Spirocyclic NK1 antagonists I: [4.5] and [5.5]-Spiroketals

Eileen M Seward,Emma Carlson,Timothy Harrison,Karen E Haworth,Richard Herbert,Fintan J Kelleher,Marc M Kurtz,Jonathan Moseley,Simon N Owen,Andrew P Owens,Sharon J Sadowski,Christopher J Swain,Brian J Williams

Bioorganic & Medicinal Chemistry Letters（2002）

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摘要

A series of novel spiroketal-based NK1 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.

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