4,4-disubstituted cyclohexylamine NK1 receptor antagonists I

被引：12
|
作者：
Elliott, JM
Castro, JL
Chicchi, GG
Cooper, LC
Dinnell, K
Hollingworth, GJ
Ridgill, MP
Rycroft, W
Kurtz, MM
Shaw, DE
Swain, CJ
Tsao, KL
Yang, LH
机构：
[1] Merck Sharp & Dohme Res Labs, Dept Med Chem, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England
[2] Merck Sharp & Dohme Res Labs, Dept Pharmacol, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England
[3] Merck Res Labs, Dept Biochem, Rahway, NJ 07065 USA
[4] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 13期
关键词：
D O I：
10.1016/S0960-894X(02)00249-4
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of novel 4,4-disubstituted cyclohexylamine based NK1 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. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1755 / 1758
页数：4
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