Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia.

Autor: Xiong Y; Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. yxiong@arenapharm.com, Ullman B, Choi JS, Cherrier M, Strah-Pleynet S, Decaire M, Feichtinger K, Frazer JM, Yoon WH, Whelan K, Sanabria EK, Grottick AJ, Al-Shamma H, Semple G
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Mar 01; Vol. 22 (5), pp. 1870-3. Date of Electronic Publication: 2012 Jan 28.
DOI: 10.1016/j.bmcl.2012.01.080
Abstrakt: A series of fused bicyclic heterocycles was identified as potent and selective 5-HT(2A) receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties, and significant improvements on deep sleep (delta power) and sleep consolidation.
(Copyright © 2012 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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