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    Aminomethyl-4-imidazoles
    2.
    发明授权
    Aminomethyl-4-imidazoles 失效
    氨基甲基-4-咪唑

    公开(公告)号：US08586617B2

    公开(公告)日：2013-11-19

    申请号：US11872203

    申请日：2007-10-15

    申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A61K31/417 ,  C07D233/64

    CPC分类号： C07D233/64

    摘要： The present invention relates to amino-4-methyl imidazoles and pharmaceutically-acceptable salts thereof. The compound 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.

    摘要翻译： 本发明涉及氨基-4-甲基咪唑及其药学上可接受的盐。 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），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病， 癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病 。

    2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as TAAR-ligands
    3.
    发明授权
    2-azetidinemethaneamines and 2-pyrrolidinemethaneamines as TAAR-ligands 失效
    2-氮杂环丁烷甲烷胺和2-吡咯烷甲烷胺作为TAAR-配体

    公开(公告)号：US08389507B2

    公开(公告)日：2013-03-05

    申请号：US12176456

    申请日：2008-07-21

    申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A01N43/00 ,  A61K31/397

    CPC分类号： C07D205/04 ,  C07D207/09

    摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful 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.

    摘要翻译： 本发明涉及其中R 1，R 2，R 3，Ar，n和o如本文所定义的式I化合物及其药学上可接受的活性盐。 式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，尤其对于TAAR1，可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病性 诸如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默氏病，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，肥胖症，血脂异常，能量消耗和同化障碍等疾病 ，体温平衡紊乱和失眠，睡眠障碍和昼夜节律，以及心血管疾病。

    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS
    4.
    发明申请
    2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 失效
    2-氨基乙酰胺和2-吡咯烷基磺酰胺作为TAAR-LIGANDS

    公开(公告)号：US20090029962A1

    公开(公告)日：2009-01-29

    申请号：US12176456

    申请日：2008-07-21

    申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A61K31/397 ,  C07D207/09 ,  C07D205/04 ,  A61K31/40

    CPC分类号： C07D205/04 ,  C07D207/09

    摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful 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.

    摘要翻译： 本发明涉及其中R 1，R 2，R 3，Ar，n和o如本文所定义的式I化合物及其药学上可接受的活性盐。 式I化合物对微量胺相关受体（TAAR）具有良好的亲和力，尤其对于TAAR1，可用于治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍（ADHD），应激相关疾病，精神病性 诸如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默氏病，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，肥胖症，血脂异常，能量消耗和同化障碍等疾病 ，体温平衡紊乱和失眠，睡眠障碍和昼夜节律，以及心血管疾病。

    AMINOMETHYL-2-IMIDAZOLES
    5.
    发明申请
    AMINOMETHYL-2-IMIDAZOLES 审中-公开
    氨基-2-咪唑烷

    公开(公告)号：US20080096906A1

    公开(公告)日：2008-04-24

    申请号：US11872192

    申请日：2007-10-15

    申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A61K31/506 ,  A61K31/4178 ,  A61P25/18 ,  A61P25/28 ,  A61P3/04 ,  C07D233/61 ,  C07D401/12 ,  C07D403/12 ,  C07D233/66 ,  A61P3/10 ,  A61P25/30 ,  A61P25/24 ,  A61K31/4439

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12

    摘要： The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen or lower alkyl; R2 is hydrogen, lower alkyl, lower alkenyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, —(CH2)x—S-lower alkyl, —(CH2)x—O-lower alkyl, —(CH2)x—NHC(O)O-lower alkyl, —(CH2)x-aryl, and —(CH2)x-heteroaryl; each R3 is selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, halogen, hydroxy, lower alkyl substituted by halogen, —O—(CH2)m-aryl, —O—(CH2)m-heteroaryl, —(CR2)m-aryl, and —(CR2)m-heteroaryl; each R is selected from the group consisting of hydrogen, lower alkyl and hydroxy; Ar is selected from the group consisting of phenyl, pyrimidin-2-yl, pyrimidin-4-yl and pyridin-3-yl; n is 0, 1 or 2; x is 0, 1, 2 or 3; m is 0 or 1; and to their pharmaceutically active salts.

    摘要翻译： 本发明涉及式I化合物，其中R 1选自氢或低级烷基; R 2是氢，低级烷基，低级烯基，被羟基取代的低级烷基，被卤素取代的低级烷基， - （CH 2） -S-低级烷基， - （CH 2）2 - 低级烷基， - （CH 2 2）x - （O）O - 低级烷基， - （CH 2）x - 芳基，和 - （CH 2 2） >杂芳基; 每个R 3选自氢，低级烷基，低级烷氧基，卤素，羟基，被卤素取代的低级烷基，-O-（CH 2 CH 2） - （CH 2）2 - 芳基， - （CH 2）2 - 亚芳基， - （CR 2） m - 芳基和 - （CR 2）m - 杂芳基; 每个R选自氢，低级烷基和羟基; Ar选自苯基，嘧啶-2-基，嘧啶-4-基和吡啶-3-基; n为0,1或2; x为0,1,2或3; m为0或1; 和其药物活性盐。

    AMINOMETHYL-4-IMIDAZOLES
    6.
    发明申请
    AMINOMETHYL-4-IMIDAZOLES 失效
    氨基甲基-4-咪唑烷

    公开(公告)号：US20080119535A1

    公开(公告)日：2008-05-22

    申请号：US11872203

    申请日：2007-10-15

    申请人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Annick Goergler ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A61K31/417 ,  C07D233/64 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P25/06 ,  A61P3/10

    CPC分类号： C07D233/64

    摘要： The present invention relates to amino-4-methyl imidazoles and pharmaceutically-acceptable salts thereof.The compound 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.

    摘要翻译： 本发明涉及氨基-4-甲基咪唑及其药学上可接受的盐。 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），应激相关疾病，精神病性精神障碍如精神分裂症，神经系统疾病如帕金森病，神经变性疾病如阿尔茨海默病， 癫痫，偏头痛，高血压，药物滥用和代谢障碍如进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡紊乱和失调，睡眠和昼夜节律紊乱以及心血管疾病 。

    Substituted-2-imidazoles
    10.
    发明授权
    Substituted-2-imidazoles 失效
    取代的2-咪唑

    公开(公告)号：US07834044B2

    公开(公告)日：2010-11-16

    申请号：US11931246

    申请日：2007-10-31

    申请人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    发明人： Guido Galley ,  Katrin Groebke Zbinden ,  Roger Norcross ,  Henri Stalder

    IPC分类号： A61K31/427 ,  A61K31/47 ,  C07D215/02 ,  C07D403/06

    CPC分类号： C07D413/06 ,  C07D401/06 ,  C07D403/06

    摘要： The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH2— and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds. The invention relates also to processes for preparing such compounds, compositions comprising such a compound or a pharmaceutically-acceptable acid addition salt thereof, and a method of treating a disease or disorder in a patient comprising administering such a compound, or pharmaceutically-acceptable acid addition salt thereof, to a patient in need of such treatment.

    摘要翻译： 本发明涉及式I化合物，其中R 1选自氢和低级烷基; 每个R 2独立地选自氢和低级烷基; 每个R 3独立地选自氢，低级烷基，低级烷氧基，苯氧基，苄氧基，卤素和被卤素取代的低级烷基; X选自-CH 2 - ， - CH-和-O-; Y选自-CH 2 - ， - CH-和键，条件是当X是-O-时，Y可能不是键; Z选自-CH 2 - 和-CH-; m为0,1或2; 且n为0,1或2; 以及这些化合物的药学上可接受的酸加成盐。 本发明还涉及制备这种化合物的方法，包含这种化合物或其药学上可接受的酸加成盐的组合物，以及治疗患者疾病或病症的方法，包括给予这种化合物或药学上可接受的酸加成 其盐，需要这种治疗的患者。