334477-38-2Relevant academic research and scientific papers
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK1 receptor antagonists
Sabbatini, Fabio M.,Fabio, Romano Di,Griffante, Cristiana,Pentassuglia, Giorgio,Zonzini, Laura,Melotto, Sergio,Alvaro, Giuseppe,Capelli, Anna M.,Pippo, Lara,Perdona', Elisabetta,Denis, Yves St.,Costa, Silvano,Corsi, Mauro
scheme or table, p. 623 - 627 (2010/06/12)
A focused exploration targeting conformationally restricted analogues of Vestipitant, resulted in the discovery of novel, in vitro potent NK1 antagonists. In particular, two of the compounds reported exhibited a good pharmacokinetic (PK) profile and produced anxiolytic-like effects in the gerbil foot tapping (GFT) in vivo model.
Novel lactam NK1 antagonists with anti-emetic activity
Hollingworth, Gregory J.,Carlson, Emma J.,Castro, José L.,Chicchi, Gary G.,Clark, Natalie,Cooper, Laura C.,Dirat, Olivier,Di Salvo, Jerry,Elliott, Jason M.,Kilburn, Ruth,Kurtz, Marc M.,Rycroft, Wayne,Tattersall, F. David,Tsao, Kwei-Lan,Swain, Christopher J.
, p. 1197 - 1201 (2007/10/03)
A series of 4,4-disubstituted cyclohexylamine NK1 antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.
Cyclohexane derivatives and their use as therapeutic agents
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Page 23, (2010/02/06)
The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
