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41. 发明申请

WO2008092877A3 8-OXA-1, 4-DIAZASPIRO [4,5] DEC-3-EN-1-YL AND 1,4, 8-TRIAZASPIRO [4,5] DEC- 3-EN-1-YL ACETAMIDES AS GLYTI TRANSPORTER INHIBITORS IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译： 8-OXA-1,4-DIAZASPIRO [4,5] DEC-3-EN-1-YL和1,4,8-三氮唑[4,5] DEC-3-EN-1-YL乙酰胺作为GLYTI运输机抑制剂治疗神经病学和神经功能障碍
公开(公告)号：WO2008092877A3
公开(公告)日：2008-10-02
申请号：PCT/EP2008051083
申请日：2008-01-30
申请人： GLAXO GROUP LTD , UNIV NOTTINGHAM , AHMAD NADIA MAMOONA , LAI JUSTINE YEUN QUAI , MARSHALL HOWARD ROBERT , NASH DAVID JOHN , PORTER RODERICK ALAN
发明人： AHMAD NADIA MAMOONA , LAI JUSTINE YEUN QUAI , MARSHALL HOWARD ROBERT , NASH DAVID JOHN , PORTER RODERICK ALAN
IPC分类号： C07D471/10 , A61K31/4188 , A61K31/438 , A61P25/18 , A61P25/28 , C07D491/10
CPC分类号： C07D471/10 , C07D491/10
摘要： Compounds of formula (I) or a salt thereof are provided wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , R 10 , X, n, p and m are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicament for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder are also disclosed. The invention further discloses pharmaceutical compositions and combinations comprising the compounds.
摘要翻译：提供式（I）化合物或其盐，其中R 1，R 2，R 3，R 4， R 5，R 5，R 6，R 7，R 9，R 10， SUP>，X，n，p和m如说明书中所定义。还公开了化合物作为药物的用途，以及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的制备。本发明还公开了包含该化合物的药物组合物和组合。

42. 发明申请

WO2007080159A3 PYRIDINE-, ISOXAZOLE, THIOPHENECARBOXAMIDE COMPOUNDS HAVING ACTIVITY AT THE GLYCINE TRANSPORTER GLYT1 AND USES THEREOF 审中-公开
标题翻译：吡咯烷，异噻唑，在GLYCINE TRANSPORTER GLYT1中具有活性的硫代酰胺化合物及其用途
公开(公告)号：WO2007080159A3
公开(公告)日：2008-01-17
申请号：PCT/EP2007050157
申请日：2007-01-08
申请人： GLAXO GROUP LTD , BRANCH CLIVE LESLIE , MARSHALL HOWARD , MCCRITCHIE JACKIE , PORTER RODERICK ALAN , SPADA SIMONE
发明人： BRANCH CLIVE LESLIE , MARSHALL HOWARD , MCCRITCHIE JACKIE , PORTER RODERICK ALAN , SPADA SIMONE
IPC分类号： C07D213/62 , C07D261/08 , C07D333/06
CPC分类号： C07D333/38 , C07D213/70 , C07D261/18
摘要： The present invention relates to compounds of formula (I), 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. Formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are as defined in the description.
摘要翻译：本发明涉及式（I）化合物，其盐或溶剂化物，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。式（I）其中R 1，R 2，R 3，R 4，R 4， 5，R 6和n如说明书中所定义。

43. 发明申请

WO2007147838A1 RADIOLABELLED LIGAND FOR THE GLYCINE 1 TRANSPORTER 审中-公开
标题翻译：甘油1号运输车无辐射配对
公开(公告)号：WO2007147838A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/056117
申请日：2007-06-20
申请人： GLAXO GROUP LIMITED , GENTILE, Gabriella , HERDON, Hugh, Jonathan , PASSCHIER, Johannes , PORTER, Roderick, Alan
发明人： GENTILE, Gabriella , HERDON, Hugh, Jonathan , PASSCHIER, Johannes , PORTER, Roderick, Alan
IPC分类号： C07B59/00 , A61K51/00
CPC分类号： C07B59/001
摘要： Compounds of formula (I) and salts and solvates thereof, which are radiolabeled ligands for the glycine 1 transporter, are provided: wherein R 1 is a radiolabeled group incorporating or consisting of a radionuclide selected from 3 H, 11 C, 14 C, 13 N, 15 O, 76 Br, 18 F, 123 I, 125 I, 131 I, 75 Br, 76 Br, 77 Br and 82 Br. Use of the compounds for the labelling and diagnostic imaging of the glycine 1 transporter functionality is disclosed.
摘要翻译：提供了作为甘氨酸1转运蛋白的放射性标记的配体的式（I）化合物及其盐和溶剂化物：其中R 1是放射性标记的基团，其包含或由选自以下的放射性核素组成： 3 H，11 C，14 C，13 N，15 O，0 S， 76 Br，18 F，123 I，125 I，131 I，SUP， 75 Br，76 Br，76 Br和82 Br。公开了将化合物用于甘氨酸1转运蛋白功能的标记和诊断成像的用途。

44. 发明申请

WO2007014762A2 GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译： GLYT1转运蛋白抑制剂及其用于治疗神经和神经过敏性疾病的用途
公开(公告)号：WO2007014762A2
公开(公告)日：2007-02-08
申请号：PCT/EP2006007632
申请日：2006-07-31
申请人： GLAXO GROUP LTD , DEAN ANTHONY WILLIAM , PORTER RODERICK ALAN
发明人： DEAN ANTHONY WILLIAM , PORTER RODERICK ALAN
CPC分类号： C07D235/02
摘要： The invention provides a compound of formula (I) or a solvate thereof: (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and n 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：本发明提供了式（I）化合物或其溶剂化物：（I）其中R 1，R 2，R 3，R 3，R 3， R 5，R 6，n和n如说明书中所定义，以及这些化合物的用途。这些化合物抑制GlyT1转运蛋白，可用于治疗某些神经和神经精神疾病，包括精神分裂症。

45. 发明申请

WO2006067430A1 2-AMINO-1-PHENYLETHYLCARBOXAMIDE DERIVATIVES 审中-公开
标题翻译： 2-氨基-1-苯基乙酰胺衍生物
公开(公告)号：WO2006067430A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004960
申请日：2005-12-21
申请人： GLAXO GROUP LIMITED , BOZZOLI, Andrea , BRANCH, Clive Leslie , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , PORTER, Roderick, Alan , SPADA, Simone
发明人： BOZZOLI, Andrea , BRANCH, Clive Leslie , MACRITCHIE, Jacqueline, Anne , MARSHALL, Howard, Robert , PORTER, Roderick, Alan , SPADA, Simone
IPC分类号： C07D215/48 , C07C233/80 , A61K31/166 , A61K31/47 , C07D215/50 , A61P25/00
CPC分类号： C07C255/57 , C07C233/78 , C07C235/66 , C07C237/48 , C07C2601/08 , C07C2602/08 , C07D215/50 , C07D295/135 , C07D405/12
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. Formula (I) wherein R 1 is a group selected from: Formulas (A), (B), (C)
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。式（I）其中R 1是选自：式（A），（B），（C）

46. 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。

47. 发明申请

WO2006050991A1 COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：在NK3受体中具有活性的化合物及其在医学中的用途
公开(公告)号：WO2006050991A1
公开(公告)日：2006-05-18
申请号：PCT/EP2005/012207
申请日：2005-11-10
申请人： SMITHKLINE BEECHAM CORPORATION , BRADLEY, Daniel Marcus , PORTER, Roderick, Alan , SMITH, Paul William , STEAD, Rachel Elizabeth Anne , VONG, Antonio, Kuok, Keong
发明人： BRADLEY, Daniel Marcus , PORTER, Roderick, Alan , SMITH, Paul William , STEAD, Rachel Elizabeth Anne , VONG, Antonio, Kuok, Keong
IPC分类号： C07D215/52 , A61K31/47 , A61P25/18 , A61P25/24
CPC分类号： C07D409/04 , C07D215/52
摘要： The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R 1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R 2 is C 1-6 alkyl or C 3-6 cycloalkyl; n is 1 or 2; R 3 is hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl; X is -(C=O)- or -SO 2 -; R 4 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 haloalkoxy, amino, monoC 1-6 alkylamino or diC 1-6 alkylamino, or R 4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy or C 1-6 haloalkoxy; R 5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK 3 receptor, compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明还涉及式（I）化合物，其药学上可接受的盐，溶剂合物或前药：其中R 1是苯基或环己基，其任一个任选被1,2或3个卤素原子，其原子可以相同或不同; R 2是C 1-6烷基或C 3-6环烷基; n为1或2; R 3是氢，C 1-6烷基或C 3-6环烷基; X是 - （C = O） - 或-SO 2 - 。 R 4是C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基，C C 1-6烷氧基C 1-6烷基，C 1-6卤代烷氧基，氨基，一C 1-6烷基氨基或二C 1-6烷基氨基或R 4是杂环基或碳环基，其中任一个可以任选被一个或多个卤素C 1-6独立地取代， C 1-6烷基，C 1-6卤代烷基，C 1-6烷氧基或C 1-6卤代烷氧基; R 5是苯基或噻吩基，其任一个任选被1,2或3个卤素原子取代; y为0,1或2; 其中当y为1或2时，Y为卤素原子，当y为2时，卤素原子可以相同或不同。还公开了这些化合物在治疗由活化NK 3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。

48. 发明申请

WO2005058885A3 PIPERIDINE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER INHIBITORS 审中-公开
公开(公告)号：WO2005058885A3
公开(公告)日：2005-06-30
申请号：PCT/EP2004/013222
申请日：2004-11-18
申请人： GLAXO GROUP LIMITED , BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
发明人： BRADLEY, Daniel, Marcus , BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D211/26
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: (I) wherein R 1 to R 8 , X and Ar 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.

49. 发明申请

WO2005058885A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2005058885A2
公开(公告)日：2005-06-30
申请号：PCT/EP2004013222
申请日：2004-11-18
申请人： GLAXO GROUP LTD , BRADLEY DANIEL MARCUS , BRANCH CLIVE LESLIE , MARSHALL HOWARD , NASH DAVID JOHN , PORTER RODERICK ALAN
发明人： BRADLEY DANIEL MARCUS , BRANCH CLIVE LESLIE , MARSHALL HOWARD , NASH DAVID JOHN , PORTER RODERICK ALAN
IPC分类号： C07D211/26 , C07D401/06 , C07D405/12 , C07D417/06 , C07D413/00
CPC分类号： C07D405/12 , C07D211/26 , C07D401/06 , C07D417/06
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: (I) wherein R to R , X and Ar 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至R 8，X和Ar如说明书中所定义的（I），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。

50. 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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