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公开(公告)号:US20110306618A1
公开(公告)日:2011-12-15
申请号:US13202779
申请日:2010-02-19
IPC分类号: A61K31/496 , A61P29/00 , A61K31/506 , C12N9/99 , C07D401/14
CPC分类号: C07D471/04
摘要: Compounds of formula (I) modulate JNK wherein X1 and X2 are each simultaneously N or CH; X3 is CH—R2 Or N—SO2R, where R is lower alkyl; R1 is aryl or heteroaryl, substituted with 0-3 lower alkyl radicals; R2 is (II), where R3 is H, lower acyl, or an amino acid, or a pharmaceutically acceptable salt thereof.
摘要翻译: 式(I)化合物调节JNK,其中X1和X2各自同时为N或CH; X3是CH-R2或N-SO2R,其中R是低级烷基; R1是被0-3个低级烷基取代的芳基或杂芳基; R2是(II),其中R3是H,低级酰基或氨基酸,或其药学上可接受的盐。
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公开(公告)号:US07678815B2
公开(公告)日:2010-03-16
申请号:US11328879
申请日:2006-01-10
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: A61K31/445 , A61K31/454 , 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R1至R4如说明书中所定义。
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公开(公告)号:US07332510B2
公开(公告)日:2008-02-19
申请号:US10858969
申请日:2004-06-02
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 , C07D401/06
CPC分类号: C07D401/06 , C07D401/14
摘要: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinbelow. 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: 本发明涉及式I的咪唑衍生物,其中R 1,R 2,R 3和R 4, 在下文中描述。 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: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:US07973165B2
公开(公告)日:2011-07-05
申请号:US11955421
申请日:2007-12-13
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: C07D401/06 , 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R1,R2,R3和R4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:US20090018171A1
公开(公告)日:2009-01-15
申请号:US12211849
申请日:2008-09-17
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 , C07D233/54 , A61K31/4164 , C07D401/02
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R1,R2,R3,R4,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。
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公开(公告)号:US07241760B2
公开(公告)日:2007-07-10
申请号:US10866255
申请日:2004-06-12
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: A61K31/5377 , A61K31/50 , C07D401/04 , C07D403/04 , C07D413/04
CPC分类号: C07D233/64 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/14
摘要: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, interalia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits, 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, >。 这些化合物可用于治疗或预防mGluR5受体介导的疾病。 这些化合物在治疗或预防急性和/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以及慢性和急性疼痛中是有用的。
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公开(公告)号:US07091222B2
公开(公告)日:2006-08-15
申请号:US10874948
申请日:2004-06-23
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 , C07D401/06
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:US07034044B2
公开(公告)日:2006-04-25
申请号:US10672950
申请日:2003-09-26
申请人: Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
发明人: Alexander Alanine , Bernd Buettelmann , Marie-Paule Heitz Neidhart , Emmanuel Pinard , Rene Wyler
IPC分类号: A61K31/4436 , A61K31/4418 , C07D409/04 , C07D213/73 , C07D213/38
CPC分类号: C07D213/73 , C07D213/38 , C07D213/53 , C07D213/74 , C07D213/79 , C07D213/84 , C07D409/04
摘要: The present invention relates to compounds of formulae The compounds of the present invention are NMDA (N-methyl-D-aspartate)-receptor subtype blockers and are used in the treatment of diseases related to this receptor.
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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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