4, 4-Disubstituted cyclohexylamine NK 1 receptor antagonists I

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

Index: 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

Full Text: HTML

Citation Number: 11

Abstract

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.