Female,
pubmed-meshheading:19926282-Humans,
pubmed-meshheading:19926282-Pyrrolidines,
pubmed-meshheading:19926282-Rats,
pubmed-meshheading:19926282-Receptors, Progesterone,
pubmed-meshheading:19926282-Sulfonamides
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pubmed:year |
2010
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pubmed:articleTitle |
Improving the developability profile of pyrrolidine progesterone receptor partial agonists.
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pubmed:affiliation |
Department of Chemistry, Metabolic Pathways Centre for Excellence in Drug Discovery, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA. lara.s.kallander@gsk.com
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pubmed:publicationType |
Journal Article
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