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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
18
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pubmed:dateCreated |
2010-8-30
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pubmed:abstractText |
The synthesis of a novel series of iminoheterocycles and their structure-activity relationship (SAR) as modulators of gamma-secretase activity will be detailed. Encouraging SAR generated from a monocyclic core led to a structurally unique bicyclic core. Selected compounds exhibit good potency as gamma-secretase modulators, excellent rat pharmacokinetics, and lowering of Abeta42 levels in various in vivo models.
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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 |
Sep
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BaraThomasT,
pubmed-author:BennettChad ECE,
pubmed-author:BuevichAlexeiA,
pubmed-author:BurnettDuane ADA,
pubmed-author:CaldwellJohn PJP,
pubmed-author:ChuInhouI,
pubmed-author:Cohen-WilliamsMaryM,
pubmed-author:HydeLynnL,
pubmed-author:JonesG CGCJr,
pubmed-author:JoseinHubertH,
pubmed-author:LeeJulieJ,
pubmed-author:MazzolaRobert DRD,
pubmed-author:McCrackenTroy MTM,
pubmed-author:McKittrickBrianB,
pubmed-author:TerracinaGiuseppeG,
pubmed-author:VoigtJohannesJ,
pubmed-author:ZhangLiliL,
pubmed-author:ZhuZhaoningZ
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pubmed:copyrightInfo |
Copyright (c) 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
5380-4
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pubmed:meshHeading |
pubmed-meshheading:20724152-Alzheimer Disease,
pubmed-meshheading:20724152-Amyloid Precursor Protein Secretases,
pubmed-meshheading:20724152-Amyloid beta-Peptides,
pubmed-meshheading:20724152-Animals,
pubmed-meshheading:20724152-Bicyclo Compounds, Heterocyclic,
pubmed-meshheading:20724152-Brain,
pubmed-meshheading:20724152-Humans,
pubmed-meshheading:20724152-Imines,
pubmed-meshheading:20724152-Mice,
pubmed-meshheading:20724152-Mice, Transgenic,
pubmed-meshheading:20724152-Peptide Fragments,
pubmed-meshheading:20724152-Rats,
pubmed-meshheading:20724152-Structure-Activity Relationship
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pubmed:year |
2010
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pubmed:articleTitle |
Iminoheterocycles as gamma-secretase modulators.
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pubmed:affiliation |
Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, United States. john.caldwell@merck.com
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pubmed:publicationType |
Journal Article
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