Discovery, synthesis and SAR of 2-acyl-1-biarylmethyl pyrazolidines, dual orexin receptor antagonists designed as fast and short-acting sleeping drugs

Author:

Surivet Jean-Philippe,Kessler Melanie,Vaillant Catherine,Aissaoui Hamed,Bezençon Olivier,Busch Louise,Kiry Manon,Lüthi Urs,Marck Nicolas,Masse Florence,Peters Jens-Uwe,Sweatman Catherine,Weigel Aude,Kohl Christopher

Publisher

Elsevier BV

Reference29 articles.

1. Twenty-three years of hypocretins: the “Rosetta Stone” of sleep/arousal circuits;de Lecea;Front Neurol Neurosci,2021

2. Discovery of [(2R,5R)-5-[(5-fluoropyridin-2-yl)oxy]methyl-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties;Coleman;ChemMedChem,2012

3. Discovery of (1R,2S)-2-30z-2-(3-fluorophenyl)-N-(5-fluor opyridin-2-yl)cyclopropanecarboxamide (E2006): a potent and efficacious oral orexin receptor antagonist;Yoshida;J Med Chem,2015

4. The quest for the best dual orexin receptor antagonist (daridorexant) for the treatment of insomnia disorders;Boss;ChemMedChem,2020

5. Hcccighlights of prescribing information of Belsomra, Dayvigo and Quviviq can be downloaded from the followings URLs respectively: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/204569s006lbl.pdf; https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212028s000lbl.pdf; https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214985s000lbl.pdf.

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