[EN] 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES<br/>[FR] DÉRIVÉS DU 2-OXA -5-AZABICYCLO [2.2.1] HEPTAN -3-YL
申请人:HOFFMANN LA ROCHE
公开号:WO2016016292A1
公开(公告)日:2016-02-04
The present invention relates to compounds of formula (I), wherein L is a bond, -C(O)NH-, -NHC(O)-, -CH2NHC(O)-, CH2C(O)NH-, -CH2NH-, -NH- or -NHC(O)NH-; R1 is hydrogen, lower alkyl, halogen, lower alkoxy-alkyl, lower alkoxy substituted by halogen, lower alkyl substituted by halogen or is phenyl or heteroaryl selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl or pyrazolyl, and wherein phenyl and heteroaryl are optionally substituted by one, two or three substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cycloalkyl or O-CH2-cycloalkyl; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
本发明涉及以下化合物的公式(I),其中L是键,-C(O)NH-,-NHC(O)-,-CH2NHC(O)-,CH2C(O)NH-,-CH2NH-,-NH-或-NHC(O)NH-;R1是氢,较低的烷基,卤素,较低的烷氧基烷基,受卤素取代的较低的烷氧基,受卤素取代的较低的烷基或为苯基或杂环芳基,所述苯基和杂环芳基从吡啶基、嘧啶基、吡啉基或吡唑基中选择,其中苯基和杂环芳基可以选择地被来自卤素、较低的烷基、较低的烷氧基、受卤素取代的较低的烷基、受卤素取代的较低的烷氧基、环烷基或O-CH2-环烷基的一个、两个或三个取代基取代;或其药用合适的酸盐,所有的消旋混合物,它们所有对应的对映体和/或光学异构体,可用于治疗抑郁症、焦虑症、躁郁症、注意力缺陷多动障碍(ADHD)、与压力有关的障碍、精神病性障碍、精神分裂症、神经疾病、帕金森病、神经退行性疾病、阿尔茨海默病、癫痫、偏头痛、高血压、物质滥用、代谢障碍、进食障碍、糖尿病、糖尿病并发症、肥胖症、血脂异常、能量消耗和吸收障碍、体温稳态障碍、睡眠和昼夜节律障碍、心血管障碍。