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Bioorg Med Chem Lett. 2010 Jul 15;20(14):4201-5. doi: 10.1016/j.bmcl.2010.05.047. Epub 2010 May 25.

Discovery of 3,9-diazabicyclo[4.2.1]nonanes as potent dual orexin receptor antagonists with sleep-promoting activity in the rat.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, Sumneytown Pike, West Point, PA 19486, United States. paul_coleman@merck.com

Abstract

Orexins are excitatory neuropeptides that regulate arousal and sleep. Orexin receptor antagonists promote sleep and offer potential as a new therapy for the treatment of insomnia. In this Letter, we describe the synthesis of constrained diazepanes having a 3,9 diazabicyclo[4.2.1]nonane bicyclic core with good oral bioavailability and sleep-promoting activity in a rat EEG model.

PMID:
20610153
DOI:
10.1016/j.bmcl.2010.05.047
[Indexed for MEDLINE]

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