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![5,6,7,8-tetrahydroimidazo[1,2-A]pyrazine derivatives as P2X7 modulators](/abs-image/US/2013/08/20/US08513248B2/abs.jpg.150x150.jpg)
1.发明授权5,6,7,8-tetrahydroimidazo[1,2-A]pyrazine derivatives as P2X7 modulators 有权5,6,7,8-四氢咪唑并[1,2-A]吡嗪衍生物作为P2X7调节剂公开(公告)号：US08513248B2
公开(公告)日：2013-08-20
申请号：US13266557
申请日：2010-04-28
申请人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Ian David Wall , Daryl Simon Walter
发明人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Ian David Wall , Daryl Simon Walter
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐：其中A为氢，C 1-4烷基，C 3-6环烷基，C 1-3烷氧基，C 1-3烷氧基C 1-4烷基，C 1-2 - 氟烷基，卤素，NR 6 R 7， 任选取代的杂芳基（Het）或任选取代的苯基，并且R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。 认为化合物或盐可以调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。 本发明还提供了化合物或盐在治疗或预防例如炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎或骨关节炎或神经变性疾病中的用途。
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公开(公告)号：US08222245B2
公开(公告)日：2012-07-17
申请号：US12747205
申请日：2008-12-19
申请人： Emmanuel Hubert Demont , Jag Paul Heer , John Skidmore , Ian David Wall , Jason Witherington , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson
发明人： Emmanuel Hubert Demont , Jag Paul Heer , John Skidmore , Ian David Wall , Jason Witherington , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson
IPC分类号： A61P17/00 , A61P37/00 , A61K31/55 , C07D223/16 , C07D267/14 , C07D271/06 , C07D413/04 , C07D413/14
CPC分类号： C07D223/16 , C07D267/14 , C07D271/06 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
摘要翻译： 本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。
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3.发明申请2-(Phenylamino)-Pyrimidin-5-Amides As Cannabinoid 2 Receptors Modulators for the Treatment of Immune or Inflammatory Disorders 审中-公开2-（苯基氨基） - 嘧啶-5-酰胺作为大麻素2受体调节剂治疗免疫或炎性疾病公开(公告)号：US20090264452A1
公开(公告)日：2009-10-22
申请号：US10597476
申请日：2005-02-01
申请人： Andrew John Eatherton , Gerard Martin Paul Giblin , William Leonard Mitchell , Alan Naylor , Derek Anthony Rawlings , Ian David Wall
发明人： Andrew John Eatherton , Gerard Martin Paul Giblin , William Leonard Mitchell , Alan Naylor , Derek Anthony Rawlings , Ian David Wall
IPC分类号： A61K31/505 , C07D239/42 , C07D405/12 , A61K31/506 , A61P29/00 , A61P37/00 , A61P19/00
CPC分类号： C07D239/42 , C07D405/12
摘要： The present invention relates to novel pyrimidine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
摘要翻译： 本发明涉及新颖的嘧啶衍生物，例如式（I）的化合物：以及这些化合物或其药物组合物在治疗由大麻素2受体的活性介导的疾病，特别是疼痛中的应用。
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4.发明申请1, 2, 4 -OXADIAZOLE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASES 审中-公开1，2，4 - 用于治疗自身免疫性疾病的奥多唑类化合物公开(公告)号：US20100273770A1
公开(公告)日：2010-10-28
申请号：US12747198
申请日：2008-12-19
申请人： Jag Paul Heer , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson , John Skidmore , Ian David Wall
发明人： Jag Paul Heer , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson , John Skidmore , Ian David Wall
IPC分类号： A61K31/55 , C07D413/10 , C07D413/14 , A61K31/553
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
摘要翻译： 本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。
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公开(公告)号：US20100174065A1
公开(公告)日：2010-07-08
申请号：US12360886
申请日：2009-01-28
申请人： Jag Paul HEER , Thomas Daniel HEIGHTMAN , David Nigel HURST , Christopher Norbert JOHNSON , John SKIDMORE , Ian David WALL
发明人： Jag Paul HEER , Thomas Daniel HEIGHTMAN , David Nigel HURST , Christopher Norbert JOHNSON , John SKIDMORE , Ian David WALL
IPC分类号： C07D413/10
CPC分类号： C07D223/16 , C07D267/14 , C07D271/06 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
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公开(公告)号：US20080280952A1
公开(公告)日：2008-11-13
申请号：US10597474
申请日：2005-02-01
IPC分类号： C07D405/12 , C07D211/72 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P37/00 , A61P29/00 , A61P19/02 , A61P19/00
CPC分类号： C07D213/82 , C07D405/12 , C07D409/12
摘要： The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.
摘要翻译： 本发明涉及新的吡啶衍生物，例如式（I）的化合物：以及这些化合物或其药物组合物在治疗由大麻素2受体的活性介导的疾病，特别是疼痛中的用途。
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![5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS](/abs-image/US/2012/07/05/US20120172366A1/abs.jpg.150x150.jpg)
7.发明申请5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 有权作为P2X7调节剂的5,6,7,8-四氢吡啶并[1,2-A]吡嗪衍生物公开(公告)号：US20120172366A1
公开(公告)日：2012-07-05
申请号：US13266557
申请日：2010-04-28
申请人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Ian David Wall , Daryl Simon Walter
发明人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Ian David Wall , Daryl Simon Walter
IPC分类号： A61K31/4985 , A61P29/00 , A61P25/16 , A61P25/08 , A61P25/14 , C07D487/04 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl, or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description.The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis or osteoarthritis or neurodegenerative disorders.
摘要翻译： 本发明提供式（I）化合物或其药学上可接受的盐：其中A为氢，C 1-4烷基，C 3-6环烷基，C 1-3烷氧基，C 1-3烷氧基C 1-4烷基，C 1-2 - 氟烷基，卤素，NR 6 R 7， 任选取代的杂芳基或任选取代的苯基，并且R 1，R 2，R 3，R 4，R 5，R 6和R 7如说明书中所定义。 认为化合物或盐可以调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。 本发明还提供了化合物或盐在治疗或预防例如炎性疼痛，神经性疼痛，内脏痛，类风湿性关节炎或骨关节炎或神经变性疾病中的用途。
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公开(公告)号：US20100273771A1
公开(公告)日：2010-10-28
申请号：US12747205
申请日：2008-12-19
申请人： Emmanuel Hubert Demont , Jag Paul Heer , John Skidmore , Ian David Wall , Jason Witherington , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson
发明人： Emmanuel Hubert Demont , Jag Paul Heer , John Skidmore , Ian David Wall , Jason Witherington , Thomas Daniel Heightman , David Nigel Hurst , Christopher Norbert Johnson
IPC分类号： A61K31/553 , C07D413/10 , A61K31/55 , A61P37/00
CPC分类号： C07D223/16 , C07D267/14 , C07D271/06 , C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
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