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61. 发明申请

US20090227628A1 2-AMINOQUINOLINES 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US20090227628A1
公开(公告)日：2009-09-10
申请号：US12394083
申请日：2009-02-27
申请人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/4709 , C07D215/38 , A61K31/47 , A61P25/24 , A61P25/22 , A61P25/00
CPC分类号： C07D215/38 , C07D405/12
摘要： The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式I的2-氨基喹啉衍生物，其中Z，R 1和Ar 1如本文所定义，含有它们的药物组合物，其制备方法。这些化合物是5-HT5A受体拮抗剂，可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍如帕金森病，精神病或胃肠疾病。

62. 发明授权

US07452909B2 Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US07452909B2
公开(公告)日：2008-11-18
申请号：US10926670
申请日：2004-08-26
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
IPC分类号： A61K31/4439 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.
摘要翻译：本发明涉及式I的咪唑衍生物，其中R 1，R 2，R 3，R 4，，X，Y和R如上所述，或其药学上可接受的盐。本发明还涉及药物组合物，其包含式I的咪唑衍生物，制备式I化合物的方法，以及治疗或预防急性和/或慢性神经障碍的方法，其包括向需要这种治疗的患者施用和/或预防治疗有效量的所述药物组合物。这些疾病包括阿尔茨海默氏病。这些疾病也包括轻度认知障碍。

63. 发明申请

US20080269256A1 PYRIDINE-2-CARBOXYAMIDE DERIVATIVES 审中-公开
标题翻译：吡啶-2-羧酰胺衍生物
公开(公告)号：US20080269256A1
公开(公告)日：2008-10-30
申请号：US12165758
申请日：2008-07-01
申请人： Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
发明人： Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
IPC分类号： A61K31/4439 , C07D401/14 , C07D417/02 , A61P25/00 , A61K31/506 , A61K31/444
CPC分类号： C07D213/81 , A61K9/2018 , A61K9/4858 , C07D401/12 , C07D409/12 , C07D417/12
摘要： The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
摘要翻译：本发明涉及式I化合物：其中R 1至R 3如本说明书中所定义，其制备方法，含有它们的药物组合物和治疗CNS疾病的方法。

64. 发明授权

US07414060B2 Pyridine-2-carboxyamide derivatives 有权
标题翻译：吡啶-2-甲酰胺衍生物
公开(公告)号：US07414060B2
公开(公告)日：2008-08-19
申请号：US11360085
申请日：2006-02-23
申请人： Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
发明人： Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
IPC分类号： C07D401/14 , A61K31/4436
CPC分类号： C07D213/81 , A61K9/2018 , A61K9/4858 , C07D401/12 , C07D409/12 , C07D417/12
摘要： The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
摘要翻译：本发明涉及式I化合物：其中R 1至R 3如本说明书中所定义，其制备方法，含有它们的药物组合物和治疗CNS疾病的方法。

65. 发明申请

US20080103306A1 IMIDAZOLE DERIVATIVES 有权
标题翻译：咪唑衍生物
公开(公告)号：US20080103306A1
公开(公告)日：2008-05-01
申请号：US11955421
申请日：2007-12-13
申请人： Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
发明人： Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
IPC分类号： C07D401/04 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to process for the preparation of an imidazole derivative of formula I, wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain.
摘要翻译：本发明涉及制备式I咪唑衍生物的方法，其中R 1，R 2，R 3和R 3， SUP> 4 如上所述。这些化合物可用于治疗或预防mGluR5受体介导的疾病。这些化合物尤其用于治疗或预防急性和/或慢性神经障碍，例如精神病，癫痫，精神分裂症，阿尔茨海默病，认知障碍和记忆缺陷以及慢性和急性疼痛。

66. 发明申请

US20070197569A1 Method for treating central nervous system disorders with substituted 2-imidazoline derivatives 审中-公开
标题翻译：用取代的2-咪唑啉衍生物治疗中枢神经系统障碍的方法
公开(公告)号：US20070197569A1
公开(公告)日：2007-08-23
申请号：US11655484
申请日：2007-01-19
申请人： Marius Hoener , Sabine Kolczewski , Henri Stalder
发明人： Marius Hoener , Sabine Kolczewski , Henri Stalder
IPC分类号： A61K31/415 , A61K31/505 , C07D233/44 , C07D239/02
CPC分类号： A61K31/4164 , A61K31/4168 , A61K31/4174
摘要： The present invention relates to a method for treating 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 which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, X, A, and n are as defined in the specification and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms thereof.
摘要翻译：本发明涉及一种治疗抑郁症，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向个体施用治疗有效量的式I化合物，其中R，X，A和n如说明书中所定义，以及药学活性盐，外消旋混合物，对映异构体，旋光异构体及其互变异构形式。

67. 发明申请

US20070105891A1 Thiazole[4,5-C]pyridine derivatives 失效
标题翻译：噻唑[4,5-C]吡啶衍生物
公开(公告)号：US20070105891A1
公开(公告)日：2007-05-10
申请号：US11590087
申请日：2006-10-31
申请人： Georg Jaeschke , Sabine Kolczewski , Richard Porter , Patrick Schnider , Eric Vieira
发明人： Georg Jaeschke , Sabine Kolczewski , Richard Porter , Patrick Schnider , Eric Vieira
IPC分类号： C07D498/02 , A61K31/4745
CPC分类号： C07D513/04
摘要： The invention relates to compounds of general formula I: wherein R1, R2 and R3 are as defined in the description such compounds are metabotropic glutamate receptor antagonists and are useful in the treatment or prevention of mGluR5 receptor mediated disorders.
摘要翻译：本发明涉及通式I的化合物：其中R 1，R 2和R 3如本说明书所定义，这样的化合物是代谢型谷氨酸受体拮抗剂，可用于治疗或预防mGluR5受体介导的病症。

68. 发明授权

US07153874B2 Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US07153874B2
公开(公告)日：2006-12-26
申请号：US10795619
申请日：2004-03-08
申请人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
发明人： Bernd Buettelmann , Simona Maria Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Hugh Philip Porter , Eric Vieira
IPC分类号： A61K31/4439 , A61K31/4178 , C07D401/06
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention provides 4-[1-Aryl-imidazol-4-ylethynyl]-2-alkyl-pyridine and 1-heteroaryl-imidazol-4-ylethynyl]-2-alkyl-pyridine derivatives and pharmaceutically acceptable salts thereof for the treatment or prevention of disorders mediated in full or in part by metabotropic glutamate receptor 5. These disorders include, e.g. acute, traumatic and chronic degenerative processes of the nervous system, such as Alzheimer's disease, senile dementia, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis and multiple sclerosis, psychiatric diseases, such as schizophrenia and anxiety, depression, pain and drug dependency.
摘要翻译：本发明提供4- [1-芳基 - 咪唑-4-基乙炔基] -2-烷基 - 吡啶和1-杂芳基 - 咪唑-4-基乙炔基] -2-烷基 - 吡啶衍生物及其药学上可接受的盐，用于治疗或预防由代谢型谷氨酸受体5完全或部分介导的病症。这些疾病包括，例如，神经系统的急性，创伤性和慢性退行性过程，例如阿尔茨海默病，老年性痴呆，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化和多发性硬化，精神疾病如精神分裂症和焦虑症，抑郁症，疼痛和药物依赖性。

69. 发明申请

US20060229323A1 (3,4-Dihydro-quinazolin-2-yl)-indan-1-yl-amines 失效
标题翻译：（3,4-二氢 - 喹唑啉-2-基） - 茚满-1-基 - 胺
公开(公告)号：US20060229323A1
公开(公告)日：2006-10-12
申请号：US11399790
申请日：2006-04-05
申请人： Alexander Alanine , Luca Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
发明人： Alexander Alanine , Luca Gobbi , Sabine Kolczewski , Thomas Luebbers , Jens-Uwe Peters , Lucinda Steward
IPC分类号： A61K31/517 , C07D239/84
CPC分类号： C07D409/04 , C07D239/84 , C07D413/04
摘要： The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I for 5-HT5A receptor related diseases, such as anxiety, depression, sleep disorders and schizophrenia.
摘要翻译：本发明涉及下式的化合物，其中R 1，R 2，和n如本文所定义，并且其药学上可接受的酸加成盐。式I化合物对5-HT 5A 5A受体具有良好的活性。因此，本发明提供式I化合物在5-HT 5A受体相关疾病如焦虑，抑郁，睡眠障碍和精神分裂症中的用途。

70. 发明申请

US20060199960A1 Pyridine-2-carboxyamide derivatives 有权
标题翻译：吡啶-2-甲酰胺衍生物
公开(公告)号：US20060199960A1
公开(公告)日：2006-09-07
申请号：US11360085
申请日：2006-02-23
申请人： Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
发明人： Georg Jaeschke , Sabine Kolczewski , Richard Porter , Eric Vieira
IPC分类号： C07D417/02 , C07D403/02 , C07D409/02 , C07D401/02
CPC分类号： C07D213/81 , A61K9/2018 , A61K9/4858 , C07D401/12 , C07D409/12 , C07D417/12
摘要： The invention relates to compounds of formula I: wherein R1 to R3 are as defined in the specification, to processes for their preparation, to pharmaceutical compositions containing them, and to methods for treating CNS disorders.
摘要翻译：本发明涉及式I化合物：其中R 1至R 3如本说明书中所定义，其制备方法，含有它们的药物组合物和治疗CNS疾病的方法。

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