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1. 发明申请

WO2009053449A1 THIAZOLES WHICH POTENTIATE AMPA RECEPTOR AND MEDICINAL USES THEREOF 审中-公开
标题翻译：潜在的AMPA受体的THIAZOLES及其药物用途
公开(公告)号：WO2009053449A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064408
申请日：2008-10-24
申请人： GLAXO GROUP LIMITED , CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, E.
发明人： CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, E.
IPC分类号： C07D277/42 , C07D417/12 , A61K31/426 , A61K31/44 , A61P25/18
CPC分类号： C07D277/42 , C07D417/12
摘要： The invention provides compounds of formula (I) and salts thereof: wherein R1, R2, R3, R4 and X are as defined in the description. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：本发明提供式（I）化合物及其盐：其中R1，R2，R3，R4和X如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

2. 发明申请

WO2009053448A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2009053448A1
公开(公告)日：2009-04-30
申请号：PCT/EP2008/064407
申请日：2008-10-24
申请人： GLAXO GROUP LIMITED , CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen, Rhys , NEESOM, James, Kenneth , THEWLIS, Kevin, Michael , WARD, Simon, E
发明人： CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen, Rhys , NEESOM, James, Kenneth , THEWLIS, Kevin, Michael , WARD, Simon, E
IPC分类号： C07D263/48 , C07D417/12 , A61K31/427 , A61P25/00
CPC分类号： C07D277/42 , C07D417/12 , C07D491/052
摘要： The invention provides compounds of formula (I) and salts thereof wherein R1, R2, R3, R4 and X are as defined in the description. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：本发明提供式（I）化合物及其盐，其中R 1，R 2，R 3，R 4和X如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

3. 发明申请

WO2006067423A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067423A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004951
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/36
CPC分类号： C07C233/78 , C07C235/50 , C07C235/60 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/02 , C07D295/13 , C07D307/22
摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂化物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

4. 发明申请

WO2007107539A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2007107539A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052568
申请日：2007-03-19
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , THATCHER, Robert , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , THATCHER, Robert , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D231/56 , C07D401/10 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/10 , C07D417/10 , A61K31/416 , A61P25/00
CPC分类号： C07D403/12 , C07D231/56 , C07D401/10 , C07D403/10 , C07D405/12 , C07D409/12 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) and salts and solvates are provided: formula (I). Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂化物：式（I）。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

5. 发明申请

WO2008053031A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008053031A1
公开(公告)日：2008-05-08
申请号：PCT/EP2007/061794
申请日：2007-11-01
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： A61P25/18 , C07D471/04 , C07D491/052 , A61K31/416 , A61K31/4162
CPC分类号： C07D491/052 , C07D471/04
摘要： Compounds of formula (I), and salts and solvates thereof are provided. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂化物。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

6. 发明申请

WO2007122241A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医药中的应用
公开(公告)号：WO2007122241A1
公开(公告)日：2007-11-01
申请号：PCT/EP2007/054007
申请日：2007-04-24
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen , MILLER, David, Drysdale , NEESOM, James , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen , HUGHES, Owen , MILLER, David, Drysdale , NEESOM, James , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D263/48 , C07D277/42 , C07D417/12 , A61K31/421 , A61K31/426 , A61K31/427 , A61P25/00
CPC分类号： C07D263/48 , C07D265/30 , C07D277/42 , C07D417/12
摘要： Compounds of formula (I), and salts and solvates thereof for use as a medicament are provided: (I) wherein R 1 , R 2 , R 4 , R 10 , X and Z are defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物用作药物：（I）其中R 1，R 2，R 4， / SUP>，R 10，X和Z在说明书中定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗由谷氨酸受体功能的减少或不平衡（如精神分裂症或认知障碍）介导的疾病或病症。

7. 发明申请

WO2008110566A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008110566A1
公开(公告)日：2008-09-18
申请号：PCT/EP2008/052906
申请日：2008-03-12
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen, Anthony , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , CHAN, Wai, Ngor , HARRISON, Stephen, Anthony , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10 , A61K31/416 , A61P25/00
CPC分类号： C07D231/56 , C07D401/04 , C07D401/14 , C07D403/10 , C07D417/10
摘要： A compound of formula (I) and salts thereof are provided: wherein A is defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中A在说明书中定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

8. 发明申请

WO2006067417A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：WO2006067417A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004943
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , GILPIN, Martin, Leonard , HARRIS, Andrew, Jonathan , LAI, Justine, Yeun, Quai , MARSHALL, Howard, Robert , MACRITCHIE, Jacqueline, Anne , NASH, David, John , PORTER, Roderick, Alan , SPADA, Simone , THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07C233/78 , A61K31/166 , C07C211/27
CPC分类号： C07C235/60 , C07C211/27 , C07C233/78 , C07C235/50 , C07C323/62
摘要： The present invention relates to compounds of Formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，它们在制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物中的用途。本发明还包括制备这些化合物及其药物制剂的方法。

9. 发明申请

WO2008148832A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEROF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：WO2008148832A1
公开(公告)日：2008-12-11
申请号：PCT/EP2008/056961
申请日：2008-06-05
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , THEWLIS, Kevin, Michael , WARD, Simon, E.
发明人： BRADLEY, Daniel, Marcus , THEWLIS, Kevin, Michael , WARD, Simon, E.
IPC分类号： C07D231/56 , C07D403/10 , C07D417/10 , A61K31/416 , A61P25/00 , C07D231/54 , C07D471/04
CPC分类号： C07D231/56 , C07D231/54 , C07D403/10 , C07D417/10 , C07D471/04
摘要： Compound of formula (I) and salts thereof are provided: wherein X, Y, Z, R 1 , R 2 and R 3 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐：其中X，Y，Z，R 1，R 2和R 3如说明书中所定义。还公开了制备方法，药物组合物及其作为药物的用途，例如用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症。

10. 发明申请

WO2003068236A1 PIPERIDINE AND PIPERAZINE DERIVATIVES POSSESSING AFFINITY AT 5HT-1 TYPE RECEPTORS 审中-公开
标题翻译： 5HT-1型受体的磷酸和哌嗪衍生物
公开(公告)号：WO2003068236A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001710
申请日：2003-02-17
申请人： GLAXO GROUP LIMITED , FLYNN, Sean, Thomas , SMITH, Paul, W , THEWLIS, Kevin, Michael , WARD, Simon, E , WYMAN, Paul, Adrian
发明人： FLYNN, Sean, Thomas , SMITH, Paul, W , THEWLIS, Kevin, Michael , WARD, Simon, E , WYMAN, Paul, Adrian
IPC分类号： A61K31/495
CPC分类号： C07D401/12 , C07D215/20 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A is optionally substituted phenyl, indolyl, quinolinyl, quinazolinyl, indazolyl or isoquinolinyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH 2 or oxygen and is a single bond; or X is nitrogen, Y is CH 2 and is a single bond; R1 is halogen, cyano, nitro, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, C 3-7 heterocyclylC 1-6 alkyl, C 3-7 heterocyclyl C 1-6 alkoxy; a is 0, 1, 2, 3 or 4; R2 is either: halogen, -CN, an optionally substituted C 3-7 cycloalkyl, an optionally substituted aryl or an optionally substituted C-linked 3-7 membered heterocyclic group; or a group -(Z)b-B wherein: (i) Z is oxygen, CH 2 , C=O, SO 2 or C=N-OR3 wherein R3 is hydrogen or C 1-6 alkyl; b is 1, 2, or 3; and B is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkanoyl, fluoroC 1-6 alkanoyl, C 1-6 alkylsulfonyl, fluoroC¿ 1-6 alkylsulfonyl, carbamoyl or C 1-6 alkylcarbamoyl, or R4 and R5, together with the nitrogen atom to which they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group; or (ii) Z is oxygen, CH or CH 2 , b is 1, and B forms the rest of an aryl or a C 3-7 heterocyclic group fused to the phenyl ring; excluding 1-[2-[2-(phenylmethyl)phenoxy]ethyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine and pharmaceutically acceptable salts thereof, and N-[4-[2-[4-[(3,4-dimethoxyphenyl)methyl]-1-piperazinyl]ethoxy]phenyl]-ethanesulfonamide and pharmaceutically acceptable salts thereof. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中A是任选取代的苯基，吲哚基，喹啉基，喹唑啉基，吲唑基或异喹啉基; X是碳，Y是CH并且是双键; 或X是CH，Y是CH 2或氧并且是单键; 或X为氮，Y为CH 2且为单键; R 1是卤素，氰基，硝基，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基，C 3-7杂环基C 1-6烷基，C 3-7杂环基C 1-6烷氧基; a是0，1，2，3或4; R 2是：卤素，-CN，任选取代的C 3-7环烷基，任选取代的芳基或任选取代的C-连接的3-7元杂环基; 或（Z）b-B基团，其中：（i）Z是氧，CH 2，C = O，SO 2或C = N-OR 3，其中R 3是氢或C 1-6烷基; b为1,2或3; 并且B是氢，C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或NR 4 R 5，其中R 4和R 5独立地是氢，C 1-6烷基，C 3-7环烷基，C 1-6烷酰基，氟C 1-6烷酰基，C 1 -6烷基磺酰基，氟代C 1-6烷基磺酰基，氨基甲酰基或C 1-6烷基氨基甲酰基，或者R 4和R 5与它们所连接的氮原子一起形成任选取代的3至7元杂环基的一部分; 或（ii）Z是氧，CH或CH 2，b是1，B形成与苯环稠合的芳基或C 3-7杂环基的其余部分; 不包括1- [2- [2-（苯基甲基）苯氧基]乙基] -4 - [（2,3,4-三甲氧基苯基）甲基] - 哌嗪及其药学上可接受的盐，以及N- [4- [2- [4 - [（3,4-二甲氧基苯基）甲基] -1-哌嗪基]乙氧基]苯基] - 乙磺酰胺及其药学上可接受的盐。还公开了制备化合物的方法和化合物在治疗中的用途，特别是CNS障碍如抑郁和焦虑。

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