4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.

Bioorg Med Chem Lett

Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK.

Published: July 2002

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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http://dx.doi.org/10.1016/s0960-894x(02)00249-4DOI Listing

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