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11. 发明申请

WO2003099792A1 7-PHENYLSULFONYL-TETRAHYDRO-3-BENZAZEPINE DERIVATIVES AS ANTIPSYCHOTIC AGENTS 审中-公开
标题翻译：作为抗菌剂的7-苯基磺酰基四氢吡喃-3-胆碱衍生物
公开(公告)号：WO2003099792A1
公开(公告)日：2003-12-04
申请号：PCT/EP2003/005728
申请日：2003-05-28
申请人： GLAXO GROUP LIMITED , GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham
发明人： GRIBBLE, Andrew, Derrick , FORBES, Ian, Thomson , LIGHTFOOT, Andrew , PAYNE, Andrew, H , WALKER, Graham
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07D209/44 , C07D217/02 , C07D217/04
摘要： The invention provides compounds of formula (I): wherein A and B represent the groups -(CH2)m- and -(CH2)n- respectively;R1 represents hydrogen or C1-6alkyl;R2 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR5R6, -SO2NR5R6, -(CH2)pNR5R6, -(CH2)pNR5COR6, optionally substituted aryl ring, optionally substituted heteroaryl ring or optionally substituted heterocyclyl ring;R3 represents hydrogen, halogen, hydroxy, cyano, nitro, hydroxyC1-6alkyl, trifluoromethyl, trifluoromethoxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, -(CH2)pC3-6cycloalkyl, -(CH2)pOC3-6cycloalkyl, -COC1-6alkyl, -SO2C1-6alkyl, -SOC1-6alkyl, -S-C1-6alkyl, -CO2C1-6alkyl, -CO2NR7R8, -SO2NR7R8, -(CH2)pNR7R8 or -(CH2)pNR7COR8;R4 represents hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, C1-6fluoroalkoxy, trifluoromethyl, trifluoromethoxy, halogen, -OSO2CF3, -(CH2)pC3-6cycloalkyl, -(CH2)qOC1-6alkyl or -(CH2)pOC3-6cycloalkyl;R5 and R6 each independently represent hydrogen, C1-6alkyl or, together with the nitrogen or other atoms to which they are attached, form an azacycloalkyl ring or an oxo-substituted azacycloalkyl ring;R7 and R8 each independently represent hydrogen or C1-6alkyl;m and n independently represent an integer selected from 1 and 2;p independently represents an integer selected from 0, 1, 2 and 3; q independently represents an integer selected from 1, 2 and 3; or a pharmaceutically acceptable salt or solvate thereof,with the proviso that the compounds 8-hydroxy-3-methyl-7-phenylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 8-hydroxy-7-4-(hydroxyphenyl)sulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine, 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline and 7-phenylsulfonyl-1,2,3,4-tetrahydroisoquinoline hydrochloride are excluded.The compounds are useful in therapy, in particular as antipsychotic agents.
摘要翻译：本发明提供式（I）化合物：其中A和B分别代表 - （CH 2）m-和 - （CH 2）n - 基团; R 1代表氢或C 1-6烷基; R 2代表氢，卤素，羟基，氰基，硝基，羟基C 1-6烷基，三氟甲基，三氟甲氧基，C 1-6烷基，C 1-6烷氧基，C 1-6氟烷氧基， - （CH 2）p C 3-6环烷基， - （CH 2）pOC 3 6-环烷基，-COC 1-6烷基，-SO 2 C 1-6烷基，（CH2）pNR5R6， - （CH2）pNR5COR6，任选取代的芳基环，任选取代的杂芳基环或任选取代的杂环基环; R 3代表（C 1 -C 6）氢，卤素，羟基，氰基，硝基，羟基C 1-6烷基，三氟甲基，三氟甲氧基，C 1-6烷基，C 1-6烷氧基，C 1-6氟烷氧基， - （CH 2）pC 3-6环烷基， - （CH 2）pOC 3 6-环烷基，-COC 1-6烷基，-SO 2 C 1-6烷基，-SOC 1-6烷基，-S-C 1-6烷基，-CO 2 C 1-6烷基，-CO 2 NR 7 R 8，-SO 2 NR 7 R 8， - （CH 2）p NR 27 R 8或 - （CH 2）p NR 7 COR 8; R 4表示氢，羟基，C 1-6烷基，C 1-6烷氧基，C 1-6氟烷氧基，三氟甲基，三氟甲氧基，卤素，-OSO 2 CF 3， - （CH 2）p C 3-6环烷基， - （CH 2）q OC 1-6烷基或 - （CH 2）pOC 3 6-环烷基; R 5和R 6各自独立地表示氢，C 1-6烷基或与氮或它们所连接的其它原子形成氮杂环烷基环或氧代取代的氮杂环烷基环; R7和R8各自独立地表示氢或C1-6烷基; m和n独立地表示选自1和2的整数; p独立地表示选自0,1,2和3的整数; q独立地表示选自1,2和3的整数; 或其药学上可接受的盐或溶剂合物，条件是化合物8-羟基-3-甲基-7-苯基磺酰基-2,3,4,5-四氢-1H-3-苯并氮杂-8-羟基-7-4 - （羟基苯基）磺酰基-2,3,4,5-四氢-1H-3-苯并氮杂，7-苯基磺酰基-1,2,3,4-四氢异喹啉和7-苯基磺酰基-1,2,3,4-四氢异喹啉盐酸盐这些化合物可用于治疗，特别是抗精神病药。

12. 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.

13. 发明申请

WO2007036718A2 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：WO2007036718A2
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003595
申请日：2006-09-27
申请人： GLAXO GROUP LIMITED , BUDZIK, Brian , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , SHI, Dongchuan , SMITH, Paul, William , WALKER, Graham
发明人： BUDZIK, Brian , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , SHI, Dongchuan , SMITH, Paul, William , WALKER, Graham
IPC分类号： C07D401/14 , A61K31/44 , A61P25/00
CPC分类号： C07D401/14
摘要： Compounds of formula (I) and salts and solvates are provided: In a first aspect therefore, the invention provides a compound of formula (I) or a salt or solvate thereof: wherein R 5 is selected from halogen, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted with one or more fluorine atoms, and cyano; R 6 is selected from halogen, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 3-6 cycloalkyl, C 3 - 6 cycloalkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, C 1-6 alkoxy substituted with one or more fluorine atoms, and cyano; and Q is hydrogen or C 1-6 alkyl. The compounds are M 1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
摘要翻译：提供了式（I）化合物及其盐和溶剂合物：因此，第一方面，本发明提供了式（I）化合物或其盐或溶剂合物：其中R 5 选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷氧基和氰基; R 6选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C _{C 3-6环烷基，被一个或多个氟原子取代的C 3-6 - 环烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基和氰基; 并且Q是氢或C 1-6烷基。这些化合物是M 1激动剂，可用于治疗，例如治疗精神病和认知功能障碍。}

14. 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。

15. 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。

16. 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。

17. 发明申请

WO2007107565A1 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：WO2007107565A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052638
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
CPC分类号： C07D235/26
摘要： Compounds of formula (I), salts and solvates are provided: formula (I), wherein Q, R and R6 are as defined 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，盐和溶剂化物：式（I）其中Q，R和R6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。

18. 发明申请

WO2007036715A2 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：WO2007036715A2
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003590
申请日：2006-09-27
申请人： GLAXO GROUP LIMITED , BUDZIK, Brian , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , SHI, Dongchuan , SMITH, Paul, William , WALKER, Graham
发明人： BUDZIK, Brian , COOPER, David, Gwyn , FORBES, Ian, Thomson , GARZYA, Vincenzo , JIN, Jian , SHI, Dongchuan , SMITH, Paul, William , WALKER, Graham
IPC分类号： C07D235/26 , C07D405/12 , A61K31/4184 , A61P25/00
CPC分类号： C07D405/12 , C07D235/26
摘要： Compounds which have activity at M 1 receptor and their uses in medicine Compounds of formula (I) and salts and solvates are provided: wherein R 4 is fluoro, R 5 is selected from hydrogen, halogen, cyano, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 1-6 alkoxy, and C 1-6 alkoxy substituted with one or more fluorine atoms; and R 6 is selected from halogen, cyano, C 1-6 alkyl, C 1-6 alkyl substituted with one or more fluorine atoms, C 3-6 cycloalkyl, C 3-6 cycloalkyl substituted with one or more fluorine atoms, C 1-6 alkoxy and C 1-6 alkoxy substituted with one or more fluorine atoms, and Q is hydrogen or C 1-6 alkyl. The compounds are expected to be useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
摘要翻译：对M 1受体具有活性的化合物及其在药物中的用途提供式（I）化合物及其盐和溶剂合物：其中R 4

19. 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。

20. 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。

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