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公开(公告)号:US07951824B2
公开(公告)日:2011-05-31
申请号:US11699786
申请日:2007-01-30
申请人: Georg Jaeschke , Will Spooren , Eric Vieira
发明人: Georg Jaeschke , Will Spooren , Eric Vieira
IPC分类号: C07D401/12 , C07D213/81 , A61K31/443
CPC分类号: C07D417/12 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D417/14
摘要: The present invention relates to novel pyridine-2-carboxyamide derivatives of formula (I) useful as metabotropic glutamate receptor antagonists: wherein Y, Z, R1, R2 and R3 are as defined in the specification herein.
摘要翻译: 本发明涉及用作代谢型谷氨酸受体拮抗剂的式(I)的新型吡啶-2-甲酰胺衍生物:其中Y,Z,R 1,R 2和R 3如本说明书中所定义。
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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。
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公开(公告)号:US20080269256A1
公开(公告)日:2008-10-30
申请号:US12165758
申请日:2008-07-01
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。
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公开(公告)号:US07414060B2
公开(公告)日:2008-08-19
申请号:US11360085
申请日:2006-02-23
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。
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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: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: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。
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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:US20050143375A1
公开(公告)日:2005-06-30
申请号:US11020451
申请日:2004-12-22
申请人: Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Philip Porter , Eric Vieira , Anthony Ford , Yu Zhong
发明人: Bernd Buettelmann , Simona Ceccarelli , Georg Jaeschke , Sabine Kolczewski , Richard Philip Porter , Eric Vieira , Anthony Ford , Yu Zhong
IPC分类号: C07D401/06 , C07D401/14 , A61K31/541 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377
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 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 of genitourinary diseases.
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, 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泌尿生殖系疾病。
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公开(公告)号:US5393875A
公开(公告)日:1995-02-28
申请号:US100959
申请日:1993-08-03
申请人: Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
发明人: Quirico Branca , Marie-Paule Heitz , Werner Neidhart , Heinz Stadler , Eric Vieira , Wolfgang Wostl
IPC分类号: A61K31/16 , A61K31/165 , A61K31/215 , A61K31/22 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/535 , A61P9/00 , A61P9/04 , A61P9/12 , C07C317/44 , C07C317/50 , C07C323/51 , C07D207/08 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D233/64 , C07D277/20 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00 , C07H15/12 , C07D295/12 , A61K37/00
CPC分类号: C07D207/08 , C07C317/44 , C07C317/50 , C07D207/12 , C07D211/22 , C07D213/40 , C07D213/53 , C07D213/56 , C07D231/12 , C07D233/56 , C07D233/64 , C07D249/08 , C07D277/30 , C07D295/088 , C07D295/185 , C07D295/205 , C07D307/54 , C07D317/24 , C07D333/24 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要: The compounds of the formula ##STR1## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the significance given in claim 1,in the form of optically pure diastereomers, mixtures of diastereomers, diastereomeric racemates or mixtures of diastereomeric racemates as well as pharmaceutically usable salts thereof inhibit the activity of the natural enzyme renin and can accordingly be used in the form of pharamaceutical preparations in the control or prevention of high blood pressure and cardiac insufficiency. They can be manufactured according to various methods which are known per se.
摘要翻译: 其中A,R 1,R 2,R 3,R 4和R 5具有权利要求1中给出的含义的化合物,其为光学纯非对映异构体,非对映异构体的混合物,非对映体外消旋物或非对映异构体外消旋物的混合物 作为其药学上可用的盐抑制天然酶肾素的活性,因此可以以药物制剂的形式用于控制或预防高血压和心脏功能不全。 它们可以根据本身已知的各种方法制造。
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