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公开(公告)号：US20130005988A1
公开(公告)日：2013-01-03
申请号：US13609553
申请日：2012-09-11
IPC分类号： C07D207/09 , C07D207/10
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.
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公开(公告)号：US08357712B2
公开(公告)日：2013-01-22
申请号：US13033645
申请日：2011-02-24
IPC分类号： A61K31/421 , C07D263/08
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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.
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公开(公告)号：US08586617B2
公开(公告)日：2013-11-19
申请号：US11872203
申请日：2007-10-15
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 。
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4.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
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。
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公开(公告)号：US08729113B2
公开(公告)日：2014-05-20
申请号：US13033645
申请日：2011-02-24
IPC分类号： A61K31/421 , C07D263/08
CPC分类号： A61K31/421 , A61K31/47 , C07D263/48 , C07D401/12 , C07D413/12 , C07F7/081
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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R1，R2，X，Y和n在本说明书中定义及其药学上可接受的酸加成盐。 本发明还提供药物组合物和这种化合物的制造方法。 这些化合物可用于治疗与微量胺相关受体的生物功能有关的疾病，这些疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，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，药物滥用和代谢障碍，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失调，睡眠障碍 昼夜节律和心血管疾病。
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公开(公告)号：US20120165294A1
公开(公告)日：2012-06-28
申请号：US13410315
申请日：2012-03-02
IPC分类号： A61K31/421 , C07F7/10 , A61K31/695 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/08 , A61P25/06 , A61P9/12 , A61P25/30 , A61P3/00 , A61P3/04 , A61P3/10 , A61P3/06 , A61P9/00 , A61P25/16 , C07D263/28
CPC分类号： C07D263/28 , C07D413/12
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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R1，R2，X，Y和n在本说明书中定义及其药学上可接受的酸加成盐。 本发明还提供药物组合物和这种化合物的制造方法。 这些化合物可用于治疗与微量胺相关受体的生物功能有关的疾病，这些疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，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，药物滥用和代谢障碍，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失调，睡眠障碍 昼夜节律和心血管疾病。
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公开(公告)号：US20100041686A1
公开(公告)日：2010-02-18
申请号：US12504702
申请日：2009-07-17
IPC分类号： A61K31/506 , C07D263/28 , C07F7/10 , A61K31/421 , C07D403/12
CPC分类号： C07D263/28 , C07D413/12
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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.
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8.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
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。
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公开(公告)号：US20080096906A1
公开(公告)日：2008-04-24
申请号：US11872192
申请日：2007-10-15
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。
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公开(公告)号：US08242153B2
公开(公告)日：2012-08-14
申请号：US12558772
申请日：2009-09-14
IPC分类号： A61K31/421 , C07D263/08
CPC分类号： A61K31/421 , A61K31/47 , C07D263/48 , C07D401/12 , C07D413/12 , C07F7/081
摘要： The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and 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R1，R2，X，Y和n在本说明书中定义及其药学上可接受的酸加成盐。 本发明还提供药物组合物和这种化合物的制造方法。 这些化合物可用于治疗与微量胺相关受体的生物功能有关的疾病，这些疾病是抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，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，药物滥用和代谢障碍，进食障碍，糖尿病，糖尿病并发症，肥胖症，血脂异常，能量消耗和同化障碍，体温平衡失调和失调，睡眠障碍 昼夜节律和心血管疾病。
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