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1. 发明申请

US20130267499A1 NOVEL TETRAHYDROPYRAZOLO [3,4-b] AZEPINE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权
标题翻译：新型四氢呋喃并[3,4-b]亚胺衍生物及其作为代谢型谷氨酸受体的独立调节剂
公开(公告)号：US20130267499A1
公开(公告)日：2013-10-10
申请号：US13809581
申请日：2011-07-11
申请人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
发明人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
IPC分类号： C07D513/12 , A61K45/06 , A61K31/55
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K2300/00
摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
摘要翻译：本发明涉及新的式（I）化合物，其中M，A和Y如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

2. 发明授权

US09765091B2 Tetrahydropyrazolo [3,4-b] azepine derivatives and their use as allosteric modulators of metabotropic glutamate receptors 有权
公开(公告)号：US09765091B2
公开(公告)日：2017-09-19
申请号：US13809581
申请日：2011-07-11
申请人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
发明人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
IPC分类号： C07D513/12 , A61K31/4162 , A61K31/429 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K31/433 , A61K31/4439 , A61K31/506 , A61B5/00 , A61K9/00 , A61K9/06 , A61K9/10 , A61K9/20 , A23L5/00
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K2300/00
摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

3. 发明申请

US20130252944A1 NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新型掺杂的吡唑衍生物及其作为代谢谷氨酸受体的独立调节剂
公开(公告)号：US20130252944A1
公开(公告)日：2013-09-26
申请号：US13809583
申请日：2011-07-11
申请人： Christelle Bolea , Sylvain Celanire , Lam Tang , Philip Jones , Nigel J. Liverton , Richard Soll , Jingchao Dong , Zhiyu Lei , Fuqing Liu , Yanling Kong , Yi Ju , Haoyong Zhang , Jieping Wei , Qiaoxin Wei , Minxiang Zhang , Yunfu Luo
发明人： Christelle Bolea , Sylvain Celanire , Lam Tang , Philip Jones , Nigel J. Liverton , Richard Soll , Jingchao Dong , Zhiyu Lei , Fuqing Liu , Yanling Kong , Yi Ju , Haoyong Zhang , Jieping Wei , Qiaoxin Wei , Minxiang Zhang , Yunfu Luo
IPC分类号： C07D513/04 , A61K31/433 , A61K31/4439 , A61K31/506 , C07D513/14 , A61K45/06
CPC分类号： C07D513/12 , A23L27/2056 , A23L33/10 , A23V2002/00 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K2300/00 , A23V2200/16 , A23V2200/322 , A23V2200/328
摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
摘要翻译：本发明涉及新的式（I）化合物，其中M，A和Y如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

4. 发明申请

US20130210807A1 Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors. 审中-公开
标题翻译：三环化合物作为代谢型谷氨酸受体的变构调节剂。
公开(公告)号：US20130210807A1
公开(公告)日：2013-08-15
申请号：US13809579
申请日：2011-07-09
申请人： Nigel J Liverton , Christelle Boléa , Sylvain Celanire , Yunfu Luo
发明人： Nigel J Liverton , Christelle Boléa , Sylvain Celanire , Yunfu Luo
IPC分类号： C07D513/04 , A61K45/06 , A61K31/55 , A61K31/433 , C07D513/14 , A61K31/506
CPC分类号： C07D513/04 , A61K31/433 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/14
摘要： The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3′ are —H or methyl, or R3 and R3 taken together form a double bond, or R3′ is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.
摘要翻译：本发明描述并要求结构式I，结构式II或结构式III的化合物：其中R1，R2，R3和R3'是-H或甲基，或R3和R3一起形成双键，或R3 '是-H并且R 2和R 3一起形成螺环丙基取代基，R 4是-H或-F，且R 5是-H，甲基，-C 1或-Br，其中R 1是-H，乙基，异丙基 - ，环丙基 - ，甲基或甲氧基 - ，R 4为-H或-F，“Y”为：（a）-CH 2 - ; （b）-CR6H-0-CR7R8-，其中R6，R7和R8独立地是-H或甲基; （c）-CR 6 H-N（R 9）-CR 7 R 8 - ，其中R 6，R 7和R 8独立地为-H或甲基; （d）-CH 2 -C（R 9）（R 10）-C（R 7）（R 8） - ，其中R 7，R 8，R 9和R 10独立地为-H或 - 甲基，或者R 7和R 8均为-F，R 9和 R 10独立地是-H或 - 甲基，或者R 9和R 10都是-F，或者R 9和R 10一起是（0 =），它们与它们所连接的碳一起形成羰基。

5. 发明申请

US20130210809A1 NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：新型2-氨基-4-吡唑并噻唑衍生物及其作为代谢谷氨酸受体的独立调节剂
公开(公告)号：US20130210809A1
公开(公告)日：2013-08-15
申请号：US13808899
申请日：2011-07-12
申请人： Christelle Boléa , Sylvain Celanire , Cédric Boudou , Lam Tang , Jean-Philippe Rocher , Nigel John Liverton
发明人： Christelle Boléa , Sylvain Celanire , Cédric Boudou , Lam Tang , Jean-Philippe Rocher , Nigel John Liverton
IPC分类号： C07D417/14 , A61K45/06 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/4439 , A61K31/433 , C07D487/04 , A61K31/541
CPC分类号： C07D417/14 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D487/04
摘要： The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
摘要翻译：本发明涉及式（1）的新化合物，其中M，A和B如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它病症。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

6. 发明申请

US20090023708A1 Compounds Comprising a Lactam or a Lactam Derivative Moiety, Processes for Making Them, and Their Uses 失效
标题翻译：包含内酰胺或内酰胺衍生物的化合物，其制备方法及其用途
公开(公告)号：US20090023708A1
公开(公告)日：2009-01-22
申请号：US12091380
申请日：2006-10-25
申请人： Sylvain Celanire , Luc Quere , Frederic Denonne , Laurent Provins
发明人： Sylvain Celanire , Luc Quere , Frederic Denonne , Laurent Provins
IPC分类号： A61K31/55 , C07D401/14 , A61K31/454 , C07D403/14 , A61K31/421 , C07D263/20 , A61K31/496 , A61K31/4025 , C07D403/12
CPC分类号： C07D207/26 , C07D205/08 , C07D207/09 , C07D207/24 , C07D207/277 , C07D209/54 , C07D211/76 , C07D223/10 , C07D263/22 , C07D295/088 , C07D487/10
摘要： The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
摘要翻译：本发明涉及包含内酰胺或内酰胺衍生物部分的式（I）化合物，其制备方法，包含所述化合物的药物组合物及其作为药物的用途。

7. 发明申请

US20080275046A1 Compounds Comprising an Oxazole or Thiazole Moiety, Processes for Making Them, and Their Uses 失效
标题翻译：包含恶唑或噻唑的化合物，其制备方法及其用途
公开(公告)号：US20080275046A1
公开(公告)日：2008-11-06
申请号：US11910191
申请日：2006-03-28
申请人： Sylvain Celanire , Frederic Denonne
发明人： Sylvain Celanire , Frederic Denonne
IPC分类号： A61K31/4545 , C07D401/14 , A61P25/28 , C07D413/14 , A61P25/18 , A61P29/00 , A61P3/04 , A61P9/00 , A61P25/16 , A61P25/22 , A61K31/5377 , A61P25/24 , A61K31/454
CPC分类号： C07D263/14 , C07D207/06 , C07D211/14 , C07D263/16 , C07D263/32 , C07D263/36 , C07D263/52 , C07D277/10 , C07D277/24 , C07D277/28 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to compounds comprising an oxazole or thiazole moiety of formula (I), processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as H3-receptor ligands, Formula (I), wherein, A1 is CH, C(alkyl), C-halogen or N; R1 is hydrogen, halogen, C1-6 alkyl or alkoxy; R2 is, Formula (II′), A3 is O or S; R3 is hydrogen, halogen, C1-6 alkyl or alkoxy; R4 is hydrogen, halogen, C1-6 alkyl, alkoxy or —O-L; R5 is hydrogen or —O-L, wherein L is an aminoalkyl group and at least one of R4 and R5 should be —O-L.
摘要翻译：本发明涉及包含式（I）的恶唑或噻唑部分的化合物，其制备方法，包含所述化合物的药物组合物及其作为H 3 - 受体配体的用途，式（I），其中，A 1是CH，C（烷基），C-卤素或N; R 1是氢，卤素，C 1-6烷基或烷氧基; R 2是式（II'），A 3是O或S; R 3是氢，卤素，C 1-6烷基或烷氧基; R 4是氢，卤素，C 1-6烷基，烷氧基或-O-L; R 5是氢或-O-L，其中L是氨基烷基，R 4和R 5中的至少一个应为-O-L。

8. 发明授权

US08524718B2 Heteroaromatic derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors 失效
标题翻译：杂芳族衍生物及其作为代谢型谷氨酸受体的正变构调节剂的用途
公开(公告)号：US08524718B2
公开(公告)日：2013-09-03
申请号：US13605893
申请日：2012-09-06
申请人： Christelle Boléa , Sylvain Celanire
发明人： Christelle Boléa , Sylvain Celanire
IPC分类号： A61K31/427 , A61K31/4155 , C07D277/20 , C07D231/10 , C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
摘要翻译：本发明涉及新的式（I）化合物，其中X1，X2，X3，X4，Y1，Y2，Y3，Y4，M1，M2，M3，Am和Bn如式（I）所定义。本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

9. 发明申请

US20120329811A1 Heteroaromatic Derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors 失效
标题翻译：杂芳族衍生物及其作为代谢型谷氨酸受体的正变构调节剂的用途
公开(公告)号：US20120329811A1
公开(公告)日：2012-12-27
申请号：US13605893
申请日：2012-09-06
申请人： Christelle Boléa , Sylvain Celanire
发明人： Christelle Boléa , Sylvain Celanire
IPC分类号： C07D417/04 , C07D417/14 , A61P25/00 , A61K31/427 , A61K31/4545 , A61K31/497 , A61K31/433 , A61K31/4439
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
摘要翻译：本发明涉及新的式（I）化合物，其中X1，X2，X3，X4，Y1，Y2，Y3，Y4，M1，M2，M3，Am和Bn如式（I）所定义。本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（mGluR4），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

10. 发明申请

US20110098300A1 Compounds Comprising A Cyclobutoxy Group 审中-公开
标题翻译：包含环丁氧基的化合物
公开(公告)号：US20110098300A1
公开(公告)日：2011-04-28
申请号：US12995084
申请日：2009-06-02
申请人： Sylvain Celanire , Laurent Provins , Frederic Denonne , Anne Valade
发明人： Sylvain Celanire , Laurent Provins , Frederic Denonne , Anne Valade
IPC分类号： A61K31/5377 , C07D211/60 , C07D413/12 , A61K31/4453 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D295/192 , C07D211/38 , C07D211/46 , C07D213/75 , C07D279/12 , C07D295/096
摘要： The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals, useful for the treatment and prevention of diseases or pathological conditions of the central nervous system including mild-cognitive impairments, Alzheimer's disease, learning and; memory disorders, cognitive disorders, attention deficit disorder, attention-deficit hyperactivity disorder, Parkinson's disease, schizophrenia, dementia, depression, epilepsy, seizures, convulsions, sleep/wake and arousal/vigilance disorders such as hypersomnia and narcolepsy, pain and/or obesity.
摘要翻译：本发明涉及包含环丁氧基的式（I）化合物，其制备方法，包含所述化合物的药物组合物及其作为药物的用途，可用于治疗和预防中枢神经系统疾病或病理状况，包括温和 - 认知障碍，阿尔茨海默病，学习和; 记忆障碍，认知障碍，注意力缺陷障碍，注意力缺陷多动障碍，帕金森病，精神分裂症，痴呆，抑郁症，癫痫，癫痫发作，抽搐，睡眠/唤醒和觉醒/警惕性障碍，如睡眠过多和发作性睡病，疼痛和/或肥胖。

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