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    TREATMENT OF AUTISM
    5.
    发明公开
    TREATMENT OF AUTISM 审中-公开

    公开(公告)号：EP3122363A4

    公开(公告)日：2017-11-08

    申请号：EP15769592

    申请日：2015-03-24

    申请人： SYNAPTEC DEV LLC

    发明人： DAVIS BONNIE M

    IPC分类号： A61K31/55 ,  A61P25/00

    CPC分类号： A61K31/55 ,  C07D491/06

    摘要： Autistic Spectrum Disorders (ASD) are a group of developmental disorders including autistic disorder, Asperger disorder and pervasive developmental disorder not otherwise specified which may be treated by use of a galanthamine analog wherein the hydroxy group of galantamine is replaced by a carbamate, carbonate or ester group and the metboxy group may be replaced by another alkoxy group of from two to six carbon atoms, a hydroxy group, hydrogen, an alkanoyloxy group or 2 to 10 carbon atoms, a benzoyloxy or substituted benzoyloxy group, a carbonate group of 1 to 10 carbon atoms or a carbamate group such as a mono alkyl or dialkyl or an aryl carbamate wherein the alkyl groups or aryl groups contain from 1 to 10 carbons, and the N-methyl group may be replaced by hydrogen, alkyl of 1 to 10 carbon atoms, benzyl, cyclopropylmethyl group or a substituted or unsubstituted benzoyloxy group. Galantamine mon-alkylcarbamates are particularly useful.

    2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES
    8.
    发明公开
    2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES 审中-公开
    2-氧杂-5-氮杂双环[2.2.1-]庚-3-基 - 衍生物

    公开(公告)号：EP3174886A1

    公开(公告)日：2017-06-07

    申请号：EP15742309.6

    申请日：2015-07-29

    申请人： F. Hoffmann-La Roche AG

    发明人： CECERE, Giuseppe ,  GALLEY, Guido ,  HU, Yimin ,  NORCROSS, Roger ,  PFLIEGER, Philippe ,  SHEN, Hong

    IPC分类号： C07D491/06 ,  A61K31/35 ,  A61K31/407 ,  A61P25/28

    CPC分类号： C07D491/08 ,  C07D491/06

    摘要： 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.

    摘要翻译： 本发明涉及式（I）化合物，其中L是一个键，-C（O）NH-，-NHC（O） - ， - CH 2 NHC（O） - ，CH 2 C（O）NH-， - CH 2 NH- ，-NH-或-NHC（O）NH-; R 1是氢，低级烷基，卤素，低级烷氧基 - 烷基，被卤素取代的低级烷氧基，被卤素取代的低级烷基或是选自吡啶基，嘧啶基，吡嗪基或吡唑基的苯基或杂芳基，其中苯基和杂芳基是 任选地被一个，两个或三个选自卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基，被卤素取代的低级烷氧基，环烷基或O-CH 2 - 环烷基取代的取代基取代; 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，注意力缺陷多动障碍（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，紊乱和体温动态平衡失调，睡眠障碍和昼夜节律，以及心血管疾病。