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21. 发明申请

WO2008003697A1 SUBSTITUTED N-PHENYLMETHYL -5-OXO-PROLINE-2-AMIDES AS P2X7-RECEPTOR ANTAGONISTS AND THEIR METHODS OF USE 审中-公开
标题翻译：作为P2X7受体拮抗剂的取代的N-苯基甲基-5-氧代-2-丙氨酰胺及其使用方法
公开(公告)号：WO2008003697A1
公开(公告)日：2008-01-10
申请号：PCT/EP2007/056675
申请日：2007-07-03
申请人： GLAXO GROUP LIMITED , CHAMBERS, Laura, J , GLEAVE, Robert , SENGER, Stefan , WALTER, Daryl, Simon
发明人： CHAMBERS, Laura, J , GLEAVE, Robert , SENGER, Stefan , WALTER, Daryl, Simon
IPC分类号： C07D207/28 , C07D401/06 , A61K31/4015 , A61K31/402 , A61P25/28 , A61P29/00
CPC分类号： C07D401/06 , C07D207/277
摘要： The present invention relates to novel oxo-prolinamide derivatives of formula (I) which modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要翻译：本发明涉及调节P2X7受体功能并能够拮抗ATP在P2X7受体上的作用的式（I）的新型氧代 - 脯氨酰胺衍生物，以及这些化合物或其药物组合物在治疗由 P2X7受体，例如疼痛，炎症和神经变性。

22. 发明申请

WO2007141269A1 NOVEL RECEPTOR ANTAGONISTS AND THEIR METHODS OF USE 审中-公开
标题翻译：新型受体拮抗剂及其使用方法
公开(公告)号：WO2007141269A1
公开(公告)日：2007-12-13
申请号：PCT/EP2007/055521
申请日：2007-06-05
申请人： GLAXO GROUP LIMITED , BESWICK, Paul, John , WALTER, Daryl, Simon
发明人： BESWICK, Paul, John , WALTER, Daryl, Simon
IPC分类号： C07D261/08 , A61K31/42
CPC分类号： C07D261/08
摘要： The present invention relates to novel isoxazole derivatives of formula (I) which bind to the P2X7 receptor and are capable of interfering with the effects of ATP at the P2X7 receptor: and the use of such compounds or pharmaceutical compositions thereof in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation and neurodegeneration.
摘要翻译：本发明涉及结合P2X7受体并且能够干扰ATP在P2X7受体上的作用的式（I）的异恶唑衍生物，以及这些化合物或其药物组合物在治疗疾病介导中的用途通过P2X7受体，例如疼痛，炎症和神经变性。

23. 发明申请

WO2006103088A1 NOVEL HYDROXYETHYLAMINE AND KETONE COMPOUNDS HAVING ASP2 INHIBITORY ACTIVITY 审中-公开
标题翻译：具有ASP2抑制活性的新型羟甲基胺和酮酮化合物
公开(公告)号：WO2006103088A1
公开(公告)日：2006-10-05
申请号：PCT/EP2006/002953
申请日：2006-03-29
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： C07D515/06 , A61K31/554 , A61P25/28
CPC分类号： C07D515/06
摘要： The present invention relates to novel hydroxyethylamine and ketone compounds having Asp2 (β-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及具有Asp2（ß-分泌酶，BACE1或Memapsin-2）抑制活性的新型羟乙基胺和酮化合物，其制备方法，含有它们的组合物及其在治疗以β淀粉样蛋白升高为特征的疾病中的用途水平或β-淀粉样蛋白沉积物，特别是阿尔茨海默病。

24. 发明申请

WO2006040151A1 SUBSITUTED HYDROXYETHYLAMINE COMPOUNDS FOR TRATING ALZHEIMER’S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的羟基乙酰胺化合物
公开(公告)号：WO2006040151A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011004
申请日：2005-10-11
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： C07D513/06 , A61K31/554 , A61P25/28
CPC分类号： C07D513/06
摘要： The present invention relates to novel hydroxyethylamine compounds of formula (1) wherein, inter alia, A-B represents -NR 5 -SO 2 -;-W-represents -(CH 2 ) 3 - or -C(H)=C(H)-CH 2 -; X-Y-Z represents -C=CR 8 -NR 9 -, having Asp2 (β-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及式（1）的新的羟乙胺化合物，其中尤其A-B代表-NR

25. 发明申请

WO2006040148A1 TRICYCLIC INDOLE DERIVATIVES FOR USE IN THE TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的三氯吲哚类衍生物
公开(公告)号：WO2006040148A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/011001
申请日：2005-10-11
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： A61K31/554 , A61P25/28 , C07D513/06
CPC分类号： C07D513/06
摘要： The present invention relates to novel ketone compounds of formula (I) having Asp2 (β-secretase, BACE1 or Memapsin-2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及具有Asp2（ß-分泌酶，BACE1或Memapsin-2）抑制活性的式（I）的新型酮化合物，其制备方法，含有它们的组合物及其用于治疗特征在于升高的疾病 β-淀粉样蛋白水平或β-淀粉样蛋白沉积物，特别是阿尔茨海默病。

26. 发明申请

WO2005113525A1 N, N’-SUBSTITUTED-1,3-DIAMINO-2-OXOPROPANE DERIVATIVES, THEIR PHARMACEUTICAL COMPOSITIONS AND USE 审中-公开
标题翻译： N，N'-取代-1,3-二氨基-2-氧代戊酸衍生物，其药物组合物和用途
公开(公告)号：WO2005113525A1
公开(公告)日：2005-12-01
申请号：PCT/EP2005/005586
申请日：2005-05-19
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： C07D275/02
CPC分类号： C07D279/02 , C07D207/267 , C07D207/27 , C07D275/02
摘要： The present invention relates to novel ketone compounds having Asp2 (β-secretase, BACE1 or Memapsin 2) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin2）抑制活性的新型酮化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白水平升高或β型为特征的疾病淀粉样蛋白沉积物，特别是阿尔茨海默氏病。

27. 发明申请

WO2004080376A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2004080376A2
公开(公告)日：2004-09-23
申请号：PCT/EP2004/002644
申请日：2004-03-11
申请人： GLAXO GROUP LIMITED , DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
发明人： DEMONT, Emmanuel, Hubert , REDSHAW, Sally , WALTER, Daryl, Simon
IPC分类号： A61K
CPC分类号： C07C311/32 , C07C311/08 , C07C311/09 , C07C311/24 , C07C317/48 , C07C323/63 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D207/267 , C07D209/08 , C07D213/76 , C07D231/12 , C07D275/02
摘要： The present invention relates to novel hydroxyethylamine compounds having Asp2 (β-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated β- amyloid levels or β-amyloid deposits, particularly Alzheimer's disease.
摘要翻译：本发明涉及具有Asp2（β-分泌酶，BACE1或Memapsin）抑制活性的新型羟乙基胺化合物，其制备方法，含有它们的组合物及其用于治疗以β-淀粉样蛋白水平升高或β- 淀粉样沉积物，特别是阿尔茨海默氏病。

28. 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。

29. 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。

30. 发明申请

WO2008125600A3 PYRAZOLE DERIVATIVES AS P2X7 MODULATORS 审中-公开
标题翻译：作为P2X7调节剂的吡唑衍生物
公开(公告)号：WO2008125600A3
公开(公告)日：2009-01-22
申请号：PCT/EP2008054382
申请日：2008-04-10
申请人： GLAXO GROUP LTD , BESWICK PAUL JOHN , DEAN DAVID KENNETH , WALTER DARYL SIMON
发明人： BESWICK PAUL JOHN , DEAN DAVID KENNETH , WALTER DARYL SIMON
IPC分类号： C07D231/12 , A61K31/415 , A61P25/00 , A61P29/00 , C07D231/16
CPC分类号： C07D231/16 , C07D231/12
摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1 represents C1-6 alkyl or C3-6 cycloalkyl, either of which is optionally substituted with 1, 2 or 3 halogen atoms; and R2 represents hydrogen, halogen, C1-6 alkyl or C3-6 cycloalkyl; and either of said C1-6 alkyl or C3-6 cycloalkyl is optionally substituted with 1, 2 or 3 halogen atoms. The pyrazole compounds of formula (I) or salts thereof modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor (P2X7 receptor antagonists). The invention also relates to the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment or prevention of disorders / diseases mediated by the P2X7 receptor, for example pain, inflammation or a neurodegenerative disease.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐：（I）其中R 1表示C 1-6烷基或C 3-6环烷基，其任一个任选被1,2或3个卤素原子取代; 并且R 2表示氢，卤素，C 1-6烷基或C 3-6环烷基; 并且所述C 1-6烷基或C 3-6环烷基中的任一个任选被1,2或3个卤素原子取代。式（I）的吡唑化合物或其盐调节P2X7受体功能，并且能够拮抗ATP在P2X7受体（P2X7受体拮抗剂）下的作用。本发明还涉及这些化合物或其盐或其药物组合物在治疗或预防P2X7受体介导的疾病/疾病中的用途，例如疼痛，炎症或神经变性疾病。

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