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公开(公告)号:US20070078155A1
公开(公告)日:2007-04-05
申请号:US11529992
申请日:2006-09-28
IPC分类号: C07D471/02 , A61K31/4745
CPC分类号: C07D471/04
摘要: The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.
摘要翻译: 本发明涉及式I的杂环衍生物,其中R 1,R 2和R 3是如说明书和权利要求中所定义的,其中 化合物是代谢型谷氨酸受体5拮抗剂。
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公开(公告)号:US20070105891A1
公开(公告)日:2007-05-10
申请号:US11590087
申请日:2006-10-31
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。
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公开(公告)号:US20060199828A1
公开(公告)日:2006-09-07
申请号:US11366007
申请日:2006-02-28
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: A61K31/506 , A61K31/4965 , A61K31/497 , C07D403/02 , C07D417/02 , C07D409/02
CPC分类号: C07D401/12 , C07D241/26 , C07D401/14 , C07D403/02 , C07D403/12 , C07D403/14 , C07D409/02 , C07D417/02 , C07D417/12 , C07D417/14
摘要: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
摘要翻译: 本发明涉及式(I)的新的吡嗪2-甲酰胺衍生物,其中R 1,R 2和R 3 3定义如上所定义 在规范中。 这些化合物可用于治疗CNS疾病。
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公开(公告)号:US20050054686A1
公开(公告)日:2005-03-10
申请号:US10926670
申请日:2004-08-26
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: C07D401/06 , C07D401/14 , A61K31/4439 , A61K31/4164 , A61K31/4178 , C07D43/02
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,包括对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。
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公开(公告)号:US20060030559A1
公开(公告)日:2006-02-09
申请号:US11141547
申请日:2005-05-31
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: A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4439 , C07D417/14 , C07D403/14 , C07D413/14
CPC分类号: C07D401/06 , C07D401/14
摘要: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
摘要翻译: 本发明涉及以下通式的二唑衍生物:其中A,E,R 1,R 2和R 3如申请中所定义 和含有它们的药物组合物。 本发明还涉及这种化合物用于治疗由代谢型谷氨酸受体(mGluR)介导的疾病的用途,例如焦虑,慢性和急性疼痛,防止肝损伤,尿失禁,肥胖,脆性-X和自闭症,阿尔茨海默病 疾病,癫痫,精神分裂症,局部缺血,亨廷顿舞蹈病,肌萎缩性侧索硬化(ALS),AID引起的痴呆和帕金森病。
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公开(公告)号:US20050009878A1
公开(公告)日:2005-01-13
申请号:US10874948
申请日:2004-06-23
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: A61K31/4178 , A61K31/4439 , A61P25/00 , A61P25/22 , C07D401/06 , C07
CPC分类号: C07D401/06 , A61K31/4178 , A61K31/4439
摘要: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are as defined hereinabove. This invention also relates to the compound's pharmaceutically acceptable salt and processes for the preparation thereof. These compounds can be used for the manufacture of pharmaceutical compositions for the treatment and 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's disease, cognitive disorders and memory deficit disorders, as well as chronic and acute pain.
摘要翻译: 本发明涉及以下通式的咪唑衍生物:其中R 1,R 2,R 3和R 4如上所定义。 本发明还涉及该化合物的药学上可接受的盐及其制备方法。 这些化合物可用于制备用于治疗和预防mGluR5受体介导的病症的药物组合物。 这些化合物尤其用于治疗或预防急性和/或慢性神经障碍如精神病,癫痫,精神分裂症,阿尔茨海默病,认知障碍和记忆缺陷障碍以及慢性和急性疼痛。
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公开(公告)号:US20060160857A1
公开(公告)日:2006-07-20
申请号:US11328879
申请日:2006-01-10
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: A61K31/445 , A61K31/454 , A61K31/426 , A61K31/427 , C07D417/02
CPC分类号: C07D277/42 , C07D417/12 , C07D417/14
摘要: The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
摘要翻译: 本发明涉及通式(I)的新型噻唑-4-甲酰胺衍生物及其制备方法,该化合物可用作代谢型谷氨酸受体拮抗剂:其中R 1至R' SUP> 4 SUP>如说明书中所定义。
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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 SUP>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。
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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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公开(公告)号:US20060160816A1
公开(公告)日:2006-07-20
申请号:US11374157
申请日:2006-03-14
申请人: David Adams , Jon Bentley , James Davidson , Matthew Dunction , Richard Porter
发明人: David Adams , Jon Bentley , James Davidson , Matthew Dunction , Richard Porter
IPC分类号: A61K31/498 , C07D487/04
CPC分类号: C07D487/04
摘要: Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.
摘要翻译: 式(I)的化合物及其药学上可接受的盐和加成化合物及其前药可用于治疗,特别是用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 糖尿病,睡眠呼吸暂停。
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