1396756-47-0Relevant articles and documents
SUBSTITUTED PROLINES / PIPERIDINES AS OREXIN RECEPTOR ANTAGONISTS
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, (2013/08/28)
The present invention is directed to compounds that can modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists
Jiang, Rong,Song, Xinyi,Bali, Purva,Smith, Anthony,Bayona, Claudia Ruiz,Lin, Li,Cameron, Michael D.,McDonald, Patricia H.,Kenny, Paul J.,Kamenecka, Theodore M.
, p. 3890 - 3894 (2012/07/13)
A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.