|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0164209,
umls-concept:C0205177,
umls-concept:C0205250,
umls-concept:C0205314,
umls-concept:C0205531,
umls-concept:C0220781,
umls-concept:C0226896,
umls-concept:C0243076,
umls-concept:C0442027,
umls-concept:C0456387,
umls-concept:C0679622,
umls-concept:C1527415,
umls-concept:C1707689,
umls-concept:C1883254
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|
pubmed:issue |
5
|
|
pubmed:dateCreated |
2006-1-27
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|
pubmed:abstractText |
The discovery of a novel, achiral pyridine class of potent and orally active neurokinin-1 (NK(1)) receptor antagonists is described. The evaluation of this class is briefly outlined, leading to the identification of netupitant 21 and befetupitant 29, two new proprietary chemical entities with high affinity and excellent CNS penetration.
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|
pubmed:language |
eng
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pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
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|
pubmed:month |
Mar
|
|
pubmed:issn |
0960-894X
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|
pubmed:author |
pubmed-author:BösMichaelM,
pubmed-author:BallardTheresa MTM,
pubmed-author:GalleyGuidoG,
pubmed-author:GodelThierryT,
pubmed-author:HigginsGuy AGA,
pubmed-author:HoffmannTorstenT,
pubmed-author:HunkelerWalterW,
pubmed-author:PoliSonia MSM,
pubmed-author:SchniderPatrickP,
pubmed-author:SleightAndrew JAJ,
pubmed-author:StadlerHeinzH
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|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
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pubmed:pagination |
1362-5
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pubmed:meshHeading |
pubmed-meshheading:16332435-Administration, Oral,
pubmed-meshheading:16332435-Amines,
pubmed-meshheading:16332435-Animals,
pubmed-meshheading:16332435-CHO Cells,
pubmed-meshheading:16332435-Cricetinae,
pubmed-meshheading:16332435-Cross-Linking Reagents,
pubmed-meshheading:16332435-Drug Design,
pubmed-meshheading:16332435-Humans,
pubmed-meshheading:16332435-Molecular Structure,
pubmed-meshheading:16332435-Pyridines,
pubmed-meshheading:16332435-Pyrimidines,
pubmed-meshheading:16332435-Receptors, Neurokinin-1,
pubmed-meshheading:16332435-Sensitivity and Specificity,
pubmed-meshheading:16332435-Structure-Activity Relationship,
pubmed-meshheading:16332435-Substrate Specificity
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pubmed:year |
2006
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|
pubmed:articleTitle |
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
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|
pubmed:affiliation |
F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland. torsten.hoffmann@roche.com
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pubmed:publicationType |
Journal Article
|
