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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

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

WO2004026866A1 N-AROYL CYCLIC AMINES AS OREXIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译： N-亚油酸环化酶作为OREXIN受体拮抗剂
公开(公告)号：WO2004026866A1
公开(公告)日：2004-04-01
申请号：PCT/EP2003/010412
申请日：2003-09-17
申请人： GLAXO GROUP LIMITED , BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , NASH, David, John , PORTER, Roderick, Alan , STEMP, Geoffrey
发明人： BRANCH, Clive, Leslie , COULTON, Steven , JOHNS, Amanda , NASH, David, John , PORTER, Roderick, Alan , STEMP, Geoffrey
IPC分类号： C07D417/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D401/14 , C07D417/14
摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及N-芳酰基环胺衍生物及其作为药物的用途。

8. 发明申请

WO2003051873A1 PIPERAZINE COMPOUNDS AND THEIR PHAMACEUTICAL USE 审中-公开
标题翻译：哌嗪化合物及其药物用途
公开(公告)号：WO2003051873A1
公开(公告)日：2003-06-26
申请号：PCT/GB2002/005676
申请日：2002-12-13
申请人： SMITHKLINE BEECHAM PLC , BRANCH, Clive, Leslie , COULTON, Steven , NASH, David, John , PORTER, Roderick, Alan
发明人： BRANCH, Clive, Leslie , COULTON, Steven , NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D417/14
CPC分类号： C07D401/14 , C07D403/14 , C07D417/14
摘要： This invention relates to piperazine derivatives and their use as pharmaceuticals.
摘要翻译：本发明涉及哌嗪衍生物及其作为药物的用途。

9. 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。

10. 发明申请

WO2004113301A1 GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译： GLYT1运输商抑制剂及其在治疗神经病学和神经病学疾病中的应用
公开(公告)号：WO2004113301A1
公开(公告)日：2004-12-29
申请号：PCT/EP2004/006593
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , BRANCH, Clive, Leslie , COULTON, Steven , PORTER, Roderick, Alan
发明人： BRANCH, Clive, Leslie , COULTON, Steven , PORTER, Roderick, Alan
IPC分类号： C07D215/58
CPC分类号： C07D209/08 , C07D209/44 , C07D215/58 , C07D217/06
摘要： Compounds of formula (I), salts, solvates and physiologically functional derivatives thereof are provided: formula (I) wherein R 1 and R 2 is independently selected from hydrogen, optionally substituted C 1-6 alkyl, optionally substituted C 3-6 cycloalkyl, optionally substituted aryl, optionally substituted arylC 1-4 alkyl and optionally substituted arylC 3-6 cycloalkyl, wherein R 1 and R 2 are not both hydrogen, or R 1 and R 2 , together with the nitrogen atom to which they are attached, are linked to form an optionally substituted 4-, 5-, 6- or 7-membered saturated ring, wherein one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S; R 3 is an optionally substituted group of formula (a): wherein m and n are independently 0, 1, 2 or 3 and m+n is 2, 3 or 4; each Z is independently -CH 2 -, -NH-, -O- or -S-; and each Y is independently CH or N; R 4 and R 5 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 6 cycloalkyl, optionally substituted aryl and optionally substituted arylC 1 -C 4 alkyl; and R 6 , R 7 , R 8 and R 9 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl and optionally substituted arylC 1 -C 4 alkyl, or R 6 and R 7 together form an optionally substituted C 3 -C 6 cycloalkyl group, or R 8 and R 9 together form an optionally substituted C 3 -C 6 cycloalkyl group. Methods of preparation and uses of the compounds in medicine for the treatment of a disorder mediated by GlyT1, for example schizophrenia, are also disclosed.
摘要翻译：提供式（I）化合物，其盐，溶剂化物和生理功能衍生物：式（I）其中R 1和R 2独立地选自氢，任选取代的C 1-6烷基，任选取代的C 3-6环烷基，任选取代的芳基，任选取代的芳基C 1-4烷基和任选取代的芳基C 3-6环烷基，其中R 1和R 2不是氢或R 1和R 2都与氮原子一起被连接以形成任选取代的4-，5-，6-或7-元饱和环，其中一个或多个碳原子任选被独立地选自N，O和S的杂原子取代; R 3是式（a）的任选取代的基团：其中m和n独立地是0,1,2或3，m + n是2,3或4; 每个Z独立地是-CH 2 - ， - NH - ， - O-或-S-; 并且每个Y独立地是CH或N; R 4和R 5独立地选自氢，任选取代的C 1 -C 6烷基，任选取代的C 3 -C 6环烷基，任选取代的芳基和任选取代的芳基C 1 -C 4烷基; R 6，R 7，R 8和R 9独立地选自氢，任选取代的C 1 -C 6烷基和任选取代的芳基C 1 -C 4烷基，或R 6和R 7独立地选自氢，一起形成任选取代的C 3 -C 6环烷基，或R 8和R 9一起形成任选取代的C 3 -C 6环烷基。还公开了用于治疗由GlyT1介导的病症（例如精神分裂症）的医药中化合物的制备和用途的方法。

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