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    • 11. 发明申请
    • MORPHOLIN-PYRIDINE DERIVATIVES
    • 吗啉 - 吡啶衍生物
    • WO2015165835A1
    • 2015-11-05
    • PCT/EP2015/059002
    • 2015-04-27
    • F. HOFFMANN-LA ROCHE AGHOFFMANN-LA ROCHE INC.
    • GALLEY, GuidoPFLIEGER, PhilippeNORCROSS, RogerCECERE, GiuseppeSHEN, HongHU, Yimin
    • C07D413/12A61K31/4245A61P25/00
    • C07D413/04C07D413/12C07D413/14
    • The present invention relates to compounds of formula (I) wherein X is CR or N; R is hydrogen, halogen or lower alkyl; L is a bond, -C(O)- or -C(O)NH-; Ar is phenyl or a five or six membered heteroaryl group, containing one or two N atoms; R 1 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or cycloalkyl; n is 0, 1, 2 or 3; 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.
    • 本发明涉及其中X为CR或N的式(I)化合物; R是氢,卤素或低级烷基; L是键,-C(O) - 或-C(O)NH-; Ar是苯基或含有一个或两个N原子的五或六元杂芳基; R1是卤素,低级烷基,被卤素取代的低级烷基,低级烷氧基,被卤素或环烷基取代的低级烷氧基; n为0,1,2或3; 或其药学上合适的酸加成盐,可用于所有外消旋混合物,其所有相应的对映异构体和/或光学异构体,其可用于治疗抑郁症,焦虑症,双相情感障碍,注意缺陷多动障碍(ADHD),应激 相关疾病,精神病,精神分裂症,神经系统疾病,帕金森病,神经变性疾病,阿尔茨海默病,癫痫,偏头痛,高血压,物质滥用,代谢紊乱,进食障碍,糖尿病,糖尿病并发症,肥胖症,血脂异常,能量障碍, 同化,紊乱和体温平衡失调,睡眠障碍和昼夜节律,以及心血管疾病。