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Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals
Eileen M Seward1, Emma Carlson, Timothy Harrison
1Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK. eileen_seward@merck.com
Bioorganic & Medicinal Chemistry Letters
|August 17, 2002
Abstract:
A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.