290832-34-7Relevant academic research and scientific papers
2-aryl indole derivative as antagonists of tachykinins
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Page/Page column 25, (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.
IL-8 receptor antagonists
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, (2008/06/13)
The present invention relates to novel compounds which inhibit the action of CXC chemokines, such as IL-8, Gro, NAP-2, ENA-78 etc., on their receptors, to the process for their preparation and to their use for obtaining drugs. According to the invention,
2-Aryl indole NK1 antagonists: Optimisation of the amide substituent
Shaw, Duncan,Chicchi, Gary G.,Elliott, Jason M.,Kurtz, Marc.,Morrison, Denise,Ridgill, Mark P.,Szeto, Nicola,Watt, Alan P.,Williams, Angela R.,Swain, Christopher J.
, p. 3031 - 3034 (2007/10/03)
The in vivo properties of a series of 2-arylindole NK1 antagonists have been improved, by modification of the amide substituent. The 1-(2-methoxyphenyl)piperazine amide was identified as a major area of metabolism in the lead compound 1. Replacement of this amine moiety by a 4-benzyl-4-hydroxypiperidine resulted in a compound 18 with reduced clearance and improved central duration of action.
2-Aryl indole NK1 receptor antagonists: Optimisation of indole substitution
Cooper, Laura C.,Chicchi, Gary G.,Dinnell, Kevin,Elliott, Jason M.,Hollingworth, Gregory J.,Kurtz, Marc M.,Locker, Karen L.,Morrison, Denise,Shaw, Duncan E.,Tsao, Kwei-Lan,Watt, Alan P.,Williams, Angela R.,Swain, Christopher J.
, p. 1233 - 1236 (2007/10/03)
The synthesis and biological evaluation of a series of 2-aryl indoles with high affinity for the human neurokinin-1 (hNK1) receptor are reported, concentrating on optimisation of the indole substitution.
