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1. 发明申请

WO2010057865A1 N- INDEN- 2 -YL- ISOPROPYLSULFONAMIDES AS AMPA RECEPTOR POTENTIATORS 审中-公开
标题翻译：作为AMPA受体拮抗剂的N-茚-2-基异吲哚磺酰胺
公开(公告)号：WO2010057865A1
公开(公告)日：2010-05-27
申请号：PCT/EP2009/065263
申请日：2009-11-17
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin , WARD, Simon, E
发明人： COULTON, Steven , GILPIN, Martin , WARD, Simon, E
IPC分类号： C07C311/07 , A61K31/18 , A61P25/28 , C07D213/643
CPC分类号： C07D213/643 , C07C311/07 , C07C2602/08
摘要： A compound of formula (I) and salts thereof are provided: Wherein n and R 1 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：其中n和R1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。

2. 发明申请

WO2007113309A2 COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF 审中-公开
标题翻译：抑制甘油运输机及其用途的化合物
公开(公告)号：WO2007113309A2
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053275
申请日：2007-04-03
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin , PORTER, Roderick, Alan
IPC分类号： C07C211/27 , C07C233/78 , C07D295/12 , A61K31/166 , A61K31/40 , A61K31/445 , A61P25/28
CPC分类号： C07C211/27 , C07C233/78 , C07D213/40 , C07D295/13
摘要： Compounds of formula (I) and salts and solvates are provided wherein R 2 is selected from phenyl substituted with n R 1 groups, and pyridyl substituted with n R 1 groups; n = 0, 1 or 2; each R 1 is independently selected from the group consisting of halo, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkyl, haloC 1-4 alkoxy and cyano; R 3 is selected from hydrogen and C 1-2 alkyl; R 4 is selected from the group consisting of ethyl, n- propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R 3 and R 4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C 1-4 alkyl, and haloC 1-4 alkyl; R 12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R 13 is selected from hydrogen, chloro and trifluoromethyl; R 14 is selected from hydrogen, trifluoromethyl and chloro; R 15 is selected from hydrogen, chloro and trifluoromethyl; R 16 is selected from hydrogen, methyl, fluoro and chloro; R 12 , R 13 , R 14 , R 15 and R 16 not all simultaneously being hydrogen. Processes for the preparation and uses of the compounds as medicaments for treating disorders such as psychoses, dementia or attention deficit disorder are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物，其中R 2选自被n R 1基团取代的苯基，和被n R 1取代的吡啶基组 n = 0,1或2; 每个R 1独立地选自卤素，C 1-4烷基，C 1-4烷氧基，卤代C 1 -C 4烷基， 1-4个C 1-4烷基，卤代C 1-4烷氧基和氰基; R 3选自氢和C 1-12烷基; R 4选自乙基，正丙基，异丙基，正丁基，异丁基和叔丁基; 或R 3和R 4与它们所连接的氮原子一起形成任选被一个或多个基团X取代的饱和5或6元杂环; 每个X独立地选自C 1-4烷基和卤代C 1-4烷基; R 12选自氢，氟，氯，溴，甲基和甲硫基; R 13选自氢，氯和三氟甲基; R 14选自氢，三氟甲基和氯; R 15选自氢，氯和三氟甲基; R 16选自氢，甲基，氟和氯; R 12，R 13，R 14，R 15和R 16不是全部同时为氢。还公开了用于制备和使用化合物作为治疗诸如精神病，痴呆或注意力缺陷障碍之类疾病的药物的方法。

3. 发明公开

EP2001831A2 COMPOUNDS WHICH INHIBIT THE GLYCINE TRANSPORTER AND USES THEREOF 审中-公开
标题翻译：抑制甘氨酸转运蛋白的化合物及其用途
公开(公告)号：EP2001831A2
公开(公告)日：2008-12-17
申请号：EP07727746.5
申请日：2007-04-03
申请人： GLAXO GROUP LIMITED
发明人： COULTON, Steven , GILPIN, Martin , PORTER, Roderick, Alan
IPC分类号： C07C211/27 , C07C233/78 , C07D295/12 , A61K31/166 , A61K31/40 , A61K31/445 , A61P25/28
CPC分类号： C07C211/27 , C07C233/78 , C07D213/40 , C07D295/13
摘要： Compounds of formula (I) and salts and solvates are provided wherein R2 is selected from phenyl substituted with n R1 groups, and pyridyl substituted with n R1 groups; n = 0, 1 or 2; each R1 is independently selected from the group consisting of halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and cyano; R3 is selected from hydrogen and C1-2 alkyl; R4 is selected from the group consisting of ethyl, n- propyl, i-propyl, n-butyl, i-butyl and t-butyl; or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic ring optionally substituted with one or more groups X; each X is independently selected from the group consisting of C1-4alkyl, and haloC1-4alkyl; R12 is selected from the group consisting of hydrogen, fluoro, chloro, bromo, methyl and methylthio; R13 is selected from hydrogen, chloro and trifluoromethyl; R14 is selected from hydrogen, trifluoromethyl and chloro; R15 is selected from hydrogen, chloro and trifluoromethyl; R16 is selected from hydrogen, methyl, fluoro and chloro; R12, R13, R14, R15 and R16 not all simultaneously being hydrogen. Processes for the preparation and uses of the compounds as medicaments for treating disorders such as psychoses, dementia or attention deficit disorder are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂化物，其中R2选自被n个R1基团取代的苯基和被n个R1基团取代的吡啶基; n = 0,1或2; 每个R 1独立地选自卤素，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷基，卤代C 1-4烷氧基和氰基; R3选自氢和C1-2烷基; R4选自乙基，正丙基，异丙基，正丁基，异丁基和叔丁基; 或者R 3和R 4与它们所连接的氮原子一起形成任选被一个或多个基团X取代的饱和5-或6-元杂环; 每个X独立地选自C 1-4烷基和卤代C 1-4烷基; R12选自氢，氟，氯，溴，甲基和甲硫基; R13选自氢，氯和三氟甲基; R14选自氢，三氟甲基和氯; R15选自氢，氯和三氟甲基; R16选自氢，甲基，氟和氯; R12，R13，R14，R15和R16不全都是氢。还公开了用于制备和使用化合物作为用于治疗诸如精神病，痴呆或注意力缺陷障碍的病症的药物的方法。

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