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11. 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。

12. 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。

13. 发明申请

WO2007090840A1 4-PHENYL-3-(2-PROPYLSULFONYLAMINO) TETRAHYDROFURAN DERIVATIVES WHICH POTENTIATE GLUTAMATE RECEPTORS AND ARE USEFUL IN THE TREATMENT OF SCHIZOPHRENIA 审中-公开
标题翻译： 4-苯基-3-（2-丙磺酰氨基）四氢呋喃衍生物，它们是谷氨酸受体，并且有助于治疗苦参碱
公开(公告)号：WO2007090840A1
公开(公告)日：2007-08-16
申请号：PCT/EP2007/051132
申请日：2007-02-06
申请人： GLAXO GROUP LIMITED , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D307/22 , C07D405/10 , C07D407/10 , A61K31/443 , A61P25/18
CPC分类号： C07D307/22 , C07D405/10 , C07D407/10 , C07D409/10
摘要： Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl and thienyl optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C 1 - 4 alkyl, haloC 1 - 4 alkyl, C 1-4 alkoxy, cyano, C(O) C 1 - 4 alkyl, NHSO 2 C 1 - 4 alkyl, NMeSO 2 C 1-4 alkyl, NHCOC 1 - 4 alkyl, NMeCOC 1 - 4 alkyl, SOC 1 - 4 alkyl, SO 2 C 1-4 alkyl and CO 2 C 1-4 alkyl, or two Y groups together form a cyclic group -O(CH 2 )O-. Processes for preparation, and uses thereof 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，其盐和溶剂化物：其中Ar选自苯基，吡啶基和任选被一个或多个Y基团取代的噻吩基; 并且每个Y基团独立地选自：卤素，C 1 -C 4 - 烷基，卤代C 1 - 烷基，C 1-4烷氧基，氰基，C（O）C 1-4烷基，NHSO 2， N 1 -C 1-4烷基，NH 2 SO 2，C 1-4烷基，NHCOC 1 烷基，N 1 -C 1-4烷基，-SO 2 - ， - ， - 烷基，SO 2 C 1-4烷基和C 2 -C 1-4烷基，或者C 1 -C 4烷基，或两个Y基团一起形成环状基团-O（CH 2 CH 2）O-。还公开了制备方法及其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的用途。

14. 发明申请

WO2006015827A1 COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的谷氨酸受体的化合物及其在医药中的应用
公开(公告)号：WO2006015827A1
公开(公告)日：2006-02-16
申请号：PCT/EP2005/008559
申请日：2005-08-05
申请人： GLAXO GROUP LIMITED , THEWLIS, Kevin, Michael , WARD, Simon, Edward
发明人： THEWLIS, Kevin, Michael , WARD, Simon, Edward
IPC分类号： C07D207/14
CPC分类号： C07D207/14 , C07D403/10 , C07D409/10
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R 1 is C 1 - 6 alkyl, haloC 1-6 alkyl, C 2-6 alkenyl, amino, monoC 1-4 alkylamino or diC 1-4 alkylamino; B is -N(R 4 )- or -0-; A and D, which may be the same or different, are -C(R 5 ) 2- ; each R 2 , which may be the same or different, is C 1-6 alkyl, halogen, haloC l-6 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, cyano, nitro or amino; n is 0, 1 or 2; R 3 is C 1-6 alkyl, haloC l-6 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, cyano, nitro, amino, -(CH 2 ) p NR 3a SO 2 R 3b ,-(CH 2 ) p NR 3a (C=O)R 3b , -(CH 2 ) p NR 3a (C=O)N(R 3c ) 2 , -(CH 2 ) p (C=O)R 3d , -(CH 2 ) p SO 2 R 3e , phenyl or heterocyclyl, wherein when R 3 is phenyl or heterocyclyl, it is optionally substituted by one or more groups independently selected from: C 1-6 alkyl, halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, cyano, nitro, amino, -(CH 2 ) p NR 3a SO 2 R 3b , -(CH 2 ) p NR 3a (C=O)R 3b , -(CH 2 ) p NR 3a (C=O)N(R 3c )2 -(CH 2 ) p (C=O)R 3d and -(CH 2 )pSO 2 R 3e ; where R 3a and each R 3c , which may be the same or different, is hydrogen or C 1-6 alkyl; R 3b and R 3e are C 1-6 alkyl or haloC l-6 alkyl; R 3d is C 1-6 alkyl, C 1-4 alkoxy or haloC 1-6 alkyl; or R 3a and R 3b , or R 3a and R 3c , together with the interconnecting atoms, may form a 5- or 6-membered ring; and p is 0, 1, or 2; R 4 is carbocyclyl or carbocyclylC 1-4 alkyl, wherein the carbocyclyl group of either is optionally substituted by one or more groups independently selected from C 1-6 alkyl and halogen; or R 4 is hydrogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkylcarbonyl, C l-6 alkylsulfonyl or C 1-6 alkylaminocarbonyl; each R 5 , which may be the same or different, is hydrogen, C 1- 6 alkyl or halogen; and R 6 is hydrogen or fluorine. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，溶剂化物或前体药物：其中R

15. 发明申请

WO2006015829A1 COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的谷氨酸受体的化合物及其在医药中的应用
公开(公告)号：WO2006015829A1
公开(公告)日：2006-02-16
申请号：PCT/EP2005/008563
申请日：2005-08-05
申请人： GLAXO GROUP LIMITED , WARD, Simon, Edward , THEWLIS, Kevin, Michael
发明人： WARD, Simon, Edward , THEWLIS, Kevin, Michael
IPC分类号： C07C311/07
CPC分类号： C07D207/27 , C07C311/07 , C07C311/08 , C07C311/37 , C07C317/28 , C07C2602/08 , C07D275/02
摘要： Compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1 4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino; each R4, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R5, which may be the same or different, is C1-6alkyl, halogen, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro or amino; q is 0,1 or 2; R6 is -NR6aSO2R6b, -NR6aC(=O)R6b, -NR6a(C=O)N(R6c)2, -(C=O)R6d, CH2NR6aSO2R6b, -CH2NR6aC(=O)R6b, -CH2NR6a(C=O)N(R6c)2 or CH2(C=O)R6d; where R6a and each R6c, which may be the same or different, is hydrogen or C1-6alkyl; R6b and R6d are C1-6alkyl or haloC1-6alkyl; or R6a and R6b, or R6a and R6c, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and R7 and R8, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano or amino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.
摘要翻译：公开了式（I）化合物，其药学上可接受的盐，溶剂化物或前体药物：其中R1是C1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，一C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; p为0,1或2; 每个R 5可以相同或不同，是C 1-6烷基，卤素，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基或氨基; q为0,1或2; R6是-NR6aSO2R6b，-NR6aC（= O）R6b，-NR6a（C = O）N（R6c）2， - （C = O）R6d，CH2NR6aSO2R6b，-CH2NR6aC（= O）R6b，-CH2NR6a（C = O ）N（R6c）2或CH2（C = O）R6d; 其中R 6a和R 6c可以相同或不同，是氢或C 1-6烷基; R6b和R6d是C1-6烷基或卤代C 1-6烷基; 或R6a和R6b或R6a和R6c与互连原子一起可以形成5-或6-元环; n为1或2; 和可以相同或不同的R 7和R 8是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基或氨基。还公开了化合物的制备方法及其在药物中的用途，例如精神分裂症的治疗。

16. 发明申请

WO2002089800A2 N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为OREXIN受体拮抗剂的N-阿洛尔循环胺衍生物
公开(公告)号：WO2002089800A2
公开(公告)日：2002-11-14
申请号：PCT/EP2002/004874
申请日：2002-05-03
申请人： SMITHKLINE BEECHAM P.L.C. , GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
发明人： GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
IPC分类号： A61K31/445
CPC分类号： C07D265/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/14
摘要： This invention relates to N-aroyl cyclic amine derivatives of formula (I): wherein: Y represents a bond, oxygen, or a group (CH 2 ) n , wherein n represents 1, 2 or 3 m represents 1, 2 or 3; p represents 0 or 1; X is O,SC=O, SO 2 , or -CH=CH; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents phenyl or a 5- or 5-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R 1 and further optional substituents; or Ar 2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R 1 represents hydrogen, optionally substituted (C 1-4 )alkoxy, halo, cyano, optionally substituted (C 1-16 )alkyl, optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acceptable salt thereof; and their use as pharmaceuticals, specifically as orexin receptor antagonists.
摘要翻译：本发明涉及式（I）的N-芳酰基环胺衍生物：其中：Y表示键，氧或基团（CH 2）n，其中n表示1,2或3m表示1,2或3; p表示0或1; X是O，SC = O，SO 2或-CH = CH; Ar 1是芳基或含有至多4个选自N，O和S的杂原子的单或双环杂芳基; 任何一个可以任选地被取代; Ar 2表示苯基或含有至多3个选自N，O和S的杂原子的5或5元杂环基，其中苯基或杂环基被R 1取代，另外任选的取代基; 或Ar 2表示含有至多3个选自N，O和S的杂原子的任选取代的双环芳族或双环杂芳族基团; R 1表示氢，任选取代的（C 1-4）烷氧基，卤素，氰基，任选取代的（C 1-6）烷基，任选取代的含有至多4个选自N，O的杂原子的5-或6-元杂环， S; 或其药学上可接受的盐; 以及它们作为药物的用途，特别是作为食欲素受体拮抗剂。

17. 发明申请

WO2002089800A3 N-AROYL CYCLIC AMINE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2002089800A3
公开(公告)日：2002-11-14
申请号：PCT/EP2002/004874
申请日：2002-05-03
申请人： SMITHKLINE BEECHAM P.L.C. , GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
发明人： GAILLARD, Pascale , JOHNSON, Christopher, Norbert , NOVELLI, Riccardo , PORTER, Roderick, Alan , STEMP, Geoffrey , THEWLIS, Kevin, Michael
IPC分类号： A61K31/445
摘要： This invention relates to N -aroyl cyclic amine derivatives of formula (I), wherein: Y represents a bond, oxygen, or a group (CH 2 ) n , wherein n represents 1, 2 or 3; m represents 1, 2 or 3; p represents 0 or 1; X is O, S C=O, SO 2 , or -CH=CH-; Ar 1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; any of which may be optionally substituted; Ar 2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R 1 and further optional substituents; or Ar 2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R 1 represents hydrogen, optionally substituted (C 1-4 )alkoxy, halo, cyano, optionally substituted (C 1-6 )alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 4 heteroatoms selected from N, O and S; or a pharmaceutical acceptable salt thereof; and their use as pharmaceuticals, specifically as orexin receptor antagonists.

18. 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。

19. 发明申请

WO2003068760A2 COMPOUNDS POSSESSING AFFINITY AT 5HT1-TYPE RECEPTORS AND USE THEREOF IN THERAPY 审中-公开
标题翻译：化合物在5HT1型受体中的有益作用及其在治疗中的应用
公开(公告)号：WO2003068760A2
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001709
申请日：2003-02-17
申请人： GLAXO GROUP LIMITED , SMITH, Paul, W , THEWLIS, Kevin, Michael , VONG, Antonio, Kuok, Keong , WARD, Simon, E
发明人： SMITH, Paul, W , THEWLIS, Kevin, Michael , VONG, Antonio, Kuok, Keong , WARD, Simon, E
IPC分类号： C07D295/00
CPC分类号： C07D401/12 , C07D215/20 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: (I) wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; R1 is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4 and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. 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：（I）其中：A为任选取代的苯基，萘基，吲哚基，喹啉基，喹唑啉基，吲唑基，异喹啉基或苯并呋喃基; 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，羟基，氰基，C 1-6烷基，卤代C 1-6烷基或C 1-6烷氧基; a是0，1，2，3或4; R2和R3与它们所连接的氮原子一起形成硝基或任选取代的3至7元杂环基，或者R 2和R 3独立地是氢，芳酰基，C 1-6烷基，C 1-6烷酰基，氟C 1-6烷基， C 1-6烷酰基，C 1-6烷基磺酰基，氟C 1-6烷基磺酰基，氨基甲酰基，C 1-6烷基氨基甲酰基，芳基C 1-6烷基或CO（CH 2）b NR 4 R 5基团，其中b为1,2,3或4，并且R 4和R 5独立地为氢或C 1-6烷基，或 R4和R5与它们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。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。

20. 发明申请

WO2009092712A1 COMPOUNDS WHICH POTENTIATE THE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：可能拮抗AMPA受体的化合物及其在医药中的应用
公开(公告)号：WO2009092712A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050607
申请日：2009-01-21
申请人： GLAXO GROUP LIMITED , THEWLIS, Kevin, Michael , WARD, Simon, E.
发明人： THEWLIS, Kevin, Michael , WARD, Simon, E.
IPC分类号： C07C311/08 , A61K31/18 , A61P25/18
CPC分类号： C07C311/08 , C07C2601/08
摘要： This invention relates to by novel N-(phenyl-1, 3-cyclopentyl)sulphonamide derivatives formula (I) and salts thereof: wherein R 1 to R 9 and p are as defined in the description. The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及新的N-（苯基-1,3-环戊基）磺酰胺衍生物式（I）及其盐：其中R1至R9和p如说明书中所定义。本发明还涉及该衍生物在治疗通过增强谷氨酸受体介导的疾病和病症中的用途，含有衍生物的组合物及其制备方法。

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