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    • 3. 发明申请
      WO2016016292A1 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES 审中-公开
    • 2-OXA-5-AZABICYCLO[2.2.1]HEPTAN-3-YL DERIVATIVES
    • 2-OXA-5-AZABICYCLO [2.2.1] HEPTAN-3-YL衍生物
    • WO2016016292A1
    • 2016-02-04
    • PCT/EP2015/067353
    • 2015-07-29
    • F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
    • CECERE, Giuseppe , GALLEY, Guido , HU, Yimin , NORCROSS, Roger , PFLIEGER, Philippe , SHEN, Hong
    • C07D491/06 , A61K31/35 , A61K31/407 , A61P25/28
    • C07D491/08 , C07D491/06
    • The present invention relates to compounds of formula (I), wherein L is a bond, -C(O)NH-, -NHC(O)-, -CH 2 NHC(O)-, CH 2 C(O)NH-, -CH 2 NH-, -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-CH 2 -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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 4. 发明申请
      WO2015181061A1 5-OXA-2-AZABICYCLO[2.2.2]OCTAN-4-YL AND 5-OXA-2-AZABICYCLO[2.2.1]HEPTAN-4-YL DERIVATIVES AS TAAR1 MODULATORS 审中-公开
    • 5-OXA-2-AZABICYCLO[2.2.2]OCTAN-4-YL AND 5-OXA-2-AZABICYCLO[2.2.1]HEPTAN-4-YL DERIVATIVES AS TAAR1 MODULATORS
    • 5-OXA-2-甲氨喋呤[2.2.2] OCT-4-YL和5-OXA-2-氮杂双环[2.2.1] HEPTAN-4-YL衍生物作为TAAR1调节剂
    • WO2015181061A1
    • 2015-12-03
    • PCT/EP2015/061348
    • 2015-05-22
    • F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
    • CECERE, Giuseppe , GALLEY, Guido , HU, Yimin , NORCROSS, Roger , PFLIEGER, Philippe , SHEN, Hong
    • C07D491/08 , A61K31/5386 , A61P25/00
    • C07D491/08
    • The invention relates to compounds of formula (I) wherein.....C.....is -CH 2 - or -CH 2 -CH 2 -; X is -NH-, -C(0)NH- or -NHC(0)NH-; Ar is phenyl or a 5 or 6-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 cycloalkyl, lower alkoxy substituted by halogen or is cycloalkyl; -( )- is -CH 2 -; n is 0 or 1; m is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof, to all racemic mixtures, all their corresponding enantiomers and/or optical isomers, which compounds 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.
    • 本发明涉及式（I）的化合物，其中..... C .....是-CH 2 - 或-CH 2 -CH 2 - ; X是-NH-，-C（O）NH-或-NHC（O）NH-; Ar是苯基或含有一个或两个N原子的5或6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，被环烷基取代的低级烷氧基，被卤素取代的低级烷氧基或是环烷基; - （） - 是-CH 2 - ; n为0或1; m为0,1或2; 或其药学上合适的酸加成盐，适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，该化合物可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD） 压力相关疾病，精神障碍，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，药物滥用，代谢紊乱，进食障碍，糖尿病，糖尿病并发症，肥胖，血脂异常，能量消耗障碍 和体温平衡的同化，紊乱和功能障碍，睡眠和昼夜节律紊乱以及心血管疾病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      WO2016030310A1 SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS 审中-公开
    • SUBSTITUTED AZETIDINE DERIVATIVES AS TAAR LIGANDS
    • 取代的AZETIDINE DERIVATIVES作为TAAR LIGANDS
    • WO2016030310A1
    • 2016-03-03
    • PCT/EP2015/069315
    • 2015-08-24
    • F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
    • CECERE, Giuseppe , GALLEY, Guido , NORCROSS, Roger , PFLIEGER, Philippe , RAUBER, Etienne
    • C07D205/04 , C07D401/12 , C07D403/12 , A61K31/4155 , A61K31/4427 , A61K31/505 , A61P25/00
    • C07D403/12 , C07D205/04 , C07D401/12
    • The present invention relates to a compound of formula I wherein R 1 is hydrogen, methoxy or fluoro; R 2 /R 2' are independently from each other hydrogen, methoxy or fluoro; R 3 /R 4 are independently from each other hydrogen or halogen; R is hydrogen or fluoro; L 1 is -CH 2 -, -NR'-, -0-, -S-, CF 2 - or CH=; R' is hydrogen or lower alkyl; L 2 is a bond, -C(0)NH-, -NH-, -CH 2 NHC(O)-, -NHC(O)- or -NHC(0)NH-; R is hydrogen, halogen, lower alkoxy, cyano or is phenyl optionally substituted by one or more substituents, selected from halogen, lower alkyl substituted by halogen or lower alkoxy, or is a five or six membered heteroaryl, selected from pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl or pyrazolyl, which heteroaryls are optionally substituted by one or more substituents, selected from halogen, lower alkyl, lower alkoxy, cyano, cycloalkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or by phenyl substituted by halogen; N is a ring nitrogen atom in position 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. The compounds of formulas I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and may be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as 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.
    • 本发明涉及式Ⅰ化合物，其中R1是氢，甲氧基或氟; R2 / R2'彼此独立地为氢，甲氧基或氟; R3 / R4彼此独立地为氢或卤素; R是氢或氟; L 1是-CH 2 - ， - NR' - ， - O - ， - S - ，CF 2 - 或CH = R'是氢或低级烷基; L 2是键，-C（O）NH - ， - NH - ， - CH 2 NHC（O） - ， - NHC（O） - 或-NHC（O）NH-; R为氢，卤素，低级烷氧基，氰基或任选被一个或多个选自卤素，被卤素或低级烷氧基取代的低级烷基取代基取代的苯基，或为选自吡啶基，嘧啶基，吡嗪基的五或六元杂芳基 哒嗪基或吡唑基，该杂芳基任选被一个或多个选自卤素，低级烷基，低级烷氧基，氰基，环烷基，被卤素取代的低级烷基，被卤素取代的低级烷氧基或被卤素取代的苯基取代的取代基取代; N是1或2位的环氮原子; 或其药学上合适的酸加成盐。 式I的化合物对微量胺相关受体（TAAR）具有良好的亲和力，特别是TAAR1，可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意力缺陷多动障碍（ADHD），应激相关疾病 精神分裂症如精神分裂症，神经系统疾病如帕金森病，神经退行性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢性疾病如进食障碍，糖尿病，糖尿病并发症，肥胖，血脂异常，能量消耗障碍 和体温平衡的同化，紊乱和功能障碍，睡眠和昼夜节律紊乱以及心血管疾病。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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