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1. 发明申请

WO2011012622A1 BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF GLYTL MEDIATED DISORDERS 审中-公开
标题翻译：用于治疗GLYTL介导的疾病的苯唑西汀衍生物
公开(公告)号：WO2011012622A1
公开(公告)日：2011-02-03
申请号：PCT/EP2010/060886
申请日：2010-07-27
申请人： GLAXO GROUP LIMITED , BLUNT, Richard , EATHERTON, Andrew John , GARZYA, Vincenzo , HEALY, Mark Patrick , MYATT, James , PORTER, Roderick Alan
发明人： BLUNT, Richard , EATHERTON, Andrew John , GARZYA, Vincenzo , HEALY, Mark Patrick , MYATT, James , PORTER, Roderick Alan
IPC分类号： C07D413/06 , C07D419/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04 , A61K31/5377 , A61P25/18
CPC分类号： C07D413/06 , C07D419/06 , C07D471/04 , C07D487/04 , C07D493/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to benzoxazinone derivatives, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in treating disorders mediated by GlyT1, including neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder.
摘要翻译：本发明涉及苯并恶嗪酮衍生物，其制备方法，药物组合物和含有它们的药物及其用于治疗由GlyT1介导的疾病，包括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。

2. 发明申请

WO2009034061A1 SPIRO-CONDENSED IMIDAZOLONE DERIVATIVES INHIBITING THE GLYCINE TRANSPORTER 审中-公开
标题翻译：螺旋状咪唑啉酮衍生物抑制糖蛋白转运蛋白
公开(公告)号：WO2009034061A1
公开(公告)日：2009-03-19
申请号：PCT/EP2008/061889
申请日：2008-09-09
申请人： GLAXO GROUP LIMITED , BLUNT, Richard , COOPER, David, Gwyn , PORTER, Roderick, Alan , WYMAN, Paul, Adrian
发明人： BLUNT, Richard , COOPER, David, Gwyn , PORTER, Roderick, Alan , WYMAN, Paul, Adrian
IPC分类号： C07D235/02 , C07D401/10 , C07D403/10 , C07D491/04 , A61K31/4184 , A61K31/4188 , A61K31/44 , A61P25/00
CPC分类号： C07D235/02 , C07D401/10 , C07D403/10 , C07D491/04
摘要： Compounds of formula (I) and salts thereof are provided: formula (I), wherein the groups are as defined in the specification. 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 comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：提供式（I）化合物及其盐：式（I），其中基团如说明书中所定义。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。本发明还包括制备这些化合物及其药物制剂的方法。

3. 发明申请

WO2007113309A3 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：WO2007113309A3
公开(公告)日：2008-09-12
申请号：PCT/EP2007053275
申请日：2007-04-03
申请人： GLAXO GROUP LTD , COULTON STEVEN , GILPIN MARTIN , PORTER RODERICK ALAN
发明人： COULTON STEVEN , GILPIN MARTIN , PORTER RODERICK ALAN
IPC分类号： C07C211/27 , A61K31/166 , A61K31/40 , A61K31/445 , A61P25/28 , C07C233/78 , C07D213/40 , C07D295/13
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。

4. 发明申请

WO2008092873A1 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：WO2008092873A1
公开(公告)日：2008-08-07
申请号：PCT/EP2008/051078
申请日：2008-01-30
申请人： GLAXO GROUP LIMITED , UNIVERSITY OF NOTTINGHAM , AHMAD, Nadia, Mamoona , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun Quai , PORTER, Roderick, Alan
发明人： AHMAD, Nadia, Mamoona , JAXA-CHAMIEC, Albert, Andrzej , LAI, Justine, Yeun Quai , PORTER, Roderick, Alan
IPC分类号： C07D209/54 , A61K31/403 , A61P25/00 , A61P25/18 , A61P25/28
CPC分类号： C07D209/54
摘要： Compounds of formula (I) or a salt thereof are provided:(I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 21 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：（I）其中R 1，R 2，R 3，R SUP R 4，R 5，R 6，R 7，R 8，R SUP， > 21＆gt;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。

5. 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。

6. 发明申请

WO2007116061A1 1-(2-ARYL-2-OXOETHYL)-3-PHENYL-1, 4-DIAZASPIRO [4.5]DEC-3-EN-2-ONE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER INHIBITORS 审中-公开
标题翻译： 1-（2-亚甲基-2-氧代乙基）-3-苯基-1,4-二氮杂萘[4.5] DEC-3-EN-2-一种衍生物及其作为甘氨酸运输抑制剂的用途
公开(公告)号：WO2007116061A1
公开(公告)日：2007-10-18
申请号：PCT/EP2007/053468
申请日：2007-04-10
申请人： GLAXO GROUP LIMITED , BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
发明人： BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D235/02 , C07D401/10 , C07D405/06 , A61K31/4184
CPC分类号： C07D235/02 , C07D401/10 , C07D405/06
摘要： Novel acetophenone compounds of formula (I), compositions containing (I), processes for the preparation of (I), and use of (I) as inhibitors of the glycine transporter, are provided. Definitions of Ar, R 5 , R 6 , R 7 , R 8 and n are provided in the specification.
摘要翻译：提供式（I）的新型苯乙酮化合物，含有（I）的组合物，（I）的制备方法和（I）用作甘氨酸转运蛋白的抑制剂。在本说明书中提供了Ar，R 5，R 6，R 7，R 8和n的定义。

7. 发明申请

WO2007104775A1 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：WO2007104775A1
公开(公告)日：2007-09-20
申请号：PCT/EP2007/052414
申请日：2007-03-14
申请人： GLAXO GROUP LIMITED , COULTON, Steven , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
发明人： COULTON, Steven , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D235/02 , A61K31/41 , A61P25/18
CPC分类号： C07D235/02
摘要： Compounds of formula (I) and salts and solvates thereof are provided: wherein R 1 to R 8 and n are 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 comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：提供式（I）化合物及其盐和溶剂化物：其中R 1至R 8和n在说明书中定义。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。本发明还包括制备这些化合物及其药物制剂的方法。

8. 发明申请

WO2005103038A1 N-[6-(4-MORPHOLINYL)-3-PYRIDINYL]-2-(TETRAHYDRO-2H-PYRAN-4-YL)-N-[(1-{[PHENYL]METHYL}-4-PIPERIDINYL)METHYL] ACETAMIDE DERIVATIVES AND RELATED COMPOUNDS AS GLYT1 TRANSPORT INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISORDERS SUCH AS SCHIZOPHRENIA 审中-公开
标题翻译： N- [6-（4-吗啉基）-3-吡啶基] -2-（四氢-2H-吡喃-4-基）-N - [（1 - {[苯基]甲基} -4-哌啶子基）甲基] 作为GLYT1运输抑制剂治疗神经病变的衍生物和相关化合物，如SCHIZOPHRENIA
公开(公告)号：WO2005103038A1
公开(公告)日：2005-11-03
申请号：PCT/GB2005/001448
申请日：2005-04-15
申请人： GLAXO GROUP LIMITED , NASH, David, John , PORTER, Roderick, Alan
发明人： NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D405/14
CPC分类号： C07D405/14 , C07D401/12
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 1 is selected from the group consisting of optionally substituted C 1-8 alkyl, optionally substituted C 3-8 cycloalkyl, optionally substituted C 3-8 heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, arylC 1-8 alkyl (wherein both aryl and C 1-8 alkyl are optionally substituted), C 3-8 heterocyclylC 1-8 alkyl (wherein the C 1-8 alkyl is optionally substituted) and heteroarylC 1-8 alkyl (wherein both heteroaryl and C 1-8 alkyl are optionally substituted); R 2 and R 3 , together with the carbon atom to which they are attached, form optionally subtituted C 3-4 cycloalkyl, or R 2 and R 3 are independently hydrogen or C 1-8 alkyl; R 4 and R 5 are both hydrogen, or R 4 and R 5 together form a C 1-4 alkylene bridge across the piperidine ring; Het is an optionally substituted 5- or 6-membered monocyclic heteroaryl group; R 6 and R 7 are independently selected from the group consisting of hydrogen, halogen and C 1-4 alkyl, or R 6 and R 7 together form a C 3-4 cycloalkyl; Ar is an optionally substituted aryl or an optionally substituted heteroaryl; and n is 0, 1, 2 or 3. 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选自任选取代的C 1-8烷基，任选取代的C 3-8环烷基，任选取代的C 3-8杂环基，任选取代的芳基，任选取代的杂芳基，芳基C 1-8烷基（其中芳基和C 1-8烷基任选被取代），C 3-8杂环C 1-6烷基（其中C 1-8烷基任选被取代）和杂芳基C 1-8烷基（其中杂芳基和C 1-8烷基均为任选取代）; R 2和R 3与它们所连接的碳原子一起形成任选取代的C3-4环烷基，或者R 2和R 3独立地是氢或C 1-8烷基; R 4和R 5都是氢，或者R 4和R 5一起形成穿过哌啶环的C 1-4亚烷基桥; Het是任选取代的5或6元单环杂芳基; R 6和R 7独立地选自氢，卤素和C 1-4烷基，或者R 6和R 7一起形成C 3-4环烷基; Ar是任选取代的芳基或任选取代的杂芳基; 并且n为0,1,2或3.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。

9. 发明申请

WO2005058882A1 COMPOUNDS HAVING MORPHOLINYL AND PIPERIDINYL GROUPS FOR USE AS GLYT1 AND GLYT2 INHIBITORS 审中-公开
标题翻译：具有作为GLYT1和GLYT2抑制剂的MORPHOLINYL和PIPERIDINYL组的化合物
公开(公告)号：WO2005058882A1
公开(公告)日：2005-06-30
申请号：PCT/EP2004/014469
申请日：2004-12-16
申请人： GLAXO GROUP LIMITED , BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
发明人： BRANCH, Clive, Leslie , MARSHALL, Howard , NASH, David, John , PORTER, Roderick, Alan
IPC分类号： C07D405/14
CPC分类号： C07D401/12 , C07D405/14
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof, wherein R 1 , R 3 and R 4 , Het, 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，R 3和R 4，Het，X和Ar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

WO2004112787A1 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：WO2004112787A1
公开(公告)日：2004-12-29
申请号：PCT/EP2004/006596
申请日：2004-06-17
申请人： GLAXO GROUP LIMITED , COULTON, Steven , PORTER, Roderick, Alan
发明人： COULTON, Steven , PORTER, Roderick, Alan
IPC分类号： A61K31/44
CPC分类号： C07D295/13
摘要： Compounds of formula (I), salts, solvates and physiologically functional derivatives thereof are disclosed. Methods of preparation and uses thereof in medicine, for the treatment of a disorder mediated by GlyT1, such as for example schizophrenia, are also disclosed.
摘要翻译：公开了式（I）化合物，其盐，溶剂化物和生理功能衍生物。还公开了用于治疗由GlyT1介导的病症（例如精神分裂症）在医学中的制备方法及其用途。

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