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1. 发明授权

US08501946B2 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine derivatives as P2X7 modulators 有权
标题翻译： 5,6,7,8-四氢[1,2,4]三唑并[4,3-a]吡嗪衍生物，为P2X7调节剂
公开(公告)号：US08501946B2
公开(公告)日：2013-08-06
申请号：US13266592
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 , Daryl Simon Walter
发明人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Daryl Simon Walter
IPC分类号： C07D495/00
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, 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，骨关节炎或神经变性疾病中的用途。

2. 发明申请

US20120157436A1 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 有权
标题翻译： 5,6,7,8-四氢[1,2,4]三唑[4,3-a]吡嗪衍生物作为P2X7调节剂
公开(公告)号：US20120157436A1
公开(公告)日：2012-06-21
申请号：US13266592
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 , Daryl Simon Walter
发明人： David Kenneth Dean , Jorge Munoz-Muriedas , Mairi Sime , Jon Graham Anthony Steadman , Rachel Elizabeth Anne Thewlis , Giancarlo Trani , Daryl Simon Walter
IPC分类号： A61K31/4985 , A61K31/506 , A61K31/5377 , A61P25/14 , A61P29/00 , A61P25/28 , A61P25/08 , A61P25/16 , C07D487/04 , A61K31/501
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, C1-2-fluoroalkyl, 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, 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，骨关节炎或神经变性疾病中的用途。

3. 发明授权

US08513248B2 5,6,7,8-tetrahydroimidazo[1,2-A]pyrazine derivatives as P2X7 modulators 有权
标题翻译： 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。

4. 发明申请

US20120172366A1 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 有权
标题翻译：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。

5. 发明申请

US20100311749A1 4-BENZOYL-1-SUBSTITUTED-PIPERAZIN-2-ONE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的4-苯甲酰基-1-取代的哌嗪-2-酮衍生物
公开(公告)号：US20100311749A1
公开(公告)日：2010-12-09
申请号：US12739462
申请日：2008-10-24
申请人： Laura Jane Chambers , Katharine Laura Collis , David Kenneth Dean , Jorge Munoz-Muriedas , Jon Graham Anthony Steadman , Daryl Simon Walter
发明人： Laura Jane Chambers , Katharine Laura Collis , David Kenneth Dean , Jorge Munoz-Muriedas , Jon Graham Anthony Steadman , Daryl Simon Walter
IPC分类号： A61K31/5377 , C07D241/08 , A61K31/495 , C07D413/10 , C07D401/06 , A61K31/496 , C07D405/06 , C07D403/10 , A61P29/00 , A61P25/28 , A61P19/02
CPC分类号： C07D241/08 , C07D401/06 , C07D401/10 , C07D403/10 , C07D407/06
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: A is C1-6alkyl, C3-6cycloalkyl, —CH2—R6, —CHMe-R7, —CMe2-R7, or optionally substituted aryl; wherein, when A is optionally substituted aryl, said aryl group is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C1-6alkyl, —CF3, C1-4alkoxy, C1fluoroalkoxy, cyano, NR8R9, and pyridyl wherein the pyridyl is optionally substituted by one methyl; R1 is chlorine, fluorine, —CF3, cyano or C1-6alkyl; R2, R3 and R5 independently are hydrogen, fluorine, chlorine, —CF3, cyano or C1-6alkyl, such that at least one of R2, R3 and R5 is other than hydrogen; R4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides for the treatment of pain, inflammation, rheumatoid arthritis, osteoarthritis, or a neurodegenerative disease.
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C 1-6烷基，C 3-6环烷基，-CH 2 -R 6，-CHMe-R 7，-CMe 2 -R 7或任选取代的芳基; 其中当A是任选取代的芳基时，所述芳基任选地被1至3个选自卤素，C 1-6烷基，-CF 3，C 1-4烷氧基，C 1-6烷氧基，氰基，NR8R9和吡啶基，其中吡啶基任选被一个甲基取代; R1是氯，氟，-CF3，氰基或C1-6烷基; R2，R3和R5独立地是氢，氟，氯，-CF3，氰基或C1-6烷基，使得R2，R3和R5中的至少一个不是氢; R4是氢。这些化合物和盐被认为是P2X7受体拮抗剂。本发明还提供治疗疼痛，炎症，类风湿性关节炎，骨关节炎或神经变性疾病。

6. 发明申请

US20100168171A1 Piperidinone Carboxamide Derivatives as P2X7 Modulators 审中-公开
标题翻译：哌啶酮甲酰胺衍生物作为P2X7调节剂
公开(公告)号：US20100168171A1
公开(公告)日：2010-07-01
申请号：US12593044
申请日：2008-03-20
申请人： Paul John Beswick , Robert James Gleave , Jon Graham Anthony Steadman , Daryl Simon Walter
发明人： Paul John Beswick , Robert James Gleave , Jon Graham Anthony Steadman , Daryl Simon Walter
IPC分类号： A61K31/45 , C07D211/78 , A61P29/00 , A61P25/28
CPC分类号： C07D211/78
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: The compounds or salts modulate P2X7 receptor function and are capable of interfering with the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease, in particular pain such as inflammatory pain, neuropathic pain or visceral pain.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：该化合物或盐调节P2X7受体功能并能够干扰ATP在P2X7受体上的作用。本发明还提供了这样的化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的病症中的用途，例如疼痛，炎症或神经变性疾病，特别是疼痛，例如炎性疼痛，神经性疼痛或内脏痛。

7. 发明申请

US20100292295A1 5-OXO-3-PYRROLIDINECARBOXAMIDE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的5-氧代-3-吡咯烷酮甲酰胺衍生物
公开(公告)号：US20100292295A1
公开(公告)日：2010-11-18
申请号：US12808017
申请日：2008-12-17
申请人： Jon Graham Anthony Steadman , Daryl Simon Walter
发明人： Jon Graham Anthony Steadman , Daryl Simon Walter
IPC分类号： A61K31/4015 , C07D207/277 , A61P19/02 , A61P25/28 , A61P25/16 , A61P29/00
CPC分类号： A61K31/4015
摘要： The present invention provides a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: wherein R1 represents C1-4 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C3-6 cycloalkylmethyl-, phenyl-X— or heteroaryl, any of which may be optionally substituted; X represents —(CR12R13)n—; n represents 0 to 2; and R7, R8, R9, R10 and R11 independently represent H, halogen, or cyano; or optionally substituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkyl; such that at least two of R7, R8, R9, R10 and R11 represent a group other than H and at least one of R7 and R11 represents a group other than H; and wherein the compound is other than N-[(2,4-dichlorophenyl)methyl]5-oxo-1-(phenylmethyl)-3-pyrrolidinecarboxamide. The compounds and salts are thought to modulate P2X7 receptor function and be capable of antagonizing the effects of ATP at the P2X7 receptor.
摘要翻译：本发明提供式（IA）化合物或其药学上可接受的盐：其中R 1表示C 1-4烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基，C 3-6环烷基甲基 - ，苯基-X - 或杂芳基，其中任何一个可以是任选取代的; X表示 - （CR12R13）n-; n表示0〜2; 且R 7，R 8，R 9，R 10和R 11独立地表示H，卤素或氰基; 或任选取代的C 1-6烷基，C 2-6烯基，C 2-6炔基或C 3-6环烷基; 使得R 7，R 8，R 9，R 10和R 11中的至少两个表示除H以外的基团，并且R 7和R 11中的至少一个表示除H以外的基团; 并且其中所述化合物不是N - [（2,4-二氯苯基）甲基] -5-氧代-1-（苯基甲基）-3-吡咯烷甲酰胺。化合物和盐被认为调节P2X7受体功能，并能够拮抗ATP在P2X7受体上的作用。

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