17-08-2017 дата публикации
Номер: US20170233385A1
Принадлежит:
The present invention discloses a series of piperidine derivatives as orexin receptor antagonists and compositions thereof, and relates to the application thereof in preparing medications for the treatment of insomnia, chronic obstructive pulmonary disease, obstructive sleep apnea, hypersomnia, anxiety, obsessive-compulsive disorder, panic attack, nicotine addiction, or binge eating disorder. 6. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein the 5-6 membered cyclohydrocarbyl or heterocyclic group are each independently selected from phenyl claim 1 , pyridyl claim 1 , furyl claim 1 , thienyl claim 1 , thiazolyl claim 1 , pyrimidinyl claim 1 , pyrazolyl claim 1 , 1 claim 1 ,2 claim 1 ,3-triazolyl or 1 claim 1 ,2 claim 1 ,5-triazolyl.11. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein Y is selected from —CH—O-E or —O-E claim 1 , wherein E is defined as in .15. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein U claim 1 , X claim 1 , and G are independently selected from NH or N—Calkyl.16. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , and Rare independently selected from H claim 1 , methyl claim 1 , or fluoro.17. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently selected from H claim 1 , methyl claim 1 , fluoro or cyclopropyl.18. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rtogether form 3-8 membered cycloalkyl;{'sub': 2', '3, 'specifically, Rand Rtogether form a cyclopropyl.'}19. The compound of or the pharmaceutically acceptable salt thereof claim 1 , wherein Calkyl is selected from methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , or hexyl claim 1 , wherein propyl claim 1 , butyl claim 1 , pentyl claim 1 , or hexyl is optionally cyclized or partially cyclized.21. A pharmaceutical ...
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