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公开(公告)号:US07189850B2
公开(公告)日:2007-03-13
申请号:US10967534
申请日:2004-10-18
IPC分类号: C07D471/10
CPC分类号: C07D471/10
摘要: The invention relates to compounds of the general formula wherein A-A is —CH2—CH2—, —CH2—CH2—CH2—, —CH2—O— or —O—CH2—; and X, R1, R2, R3, R4, R5, R6, n, and p are as defined herein, or a pharmaceutically acceptable salt thereof for the treatment of psychoses, pain, neurodegenerative dysfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译: 本发明涉及以下通式的化合物:其中AA是-CH 2 -CH 2 - , - CH 2 -CH 2 -CH 2 - , - CH 2 -O-O-或-O-CH 2 - ; - 和X,R 1,R 2,R 3,R 4,R 5, 本发明中,n和p如本文所定义,或其药学上可接受的盐用于治疗精神病,疼痛,记忆和学习中的神经变性功能障碍,精神分裂症,痴呆等疾病 哪些认知过程受损,如注意力缺陷障碍或阿尔茨海默病。
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公开(公告)号:US07176316B2
公开(公告)日:2007-02-13
申请号:US10778560
申请日:2004-02-13
IPC分类号: C07D211/56
CPC分类号: C07D413/12 , C07D211/58 , C07D401/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/14
摘要: The present invention relates to compounds of the general formula wherein X and Y are each independently selected from —CH2— or —O—, with the proviso that X and Y are not simultaneously —O—; A is —S(O)2— or —C(O)—; and R1, R2, R3, and R4 are as defined in the specification. The compounds are GlyT-1 inhibitors and are useful for the treatment of psychoses, pain, dysfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译: 本发明涉及通式的化合物,其中X和Y各自独立地选自-CH 2 - 或-O-,条件是X和Y不同时为-O-; A是-S(O)2 - 或-C(O) - ; R 1,R 2,R 3,R 4和R 4如说明书中所定义。 化合物是GlyT-1抑制剂,可用于治疗精神病,疼痛,记忆功能障碍,学习障碍,精神分裂症,痴呆等认知过程受损的其他疾病,如注意力缺陷障碍或阿尔茨海默病。
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公开(公告)号:US07173133B2
公开(公告)日:2007-02-06
申请号:US11028281
申请日:2005-01-03
IPC分类号: C07D471/10 , C07D405/14
CPC分类号: C07D471/10
摘要: The present invention relates to compounds of formula wherein A-B is —CH2—CH2—, —CH2—O— or —O—CH2—; X is hydrogen or hydroxy; R1 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, cyano, CF3, —OCF3, lower alkoxy, —SO2-lower alkyl and heteroaryl; R2 is aryl, optionally substituted by one or two substituents selected from the group consisting of halogen, lower alkyl, CF3, and lower alkoxy; R3 is hydrogen or lower alkyl; n is 0, 1 or 2; or a pharmaceutically active salt thereof. The compounds of the invention may be used in the treatment of neurological and neuropsychiatric disorders.
摘要翻译: 本发明涉及下式的化合物其中AB是-CH 2 -CH 2 - , - CH 2 -O - 或-O- CH 2 - ; X是氢或羟基; R 1是芳基,任选被一个或两个选自卤素,低级烷基,氰基,CF 3,-OCF 3, 低级烷氧基,-SO 2 - 低级烷基和杂芳基; R 2是任选被一个或两个选自卤素,低级烷基,CF 3 N 3和低级烷氧基的取代基取代的芳基; R 3是氢或低级烷基; n为0,1或2; 或其药物活性盐。 本发明的化合物可用于治疗神经和神经精神障碍。
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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:US20120232104A1
公开(公告)日:2012-09-13
申请号:US13477336
申请日:2012-05-22
申请人: Konrad Bleicher , Simona Maria Ceccarelli , Odile Chomienne , Patrizio Mattei , Tanja Schulz-Gasch , Christoph Martin Stahl
发明人: Konrad Bleicher , Simona Maria Ceccarelli , Odile Chomienne , Patrizio Mattei , Tanja Schulz-Gasch , Christoph Martin Stahl
IPC分类号: A61K31/196 , C07C311/29 , A61K31/24 , C07D413/04 , A61K31/422 , C07D409/04 , A61K31/506 , A61K31/4155 , C07D213/79 , C07D213/803 , A61K31/44 , C07C303/38 , C07C303/40 , C07D257/04 , A61K31/41 , C07D271/07 , A61K31/4245 , C07D291/04 , A61P3/10 , A61P3/08 , A61P3/04 , A61P9/12 , A61P3/00 , A61P3/06 , A61P1/16 , A61P9/10 , A61P9/04 , A61P13/12 , C07C311/21
CPC分类号: C07D413/04 , C07C311/21 , C07C311/29 , C07D257/04 , C07D271/07 , C07D291/04 , C07D409/04
摘要: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
摘要翻译: 本发明涉及式(I)的新型磺酰胺衍生物,其中R2,R3,R4,A,X,Y1,Y2,Y3,Y4和Z1如说明书和权利要求书中所定义,以及生理上可接受的盐 及其酯。 这些化合物抑制L-CPT1,可用作药物。
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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: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:US08481548B2
公开(公告)日:2013-07-09
申请号:US11930258
申请日:2007-10-31
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 , A61K31/497 , A61K31/506 , C07D401/14 , C07D403/14
CPC分类号: C07D401/06 , C07D401/14
摘要: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 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, cognititve 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:US07964620B2
公开(公告)日:2011-06-21
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 , A61K31/4164 , C07D401/06 , C07D233/64
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,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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