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4, 4-Disubstituted cyclohexylamine NK 1 receptor antagonists I

…, JL Castro, GG Chicchi, LC Cooper, K Dinnell…

文献索引:Elliott, Jason M; Castro, Jose L; Chicchi, Gary G; Cooper, Laura C; Dinnell, Kevin; Hollingworth, Gregory J; Ridgill, Mark P; Rycroft, Wayne; Kurtz, Marc M; Shaw, Duncan E; Swain, Christopher J; Tsao, Kwei-Lan; Yang, Lihu Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 13 p. 1755 - 1758

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被引用次数: 11

摘要

A series of novel 4, 4-disubstituted cyclohexylamine based NK1 antagonists is described. The effect of changes to the C1–C4 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.