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1. 发明申请

WO2007147834A1 GLYCINE TRANSPORTER INHIBITING COMPOUNDS AND USES IN MEDICINE 审中-公开
标题翻译： GLYCINE运输机抑制化合物和药物用途
公开(公告)号：WO2007147834A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056112
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
IPC分类号： C07C323/62 , C07D295/135 , A61K31/166 , A61K31/40 , A61P25/18
CPC分类号： C07C323/62 , C07C2601/08 , C07D295/125 , C07D295/135
摘要： Compounds of formula (I) and salts and solvates thereof are provided: wherein either 1 ) R1, R2, R3 and R4 and all methyl, or 2) R1 and R2 form a pyrrolidinyl group and R3 and R4 are both methyl, or 3) R1 and R2 are both methyl and R3 and R4 together form a cyclopentyl group. Uses in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, such as psychoses, dementia or attention deficit disorder, and processes to make these compounds and pharmaceutical formulations thereof are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物：其中1）R1，R2，R3和R4以及全部甲基，或2）R1和R2形成吡咯烷基，R3和R4均为甲基，或3） R1和R2都是甲基，R3和R4一起形成环戊基。还公开了用于制备用于治疗神经和神经精神障碍的药物的用途，例如精神病，痴呆或注意力缺陷障碍，以及制备这些化合物及其药物制剂的方法。

2. 发明申请

WO2006094840A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006094840A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002480
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , A61P25/00 , A61K31/495
CPC分类号： C07D295/192
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

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

WO2007147839A1 GLYCINE TRANSPORTER INHIBITING COMPOUNDS AND USES IN MEDICINE 审中-公开
标题翻译：甘氨酸转运蛋白抑制化合物和药物用途
公开(公告)号：WO2007147839A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056120
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
IPC分类号： C07C235/50 , C07C235/60 , C07D295/12 , A61K31/166
CPC分类号： C07C235/60 , C07D295/13
摘要： Compounds of formula (I) and salts and solvates thereof are provided: wherein R1 and R2 are both methyl, or R1 and R2 form a pyrrolidinyl group. Uses in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, such as psychoses, dementia or attention deficit disorder, and processes to make these compounds and pharmaceutical formulations thereof are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物：其中R1和R2均为甲基，或R1和R2形成吡咯烷基。还公开了用于治疗神经和神经精神障碍的药物的用途，例如精神病，痴呆或注意力缺陷障碍，以及制备这些化合物及其药物制剂的方法。

5. 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。

6. 发明申请

WO2006067414A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006067414A2
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004937
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BOZZOLI, Andrea , BRADLEY, Daniel, Marcus , COULTON, Steven , GILPIN, Martin, Leonard , MACRITCHIE, Jacqueline, Anne , PORTER, Roderick, Alan , THEWLIS, Kevin, Michael
发明人： BOZZOLI, Andrea , BRADLEY, Daniel, Marcus , COULTON, Steven , GILPIN, Martin, Leonard , MACRITCHIE, Jacqueline, Anne , PORTER, Roderick, Alan , THEWLIS, Kevin, Michael
IPC分类号： C07C233/78 , C07D409/12 , C07D215/50 , C07D333/20 , A61K31/166 , A61K31/381 , A61K31/47 , C07C211/36 , C07C211/29
CPC分类号： C07C211/36 , C07C211/29 , C07C229/34 , C07C233/78 , C07C271/22 , C07C2601/08 , C07D215/50 , C07D295/13 , C07D333/20 , C07D409/12
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，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。

7. 发明申请

WO2007147836A1 GLYCINE TRANSPORTER INHIBITING COMPOUNDS AND USES IN MEDICINE 审中-公开
标题翻译：甘氨酸转运蛋白抑制化合物和药物用途
公开(公告)号：WO2007147836A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056115
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
发明人： COULTON, Steven , GILPIN, Martin, Leonard , PORTER, Roderick, Alan
IPC分类号： C07C235/60 , A61K31/166 , A61P25/18
CPC分类号： C07C235/60 , C07C2601/08
摘要： N -[[1-dimethylaminojcyclopentyl](phenyl)methyl]-4-fluoro-2-methyl-6- (methyloxy)benzamide:and salts and solvates thereof are provided. Uses in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, such as psychoses, dementia or attention deficit disorder, and processes to make these compounds and pharmaceutical formulations thereof are also disclosed.
摘要翻译： N - [[1-

8. 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。

9. 发明申请

WO2006094843A1 PIPERAZINE DERIVATIVES AS GLYT1 INHIBITORS 审中-公开
标题翻译：哌嗪衍生物作为GLYT1抑制剂
公开(公告)号：WO2006094843A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002485
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , BROWN, Bethany, Joy , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , STASI, Luigi, Piero
IPC分类号： C07D295/18 , C07D239/42 , C07D241/44 , C07D215/38 , C07D487/04 , C07D213/85 , C07D213/73 , C07D213/75 , A61P25/00 , A61K31/495 , A61K31/5377 , A61K31/4709 , A61K31/444 , A61K31/437 , A61K31/498
CPC分类号： C07D213/73 , C07D213/75 , C07D213/85 , C07D215/38 , C07D239/42 , C07D241/44 , C07D295/192 , C07D487/04
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

10. 发明申请

WO2006094842A1 ACYLATED PIPERIDIHES AS GLYCINE TRANSPORTER INHIBITORS 审中-公开
标题翻译：丙酰胆碱作为甘氨酸运输抑制剂
公开(公告)号：WO2006094842A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/002484
申请日：2006-03-09
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , WARD, Simon, Edward
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , CHAN, Wai, Ngor , COULTON, Steven , DEAN, Anthony, William , DOYLE, Paul, Martin , EVANS, Brian , GILPIN, Martin, Leonard , GOUGH, Sharon, Lisa , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , NASH, David, John , PORTER, Roderick, Alan , WARD, Simon, Edward
IPC分类号： C07D295/18 , C07D307/38 , C07D307/54 , C07D213/56 , C07D209/08 , C07D471/04 , C07D307/64 , C07D231/12 , A61P25/00 , A61K31/445 , A61K31/4523 , A61K31/4525 , A61K31/4545
CPC分类号： C07D231/12 , C07D209/08 , C07D213/56 , C07D213/74 , C07D295/192 , C07D307/54 , C07D333/24 , C07D405/12 , C07D471/04
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 , n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂化物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

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