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1. 发明申请

WO2008119720A8 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
公开(公告)号：WO2008119720A8
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053600
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , WALKER, Graham , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , WALKER, Graham , WYMAN, Paul, Adrian
IPC分类号： C07D401/04 , A61K31/454 , A61P25/00
摘要： Compounds of formula I or a salt thereof are provided wherein R 4 , R 5 , R 6 , Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.

2. 发明申请

WO2009037296A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体具有活性的化合物及其在医学中的用途
公开(公告)号：WO2009037296A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062403
申请日：2008-09-18
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
IPC分类号： A61K31/423 , C07D401/04 , C07D413/04 , C07D498/04 , A61P25/28
CPC分类号： C07D413/04
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R 4 , R 5 , R 6 , Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6， Q，A，Y和R如说明书中所定义。公开了这些化合物作为药物的用途以及在制造用于治疗精神障碍，认知障碍和阿尔茨海默病的药物中的用途。本发明还公开了包含这些化合物的药物组合物。

3. 发明申请

WO2009037293A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的化合物及其在医学中的用途
公开(公告)号：WO2009037293A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062398
申请日：2008-09-18
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , WYMAN, Paul, Adrian
IPC分类号： A61K31/423 , C07D413/14 , A61P25/28
CPC分类号： C07D413/14
摘要： Compounds of formula (I) and salts thereof are provided: formula (I) wherein R 4 , R 5 , R 6 , Q, A, and Y are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物及其盐：式（I）其中R 4，R 5，R 6，Q，A和Y如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

4. 发明申请

WO2007107566A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：WO2007107566A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052639
申请日：2007-03-20
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , LOUCHART, Yann , WALKER, Graham , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , LOUCHART, Yann , WALKER, Graham , WYMAN, Paul, Adrian
IPC分类号： A61K31/4184 , C07D235/26 , A61P25/18
CPC分类号： C07D235/26
摘要： Compounds of Formula (I) and salts and solvates are provided; wherein R, R5, R6 and Q are defined as in the claims. Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
摘要翻译：提供式（I）化合物和盐和溶剂合物; 其中R，R 5，R 6和Q如权利要求中所定义。还公开了化合物用于治疗的用途，例如治疗精神病和认知障碍。

5. 发明申请

WO2003068236A1 PIPERIDINE AND PIPERAZINE DERIVATIVES POSSESSING AFFINITY AT 5HT-1 TYPE RECEPTORS 审中-公开
标题翻译： 5HT-1型受体的磷酸和哌嗪衍生物
公开(公告)号：WO2003068236A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001710
申请日：2003-02-17
申请人： GLAXO GROUP LIMITED , FLYNN, Sean, Thomas , SMITH, Paul, W , THEWLIS, Kevin, Michael , WARD, Simon, E , WYMAN, Paul, Adrian
发明人： FLYNN, Sean, Thomas , SMITH, Paul, W , THEWLIS, Kevin, Michael , WARD, Simon, E , WYMAN, Paul, Adrian
IPC分类号： A61K31/495
CPC分类号： C07D401/12 , C07D215/20 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:wherein A is optionally substituted phenyl, indolyl, quinolinyl, quinazolinyl, indazolyl or isoquinolinyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH 2 or oxygen and is a single bond; or X is nitrogen, Y is CH 2 and is a single bond; R1 is halogen, cyano, nitro, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, C 3-7 heterocyclylC 1-6 alkyl, C 3-7 heterocyclyl C 1-6 alkoxy; a is 0, 1, 2, 3 or 4; R2 is either: halogen, -CN, an optionally substituted C 3-7 cycloalkyl, an optionally substituted aryl or an optionally substituted C-linked 3-7 membered heterocyclic group; or a group -(Z)b-B wherein: (i) Z is oxygen, CH 2 , C=O, SO 2 or C=N-OR3 wherein R3 is hydrogen or C 1-6 alkyl; b is 1, 2, or 3; and B is hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkanoyl, fluoroC 1-6 alkanoyl, C 1-6 alkylsulfonyl, fluoroC¿ 1-6 alkylsulfonyl, carbamoyl or C 1-6 alkylcarbamoyl, or R4 and R5, together with the nitrogen atom to which they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group; or (ii) Z is oxygen, CH or CH 2 , b is 1, and B forms the rest of an aryl or a C 3-7 heterocyclic group fused to the phenyl ring; excluding 1-[2-[2-(phenylmethyl)phenoxy]ethyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine and pharmaceutically acceptable salts thereof, and N-[4-[2-[4-[(3,4-dimethoxyphenyl)methyl]-1-piperazinyl]ethoxy]phenyl]-ethanesulfonamide and pharmaceutically acceptable salts thereof. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：其中A是任选取代的苯基，吲哚基，喹啉基，喹唑啉基，吲唑基或异喹啉基; X是碳，Y是CH并且是双键; 或X是CH，Y是CH 2或氧并且是单键; 或X为氮，Y为CH 2且为单键; R 1是卤素，氰基，硝基，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基，C 3-7杂环基C 1-6烷基，C 3-7杂环基C 1-6烷氧基; a是0，1，2，3或4; R 2是：卤素，-CN，任选取代的C 3-7环烷基，任选取代的芳基或任选取代的C-连接的3-7元杂环基; 或（Z）b-B基团，其中：（i）Z是氧，CH 2，C = O，SO 2或C = N-OR 3，其中R 3是氢或C 1-6烷基; b为1,2或3; 并且B是氢，C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或NR 4 R 5，其中R 4和R 5独立地是氢，C 1-6烷基，C 3-7环烷基，C 1-6烷酰基，氟C 1-6烷酰基，C 1 -6烷基磺酰基，氟代C 1-6烷基磺酰基，氨基甲酰基或C 1-6烷基氨基甲酰基，或者R 4和R 5与它们所连接的氮原子一起形成任选取代的3至7元杂环基的一部分; 或（ii）Z是氧，CH或CH 2，b是1，B形成与苯环稠合的芳基或C 3-7杂环基的其余部分; 不包括1- [2- [2-（苯基甲基）苯氧基]乙基] -4 - [（2,3,4-三甲氧基苯基）甲基] - 哌嗪及其药学上可接受的盐，以及N- [4- [2- [4 - [（3,4-二甲氧基苯基）甲基] -1-哌嗪基]乙氧基]苯基] - 乙磺酰胺及其药学上可接受的盐。还公开了制备化合物的方法和化合物在治疗中的用途，特别是CNS障碍如抑郁和焦虑。

6. 发明申请

WO2009037294A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的化合物及其在医学中的用途
公开(公告)号：WO2009037294A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062400
申请日：2008-09-18
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JOHNSON, Dale, James , STEVENSON, Graeme, Irvine , WYMAN, Paul, Adrian
IPC分类号： A61K31/423 , C07D401/04 , C07D413/04 , C07D498/04 , A61P25/28
CPC分类号： C07D498/04 , C07D209/34 , C07D215/227
摘要： Compounds of formula (I) or a salt thereof are provided: wherein R 4 , R 5 , R 6 , Q, A, Y and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders, cognitive impairments and Alzheimer's Disease are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：其中R 4，R 5，R 6，Q，A，Y和R如说明书中所定义。公开了化合物作为药物的用途和用于治疗精神病，认知障碍和阿尔茨海默氏病的药物的制备。本发明还公开了包含该化合物的药物组合物。

7. 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。

8. 发明申请

WO2008119719A1 1- (1-CYCLOHEXYL-4-PIPERIDINYL) -1, 3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE M1 RECEPTOR AND THEIR USE IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的1-（1-环辛基-4-哌啶基）-1,3-二氢-2H-苯并咪唑-2-酮衍生物及其在医药中的用途
公开(公告)号：WO2008119719A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053598
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , WYMAN, Paul, Adrian
IPC分类号： C07D401/04 , A61K31/454 , A61P25/00
CPC分类号： C07D401/04 , C07D401/14
摘要： Compounds of formula (I) or a salt thereof are provided, wherein R 4 , R 5 , R 6 , Q, R 1 and R 2 are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐，其中R 4，R 5，R 6，Q，R 5， 1＆lt;和＆lt; 2＆gt; 2＆gt;如说明书中所定义。公开了化合物作为药物和用于制备治疗精神病和认知障碍的药物的用途。本发明还公开了包含该化合物的药物组合物。

9. 发明申请

WO2008119718A1 COMPOUNDS WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体和其在医学中的用途具有活性的化合物
公开(公告)号：WO2008119718A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053597
申请日：2008-03-27
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , WALKER, Graham , WYMAN, Paul, Adrian , YANG, Zheng
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , WALKER, Graham , WYMAN, Paul, Adrian , YANG, Zheng
IPC分类号： C07D235/26 , A61K31/4184 , A61P25/18 , C07D405/14
CPC分类号： C07D235/26 , C07D405/04 , C07D405/12 , C07D405/14
摘要： Compounds of formula (I) or a salt thereof are provided: (I) wherein R 4 , R 5 , R 6 , Q and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
摘要翻译：提供式（I）化合物或其盐：（I）其中R 4，R 5，R 6，Q和R 如说明书中所定义。公开了化合物用作药物和用于制备治疗精神病和认知障碍的药物的用途。本发明还公开了包含该化合物的药物组合物。

10. 发明申请

WO2007107567A1 BENZIMIDAZOLES WHICH HAVE ACTIVITY AT M1 RECEPTOR AND THEIR USES IN MEDICINE 审中-公开
标题翻译：在M1受体上具有活性的BENZIMIDAZOLES及其在医学中的用途
公开(公告)号：WO2007107567A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052640
申请日：2007-03-20
申请人： GLAXO GROUP LIMITED , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , LOUCHART, Yann , WALKER, Graham , WYMAN, Paul, Adrian
发明人： COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , LOUCHART, Yann , WALKER, Graham , WYMAN, Paul, Adrian
IPC分类号： A61K31/4184 , C07D235/26 , A61P25/18
CPC分类号： C07D235/26
摘要： Compounds of formula (I), salts and solvates are provided, wherein Q, R, R 4 - R 6 are as def ined in the Claims. Uses of the Compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.
摘要翻译：提供了式（I）化合物，盐和溶剂合物，其中Q，R，R 4，R 6和R 6如权利要求中所定义。还公开了化合物用于治疗的用途，例如治疗精神病和认知障碍。

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