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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
9
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pubmed:dateCreated |
2011-4-25
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pubmed:abstractText |
In our ongoing efforts to develop CGRP receptor antagonists for the treatment of migraine, we aimed to improve upon telecagepant by targeting a compound with a lower projected clinical dose. Imidazoazepanes were identified as potent caprolactam replacements and SAR of the imidazole yielded the tertiary methyl ether as an optimal substituent for potency and hERG selectivity. Combination with the azabenzoxazinone spiropiperidine ultimately led to preclinical candidate 30 (MK-2918).
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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 |
May
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BurgeyChristopher SCS,
pubmed-author:DengJames ZJZ,
pubmed-author:KaneStefanie ASA,
pubmed-author:MosserScott DSD,
pubmed-author:NguyenDiem NDN,
pubmed-author:PaoneDaniel VDV,
pubmed-author:PotteigerCraig MCM,
pubmed-author:REESH BHBJr,
pubmed-author:RollerShaneS,
pubmed-author:SalvatoreChristopher ACA,
pubmed-author:SelnickHarold GHG,
pubmed-author:ShawAnthony WAW,
pubmed-author:VaccaJoseph PJP,
pubmed-author:WilliamsTheresa MTM
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pubmed:copyrightInfo |
Copyright © 2010 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 |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2683-6
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pubmed:meshHeading |
pubmed-meshheading:21251825-Analgesics, Non-Narcotic,
pubmed-meshheading:21251825-Animals,
pubmed-meshheading:21251825-Azepines,
pubmed-meshheading:21251825-Biological Availability,
pubmed-meshheading:21251825-Caprolactam,
pubmed-meshheading:21251825-Cells, Cultured,
pubmed-meshheading:21251825-Dogs,
pubmed-meshheading:21251825-Humans,
pubmed-meshheading:21251825-Imidazoles,
pubmed-meshheading:21251825-Inhibitory Concentration 50,
pubmed-meshheading:21251825-Macaca mulatta,
pubmed-meshheading:21251825-Migraine Disorders,
pubmed-meshheading:21251825-Molecular Structure,
pubmed-meshheading:21251825-Rats,
pubmed-meshheading:21251825-Receptors, Calcitonin Gene-Related Peptide,
pubmed-meshheading:21251825-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
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pubmed:affiliation |
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. daniel_paone@merck.com
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pubmed:publicationType |
Journal Article
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