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rdf:type |
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lifeskim:mentions |
umls-concept:C0002482,
umls-concept:C0006948,
umls-concept:C0205177,
umls-concept:C0205531,
umls-concept:C0205549,
umls-concept:C0226896,
umls-concept:C0243077,
umls-concept:C0379528,
umls-concept:C0442027,
umls-concept:C0559956,
umls-concept:C1527415,
umls-concept:C1880355
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-9
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pubmed:abstractText |
The design of amide and heteroaryl amide isosteres as replacements for the carbamate substructure in previously disclosed 2,6-disubstituted piperidine N-arylsulfonamides is described. In several cases, amides lessened CYP liabilities in this class of gamma-secretase inhibitors. Selected compounds showed significant reduction of Abeta levels upon oral dosing in a transgenic murine model of Alzheimer's disease.
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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:ChuInhouI,
pubmed-author:CladerJohn WJW,
pubmed-author:Del VecchioRobert ARA,
pubmed-author:FavreauLeonardL,
pubmed-author:GreenleeWilliam JWJ,
pubmed-author:HydeLynn ALA,
pubmed-author:JonesG CGCJr,
pubmed-author:McBriarMark DMD,
pubmed-author:NomeirAmin AAA,
pubmed-author:ParkerEric MEM,
pubmed-author:PissarnitskiDmitri ADA,
pubmed-author:ZhangLiliL,
pubmed-author:ZhaoZhiqiangZ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
215-9
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:17988864-Amides,
pubmed-meshheading:17988864-Amyloid Precursor Protein Secretases,
pubmed-meshheading:17988864-Amyloid beta-Peptides,
pubmed-meshheading:17988864-Animals,
pubmed-meshheading:17988864-Carbamates,
pubmed-meshheading:17988864-Cytochrome P-450 Enzyme System,
pubmed-meshheading:17988864-Heterocyclic Compounds,
pubmed-meshheading:17988864-Mice,
pubmed-meshheading:17988864-Oxadiazoles,
pubmed-meshheading:17988864-Piperidines,
pubmed-meshheading:17988864-Protease Inhibitors,
pubmed-meshheading:17988864-Rats,
pubmed-meshheading:17988864-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
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pubmed:affiliation |
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. mark.mcbriar@spcorp.com
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pubmed:publicationType |
Journal Article
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