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Front Cover: The Quest for the Best Dual Orexin Receptor Antagonist (Daridorexant) for the Treatment of Insomnia Disorders (ChemMedChem 23/2020)
ChemMedChem ( IF 3.4 ) Pub Date : 2020-11-19 , DOI: 10.1002/cmdc.202000881
Christoph Boss 1 , John Gatfield 1 , Christine Brotschi 1 , Bibia Heidmann 1 , Thierry Sifferlen 1 , Markus Raumer 1 , Gunther Schmidt 1 , Jodi T. Williams 1 , Alexander Treiber 1 , Catherine Roch 1
Affiliation  

The Front Cover illustrates a circadian rhythm accompanied by daridorexant, Idorsia′s dual orexin receptor antagonist (DORA), investigated for the treatment of insomnia. It represents the quest for a DORA that would provide the next‐day benefits of a fully restorative night. The team at Idorsia set‐out to design a compound that antagonizes both orexin receptors, has a rapid onset of effect, and a duration of action sufficient for the night but short enough to avoid any negative residual activity the following morning, at optimally effective doses. The authors describe how these efforts resulted in daridorexant, a DORA which has recently successfully completed Phase 3 clinical studies. Good night insomnia! Artwork by Markenfels AG. More information can be found in the Full Paper by Christoph Boss et al.
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中文翻译:

寻求最佳的双重Orexin受体拮抗剂(Daridorexant),用于治疗失眠症

前盖说明了昼夜节律,并伴有daridorexant(一种针对Idorsia的双重orexin受体拮抗剂(DORA)),用于治疗失眠症。它代表了对DORA的追求,该DORA将提供完全恢复性夜晚的第二天收益。Idorsia的研究小组着手设计一种能拮抗两种食欲素受体,起效迅速,作用持续时间足以过夜的药物,但时间短得足以避免次日早晨出现任何残留残留活性的化合物(最佳剂量) 。作者描述了这些努力如何导致daridorexant(DORA)最近成功完成了3期临床研究。晚安失眠!Markenfels AG的作品。可以在Christoph Boss等人的《全文》中找到更多信息。
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更新日期:2020-12-03
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