Spirocyclic NK₁ antagonists II: [4.5]-spiroethers

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• 作者：Williams ; Brian J. ; Cascieri ; Margaret A. ; Chicchi ; Gary G. ; Harrison ; Timothy ; Owens ; Andrew P. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2002
• 出版时间：October 7, 2002
• 年：2002
• 卷：12
• 期：1
• 页码：2719-2722
• 全文大小：117 K

文摘

A series of novel spiroether-based neurokinin-1 (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.