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1. 发明申请

US20130005988A1 2-AZETIDINEMETHANEAMINES AND 2-PYRROLIDINEMETHANEAMINES AS TAAR-LIGANDS 审中-公开
公开(公告)号：US20130005988A1
公开(公告)日：2013-01-03
申请号：US13609553
申请日：2012-09-11
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： 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.

2. 发明申请

US20120071506A1 METHODS FOR TREATING CNS DISORDERS WITH BICYCLO-SUBSTITUTED 2-IMIDAZOLINE AND 2-IMIDAZOLES 审中-公开
标题翻译：用双相取代的2-咪唑啉和2-咪唑烷处理CNS病症的方法
公开(公告)号：US20120071506A1
公开(公告)日：2012-03-22
申请号：US13303465
申请日：2011-11-23
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： A61K31/4709 , A61K31/4178 , C07D401/04 , C07D401/06 , C07D405/04 , C07D233/60 , C07D233/58 , C07D233/20 , A61P25/20 , C07D233/06 , C07D233/24 , C07D405/06 , C07D233/22 , A61P25/24 , A61P25/22 , A61P25/18 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/08 , A61P25/06 , A61P9/12 , A61P25/30 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06 , A61P43/00 , A61P9/00 , A61K31/4164
CPC分类号： C07D233/56 , A61K31/4166 , A61K31/4174 , A61K31/4709 , C07D233/06 , C07D233/20 , C07D233/22 , C07D233/64 , C07D401/04 , C07D401/06 , C07D405/04
摘要： The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, 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 which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms. The invention also relates to novel compounds of formula I, compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及一种治疗选自抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病性精神分裂症，神经性疾病如帕金森病，神经变性疾病如阿尔茨海默病，癫痫，偏头痛，高血压，药物滥用和代谢紊乱，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其包括向个体施用治疗有效量的式I化合物，其中R 1，R 2，Q，W，X，Y，m和n如说明书中所定义，以及它们的药学活性盐，外消旋混合物，对映体，光学异构体和互变异构体。本发明还涉及式I的新化合物，含有它们的组合物及其制备方法。

3. 发明授权

US07902238B2 2-aminooxazolines as TAAR1 ligands 有权
标题翻译： 2-氨基恶唑啉作为TAAR1配体
公开(公告)号：US07902238B2
公开(公告)日：2011-03-08
申请号：US12028028
申请日：2008-02-08
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： A61K31/42 , C07D263/28
CPC分类号： C07D263/28 , C07D413/06
摘要： The invention relates to compounds of formula wherein R1, R2, and R3 are as defined herein and to a pharmaceutically suitable acid addition salts thereof for the treatment of CNS disorders.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2和R 3如本文所定义，及其药学上合适的酸加成盐，用于治疗CNS病症。

4. 发明申请

US20120004230A1 IMIDAZOLE DERIVATIVES 失效
标题翻译：咪唑衍生物
公开(公告)号：US20120004230A1
公开(公告)日：2012-01-05
申请号：US13235542
申请日：2011-09-19
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： A61K31/4174 , C07D233/64 , C07D413/10 , C07D405/12 , C07D233/88 , A61P25/22 , A61K31/5377 , A61K31/4178 , A61P25/00 , A61P25/24 , A61P25/18 , A61P25/16 , C07D233/58 , A61K31/4164
CPC分类号： C07D233/64
摘要： The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1.The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound.The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.
摘要翻译：本发明涉及对微量胺相关受体（TAAR）具有良好亲和力的咪唑衍生物，特别是TAAR1。本发明还涉及上述化合物的药学上合适的酸加成盐。本发明还涉及包含如上所述的咪唑衍生物或其药学上合适的酸加成盐的组合物及其制备方法。

5. 发明授权

US07834044B2 Substituted-2-imidazoles 失效
标题翻译：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。

6. 发明申请

US20100120864A1 2-AMINOOXAZOLINES AS TAAR1 LIGANDS 审中-公开
标题翻译： 2-AMINOOXAZOLINES as TAAR1 LIGANDS
公开(公告)号：US20100120864A1
公开(公告)日：2010-05-13
申请号：US12639076
申请日：2009-12-16
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： A61K31/4439 , A61K31/421 , C07D263/08 , C07D413/02 , A61P25/00 , A61P3/00 , A61P9/00
CPC分类号： C07D263/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07F7/0812
摘要： The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include 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：本发明涉及其中X，Y，R 1，R 2和n如本文所定义或其药学上合适的酸加成盐的式I化合物。本发明还涉及含有这些化合物的药物组合物和用于治疗与微量胺相关受体的生物功能相关的疾病的方法，所述疾病包括抑郁症，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，药物滥用和代谢紊乱，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，体温稳态，睡眠障碍和昼夜节律，以及心血管疾病。

7. 发明申请

US20080261920A1 2-Aminooxazolines as TAAR1 ligands 审中-公开
标题翻译： 2-氨基恶唑烷作为TAAR1配体
公开(公告)号：US20080261920A1
公开(公告)日：2008-10-23
申请号：US12011384
申请日：2008-01-25
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： A61K31/421 , A61K31/4439 , A61K31/695 , C07D263/28 , C07D413/04 , C07F7/02 , A61P9/00
CPC分类号： C07D263/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07F7/0812
摘要： The invention relates to compounds of formula I wherein X, Y, R1, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include 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X，Y，R 1，R 2和n如本文所定义，或其药学上合适的酸加成盐。本发明还涉及含有这些化合物的药物组合物和用于治疗与微量胺相关受体的生物功能相关的疾病的方法，所述疾病包括抑郁症，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，药物滥用和代谢紊乱，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，体温稳态，睡眠障碍和昼夜节律，以及心血管疾病。

8. 发明申请

US20120196903A1 2-AMINOOXAZOLINES AS TAAR1 LIGANDS 有权
标题翻译： 2-AMINOOXAZOLINES as TAAR1 LIGANDS
公开(公告)号：US20120196903A1
公开(公告)日：2012-08-02
申请号：US13426736
申请日：2012-03-22
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： A61K31/421 , C07D413/04 , A61K31/4439 , A61P25/24 , A61P25/22 , A61P25/00 , A61P25/18 , A61P25/16 , A61P25/28 , A61P25/08 , A61P25/06 , A61P25/30 , A61P3/00 , A61P3/10 , A61P3/04 , A61P3/06 , A61P9/00 , C07D263/28
CPC分类号： C07D263/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07F7/0812
摘要： The invention relates to compounds of formula I wherein X, Y, R′, R2, and n are as defined herein or to a pharmaceutically suitable acid addition salt thereof. The invention also relates to pharmaceutical compositions containing such compounds and methods for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases include 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：本发明涉及其中X，Y，R'，R 2和n如本文所定义或其药学上合适的酸加成盐的式I化合物。本发明还涉及含有这些化合物的药物组合物和用于治疗与微量胺相关受体的生物功能相关的疾病的方法，所述疾病包括抑郁症，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，药物滥用和代谢紊乱，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，体温稳态，睡眠障碍和昼夜节律，以及心血管疾病。

9. 发明申请

US20110281871A1 TAAR1 LIGANDS 审中-公开
标题翻译： TAAR1配偶
公开(公告)号：US20110281871A1
公开(公告)日：2011-11-17
申请号：US13190510
申请日：2011-07-26
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： A61K31/5377 , A61K31/4545 , A61K31/4439 , A61K31/44 , A61K31/166 , C07D401/14 , C07D401/04 , C07D401/12 , C07D413/04 , C07D213/78 , C07C233/66 , A61K31/496 , C07D405/14
CPC分类号： C07D213/80 , C07C233/66 , C07D213/82 , C07D235/08 , C07D401/12 , C07D405/12
摘要： The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The 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 CNS disorders.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，X，L，W，n和o在本文中定义及其药学上合适的酸加成盐，但以下化合物6-（4-甲基 - 哌嗪（CAS 199478-31-4），N-（3,4-二氯 - 苄基）-3-氟 - 苯甲酰胺（CAS 424815-98-5），N-（4 - 氯 - 苄基）-3-氟 - 苯甲酰胺（CAS 544661-83-8），N-（3-氯 - 苄基）-3-氟 - 苯甲酰胺（CAS 796051-07-5）和N-苯乙基-6 - 苯基氨基 - 烟酰胺（CAS 571913-74-1）。式I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CNS疾病。

10. 发明授权

US07875645B2 Method for the treatment of CNS disorders with substituted 2-imidazoles or imidazole derivatives 失效
标题翻译：用取代的2-咪唑或咪唑衍生物治疗CNS障碍的方法
公开(公告)号：US07875645B2
公开(公告)日：2011-01-25
申请号：US11655468
申请日：2007-01-19
申请人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
发明人： Guido Galley , Katrin Groebke Zbinden , Marius Hoener , Sabine Kolczewski , Roger Norcross , Henri Stalder
IPC分类号： A61K31/415 , C07D233/56
CPC分类号： C07D233/06 , A61K31/4164 , A61K31/4178 , C07D233/20 , C07D233/22 , C07D233/56 , C07D233/64 , C07D401/10 , C07D403/06 , C07D405/06 , C07D409/06
摘要： The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, 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 which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
摘要翻译：本发明涉及治疗抑郁症，焦虑障碍，双相情感障碍，注意缺陷多动障碍，应激相关障碍，精神病如精神分裂症，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，其包括给予个体治疗有效量的式I化合物，其中R，R 1，R 2，A和n如说明书中所定义，并且其药物活性盐。本发明还涉及式I的新型化合物，含有它们的药物组合物及其制备方法。

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