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Novel lactam NK1 antagonists with anti-emetic activity
Authors:Hollingworth Gregory J  Carlson Emma J  Castro José L  Chicchi Gary G  Clark Natalie  Cooper Laura C  Dirat Olivier  Salvo Jerry Di  Elliott Jason M  Kilburn Ruth  Kurtz Marc M  Rycroft Wayne  Tattersall F David  Tsao Kwei-Lan  Swain Christopher J
Affiliation:Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. greg_hollingworth@merck.com
Abstract:
A series of 4,4-disubstituted cyclohexylamine NK(1) antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.
Keywords:
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