4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I |
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| Authors: | Elliott Jason M Castro Jose L Chicchi Gary G Cooper Laura C Dinnell Kevin Hollingworth Gregory J Ridgill Mark P Rycroft Wayne Kurtz Marc M Shaw Duncan E Swain Christopher J Tsao Kwei-Lan Yang Lihu |
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| Affiliation: | Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. jason_elliot@merck.com |
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| Abstract: | ![]()
A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action. |
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