Novel Lactam NK1 Antagonists with Anti-Emetic Activity

GJ Hollingworth,EJ Carlson,JL Castro,GG Chicchi,N Clark,LC Cooper,O Dirat,J Di Salvo,JM Elliott,R Kilburn,MM Kurtz,W Rycroft,FD Tattersall, KL Tsao,CJ Swain

Bioorganic & medicinal chemistry letters（2006）

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摘要

A series of 4,4-disubstituted cyclohexylamine NK(1) antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.

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关键词

NK1,neurokinin,tachykinin,substance P,emesis,antiemetic,lactam

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