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Identification of fused bicyclic heterocycles as potent and selective 5-HT(2A) receptor antagonists for the treatment of insomnia |
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| Authors: | Xiong Yifeng Ullman Brett Choi Jin-Sun Karoline Cherrier Martin Strah-Pleynet Sonja Decaire Marc Feichtinger Konrad Frazer John M Yoon Woo H Whelan Kevin Sanabria Erin K Grottick Andrew J Al-Shamma Hussien Semple Graeme |
| Affiliation: | Arena Pharmaceuticals Inc., 6166 Nancy Ridge Drive, San Diego, CA 92121, USA. yxiong@arenapharm.com |
| Abstract: | 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. |
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