290830-49-8Relevant academic research and scientific papers
2-aryl indole derivative as antagonists of tachykinins
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Page/Page column 32, (2008/06/13)
The present invention relates to compounds of the formula (I): wherein R1a, R1b, R2, R3, R4, R5, X and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
2-Aryl indole NK1 receptor antagonists: Optimisation of the 2-aryl ring and the indole nitrogen substituent
Dinnell, Kevin,Chicchi, Gary G.,Dhar, Madhumeeta J.,Elliott, Jason M.,Hollingworth, Gregory J.,Kurtz, Marc M.,Ridgill, Mark P.,Rycroft, Wayne,Tsao, Kwei-Lan,Williams, Angela R.,Swain, Christopher J.
, p. 1237 - 1240 (2007/10/03)
Novel 2-aryl indole hNK1 receptor ligands were prepared utilising palladium cross-coupling chemistry of a late intermediate as a key step. Compounds with high hNK1 receptor binding affinity and good brain penetration (e.g., 9d) were synthesised.
