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1. 发明申请

WO2009053459A1 4-BENZ0YL-1-SUBSTITUTED-PIPERAZIN-2-0NE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的4-苄氧基-1-取代的哌嗪-2-酮衍生物
公开(公告)号：WO2009053459A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064429
申请日：2008-10-24
申请人： GLAXO GROUP LIMITED , CHAMBERS, Laura, Jane , COLLIS, Katharine, Laura , DEAN, David, Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
发明人： CHAMBERS, Laura, Jane , COLLIS, Katharine, Laura , DEAN, David, Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
IPC分类号： C07D241/08 , C07D401/06 , C07D401/10 , C07D403/10 , C07D407/06 , A61K31/496 , A61P29/00 , A61P19/02 , A61P25/28
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 C 1-6 alkyl, C 3-6 cycloalkyl, -CH 2 -R 6 , -CHMe-R 7 , -CMe 2 -R 7 , 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, C 1-6 alkyl, -CF 3 , C 1-4 alkoxy, C 1 fluoroalkoxy, cyano, NR 8 R 9 ; and pyridyl wherein the pyridyl is optionally substituted by one methyl; R 1 is chlorine, fluorine, -CF 3 , cyano or C 1-6 alkyl; R 2 , R 3 and R 5 independently are hydrogen, fluorine, chlorine, -CF 3 , cyano or C 1-6 alkyl, such that at least one of R 2 , R 3 and R 5 is other than hydrogen; R 4 is hydrogen. These compounds and salts are thought to be P2X7 receptor antagonists. The invention also provides the use of the compound or salt for the manufacture of a medicament 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个可以相同或不同的取代基取代，所述取代基可以选自卤素，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。本发明还提供了化合物或盐在制备用于治疗疼痛，炎症，类风湿性关节炎，骨关节炎或神经变性疾病的药物中的用途。

2. 发明申请

WO2010125102A1 5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
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：WO2010125102A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055715
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALTER, Daryl Simon
发明人： DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALTER, Daryl Simon
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00 , A61P29/00
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, C 1-4 alkyl, C 3-6 cycloalkyl, C 1-3 alkoxy, C 1-3 alkoxy C 1-4 alkyl, C 1-2 fluoroalkyl, halogen, NR 6 R 7 , optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 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 1-10 - 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。

3. 发明申请

WO2010125101A1 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
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：WO2010125101A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055714
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALL, Ian David , WALTER, Daryl Simon
发明人： DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , SIME, Mairi , STEADMAN, Jon Graham Anthony , THEWLIS, Rachel Elizabeth Anne , TRANI, Giancarlo , WALL, Ian David , WALTER, Daryl Simon
IPC分类号： C07D487/04 , A61P29/00 , A61K31/4985
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, C 1-4 alkyl, C 3-6 cycloalkyl, C 1-3 alkoxy, C 1-3 alkoxy C 1-4 alkyl, C 1-2 fluoroalkyl, halogen, NR 6 R 7 optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 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 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

WO2010125103A1 DIKETOPIPERAZINE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译： DIKETOPIPERAZINE衍生物作为P2X7调节剂
公开(公告)号：WO2010125103A1
公开(公告)日：2010-11-04
申请号：PCT/EP2010/055716
申请日：2010-04-28
申请人： GLAXO GROUP LIMITED , CHAMBERS, Laura Jane , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
发明人： CHAMBERS, Laura Jane , DEAN, David Kenneth , MUNOZ-MURIEDAS, Jorge , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
IPC分类号： C07D241/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D413/04 , A61K31/4965 , A61K31/497 , A61P25/28 , A61P25/08 , A61P29/00
CPC分类号： C07D241/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D405/04 , C07D413/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein: A represents an aryl, heteroaryl or heterocyclyl group; and any ring or ring system of said aryl or heteroaryl is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of halogen, C 1-6 alkyl, -CF 3 , - OCF 3 , cyano, C 1-6 alkoxy, -NR 10 R 11 , -X-aryl, -X-heteroaryl and -X-heterocyclyl; R 1 , R 2 , R 3 , R 4 and R 5 independently represent hydrogen, fluorine, chlorine, -CF 3 , cyano or C 1-6 alkyl, such that at least one of R 1 , R 2 , R 3 , R 4 and R 5 is other than hydrogen; R 6 , R 7 , R 8 , R 9 , R 10 and R 11 independently represent hydrogen or C 1-6 alkyl; X represents a linker selected from a bond, -(CH 2 ) n - and -O-(CH 2 ) n -; and n represents an integer from 1 to 3. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor ("P2X7 receptor antagonists").
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐：（I）其中：A表示芳基，杂芳基或杂环基; 并且所述芳基或杂芳基的任何环或环系统任选地被1至3个可以相同或不同的取代基取代，所述取代基可以选自卤素，C 1-6烷基，-CF 3，-OCF 3，氰基，C 1 -6-烷氧基，-NR10R11，-X-芳基，-X-杂芳基和-X-杂环基; R 1，R 2，R 3，R 4和R 5独立地表示氢，氟，氯，-CF 3，氰基或C 1-6烷基，使得R 1，R 2，R 3，R 4和R 5中的至少一个不是氢; R6，R7，R8，R9，R10和R11独立地表示氢或C1-6烷基; X表示选自键， - （CH 2）n - 和-O-（CH 2）n - 的连接体; 并且n表示1至3的整数。化合物或盐调节P2X7受体功能并且能够拮抗ATP在P2X7受体（“P2X7受体拮抗剂”）的作用。

5. 发明申请

WO2009077559A2 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：WO2009077559A2
公开(公告)日：2009-06-25
申请号：PCT/EP2008/067733
申请日：2008-12-17
申请人： GLAXO GROUP LIMITED , STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
发明人： STEADMAN, Jon Graham Anthony , WALTER, Daryl Simon
IPC分类号： A61K31/4015 , A61P25/00 , 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: R 1 represents C 1-4 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 3-6 cycloalkylmethyl-, phenyl-X- or heteroaryl, any of which may be optionally substituted; X represents -(CR 12 R 13 ) n -; n represents 0 to 2; and R 7 , R 8 , R 9 , R 10 and R 11 independently represent H, halogen, or cyano; or optionally substituted C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 3-6 cycloalkyl; such that at least two of R 7 , R 8 , R 9 , R 10 and R 11 represent a group other than H and at least one of R 7 and R 11 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，其中任何一个可以任选被取代; 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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