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1. 发明申请

WO2011151361A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2011151361A1
公开(公告)日：2011-12-08
申请号：PCT/EP2011/059011
申请日：2011-06-01
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , CREMONESI, Susanna , GARZYA, Vincenzo , MICHELI, Fabrizio , RUPCIC, Renata , SABBATINI, Fabio Maria
发明人： BERTANI, Barbara , CREMONESI, Susanna , GARZYA, Vincenzo , MICHELI, Fabrizio , RUPCIC, Renata , SABBATINI, Fabio Maria
IPC分类号： C07D513/04 , A61K31/542 , A61P25/00
CPC分类号： C07D513/04
摘要： The invention relates to tricyclic derivatives, and their use in treating diseases and conditions mediated by antagonism of the mGluR 5 receptor, in particular substance related disorders. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
摘要翻译：本发明涉及三环衍生物及其在治疗由mGluR5受体的拮抗作用介导的疾病和病症中的用途，特别是与物质有关的疾病。此外，本发明涉及含有衍生物的组合物及其制备方法。

2. 发明申请

WO2010146025A1 TRICYCLIC AZABICYCLO [4.1.0] HEPTANE DERIVATIVES AS INHIBITORS OF SEROTONIN, DOPAMINE AND NOREPINEPHRINE RE-UPTAKE 审中-公开
标题翻译：三联唑啉酮[4.1.0]作为丝氨酸，多巴胺和肾上腺素再摄取抑制剂的HEPTANE衍生物
公开(公告)号：WO2010146025A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058331
申请日：2010-06-15
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , ROSCIC, Maja , ZONZINI, Laura
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , ROSCIC, Maja , ZONZINI, Laura
IPC分类号： C07D471/10 , C07D498/10 , A61K31/553 , A61K31/439 , A61P25/30 , A61P25/24 , A61P25/16 , A61P25/22 , A61P25/28
CPC分类号： C07D471/10 , C07D498/10
摘要： The invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及式（I）化合物，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE）再吸收抑制剂。

3. 发明申请

WO2008037681A1 5-{2-[4-(2-METHYL-5-QUINOLINYL)-L-PIPERIDINYL] ETHYL} QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIREMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
标题翻译：作为5HT1A受体调节剂的5- {2- [4-（2-甲基-5-喹啉基）-L-哌啶子基]乙基}喹啉酮衍生物，用于治疗性功能障碍，认知障碍，精神病，焦虑，抑郁等。
公开(公告)号：WO2008037681A1
公开(公告)日：2008-04-03
申请号：PCT/EP2007/060082
申请日：2007-09-24
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
发明人： BERTANI, Barbara , BROMIDGE, Steven, Mark , GIANOTTI, Massimo , PASQUARELLO, Alessandra , ZUCCHELLI, Valeria
IPC分类号： C07D401/12 , C07D401/14 , C07D487/08 , A61K31/496
CPC分类号： C07D401/12 , C07D401/14 , C07D487/08
摘要： The invention provides compounds of formula (I) wherein R 1 is C 1-6 alkyl, halo or haloC 1-6 alkyl; R 2 is hydrogen or C 1-6 alkyl; ===== is a single or double bond; each R 3 and R 4 , which may be the same or different, are hydrogen, C 1-6 alkyl or haloC 1-6 alkyl; wherein i) when ===== is a double bond p and q are 1, and ii) when ===== is a single bond, p and q are 2, and one of R 3 and one of R 4 together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R 5 , which may be the same or different, is C 1-6 alkyl or halo; or two R 5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R 6 which may be the same or different, is C 1-6 alkyl or halo; and m is 0, 1, 2 or 3.
摘要翻译：本发明提供了式（I）的化合物，其中R 1是C 1-6烷基，卤素或卤代C 1-6 烷基; R 2是氢或C 1-6烷基; ^{===== 是单键或双键; 每个R 3和R 4可以相同或不同，为氢，C 1-6烷基或卤代C 1 -6 烷基; 其中i）当^{===== 是双键时p和q是1，并且ii）当^{===== 是单键时，p和q 是2，并且R 3和R 4中的一个与它们的相互连接原子一起形成环丙烷环，其可以被一个或两个卤素或甲基取代，哪些组可能是相同的或不同的; X是CH或N; 当存在时，每个R 5可以相同或不同，为C 1-6烷基或卤代; 或者两个R 5基团可以连接形成桥，该桥包含一个或两个原子; n是0,1,2或3; 当存在时，每个R 6可以相同或不同，为C 1-6烷基或卤代; 而m是0,1,2或3。}}}

4. 发明申请

WO2007113258A1 AZABICYCLO [3. 1. O] HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXANE衍生物
公开(公告)号：WO2007113258A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053115
申请日：2007-03-30
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , FABRIZIO, Micheli , PASQUARELLO, Alessandra , TERRENI, Silvia
发明人： BERTANI, Barbara , FABRIZIO, Micheli , PASQUARELLO, Alessandra , TERRENI, Silvia
IPC分类号： C07D401/06 , C07D401/14 , A61K31/4439 , A61P25/00
CPC分类号： C07D401/06 , C07D401/14
摘要： The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof where the substitvents are as defined in claim 1 processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中方案如权利要求1所定义，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为多巴胺D3受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫性疾病或早泄。

5. 发明申请

WO1997012870A1 TETRAHYDROQUINOLINES AS NMDA ANTAGONISTS 审中-公开
标题翻译：四氢喹啉作为NMDA拮抗剂
公开(公告)号：WO1997012870A1
公开(公告)日：1997-04-10
申请号：PCT/EP1996004206
申请日：1996-09-26
申请人： GLAXO WELLCOME S.P.A. , Di FABIO, Romano , GIACOBBE, Simone , BERTANI, Barbara , MICHELI, Fabrizio
发明人： GLAXO WELLCOME S.P.A.
IPC分类号： C07D215/48
CPC分类号： C07D215/48
摘要： Compounds of formula (I) or a salt, or metabolically labile ester thereof, processes for the preparation thereof and their use as antagonists of excitatory amino acids.
摘要翻译：式（I）化合物或其盐或其代谢不稳定的酯的制备方法及其作为兴奋性氨基酸的拮抗剂的用途。

6. 发明申请

WO2008037681A8 5-{2-[4-(2-METHYL-5-QUINOLINYL)-L-PIPERIDINYL] ETHYL} QUINOLINONE DERIVATIVES AS 5HT1A RECEPTOR MODULATORS FOR TREATING SEXUAL DYSFUNCTION, COGNITION IMPAIREMENT, PSYCHOTIC DISORDERS, ANXIETY, DEPRESSION, ETC. 审中-公开
标题翻译： 5- {2- [4-（2-甲基-5-喹啉啉）-L-哌啶基]乙基}喹啉酮衍生物作为5HT1A受体调节剂，用于治疗性功能障碍，认知障碍，心理障碍，异常，呕吐等。
公开(公告)号：WO2008037681A8
公开(公告)日：2008-05-15
申请号：PCT/EP2007060082
申请日：2007-09-24
申请人： GLAXO GROUP LTD , BERTANI BARBARA , BROMIDGE STEVEN MARK , GIANOTTI MASSIMO , PASQUARELLO ALESSANDRA , ZUCCHELLI VALERIA
发明人： BERTANI BARBARA , BROMIDGE STEVEN MARK , GIANOTTI MASSIMO , PASQUARELLO ALESSANDRA , ZUCCHELLI VALERIA
IPC分类号： C07D401/12 , A61K31/496 , C07D401/14 , C07D487/08
CPC分类号： C07D401/12 , C07D401/14 , C07D487/08
摘要： The invention provides compounds of formula (I) wherein R 1 is C 1-6 alkyl, halo or haloC 1-6 alkyl; R 2 is hydrogen or C 1-6 alkyl; ===== is a single or double bond; each R 3 and R 4 , which may be the same or different, are hydrogen, C 1-6 alkyl or haloC 1-6 alkyl; wherein i) when ===== is a double bond p and q are 1, and ii) when ===== is a single bond, p and q are 2, and one of R 3 and one of R 4 together with their interconnecting atoms, forms a cyclopropane ring which may be substituted by one or two halo or methyl groups, which groups may be the same or different; X is CH or N; when present each R 5 , which may be the same or different, is C 1-6 alkyl or halo; or two R 5 groups may join to form a bridge, which bridge contains one or two atoms; n is 0, 1, 2 or 3; when present each R 6 which may be the same or different, is C 1-6 alkyl or halo; and m is 0, 1, 2 or 3.
摘要翻译：本发明提供式（I）化合物，其中R 1是C 1-6烷基，卤素或卤代C 1-6烷基; R 2是氢或C 1-6烷基; ^{===== 是单键或双键; 每个R 3和R 4可以相同或不同，是氢，C 1-6烷基或卤代C 1 -6 烷基; 其中i）当^{===== 是双键p且q是1时，和ii）当^{===== 是单键时，p和q 是2，R 3和R 4中的一个与它们的互连原子一起形成可被一个或两个卤素或甲基取代的环丙烷环，哪些组可以相同或不同; X是CH或N; 当存在时可以相同或不同的每个R 5为C 1-6烷基或卤素; 或两个R 5+基团可以连接形成桥，该桥包含一个或两个原子; n为0,1,2或3; 当存在时可以相同或不同的每个R 6是C 1-6烷基或卤素; m为0,1,2或3。}}}

7. 发明申请

WO2007125061A1 SPIROCOMPOUNDS USEFUL AS MODULATORS FOR DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂的螺旋体有用
公开(公告)号：WO2007125061A1
公开(公告)日：2007-11-08
申请号：PCT/EP2007/054003
申请日：2007-04-24
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TARSI, Luca , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/506 , A61P25/18
CPC分类号： C07D403/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/10
摘要： The present invention relates to compounds of formula (I) or salts thereof wherein A, X and R 4 are defined herein, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or to enhance cognition.
摘要翻译：本发明涉及式（I）化合物或其盐，其中A，X和R 4在本文中定义，其制备方法，用于这些方法的中间体，含有它们的药物组合物及其用途在治疗中，作为多巴胺D 3受体的调节剂，例如，治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症，早泄或增强认知。

8. 发明申请

WO2005014552A1 QUINOLINE AND QUINAZOLINE DERIVATIVES HAVING AFFINITY FOR 5HT1-TYPE RECEPTORS 审中-公开
标题翻译：具有5HT1型受体亲和力的喹啉和喹唑啉衍生物
公开(公告)号：WO2005014552A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008000
申请日：2004-07-15
申请人： GLAXO GROUP LIMITED , BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
发明人： BERGAUER, Markus , BERTANI, Barbara , BIAGETTI, Matteo , BROMIDGE, Steven Mark , FALCHI, Alessandro , LESLIE, Colin Philip , MERLO, Giancarlo , PIZZI, Domenica Antonia , RINALDI, Marilisa , STASI, Luigi Piero , TIBASCO, Jessica , VONG, Antonio, Kuok, Keong , WARD, Simon, Edward
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C04B35/632
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are provided: wherein R 1 , m, X, R 2 , n, W, p, Y, Z, R 3 , R 4 , R 5 and q have the meanings as defined in the description. Methods of preparation and uses thereof in therapy, particularly for CNS disorders such as depression or anxiety, are also disclosed.
摘要翻译：提供式（I）化合物及其药学上可接受的盐：其中R1，m，X，R2，n，W，p，Y，Z，R3，R4，R5和q具有如说明书中所定义的含义。还公开了其治疗方法及其在治疗中的用途，特别是CNS疾病如抑郁或焦虑症。

9. 发明申请

WO2009043884A1 AZABICYCLO [3. 1. 0] HEXYL DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZABICYCLO [3。作为DOPAMINE D3受体的调节剂的HEXYL衍生物
公开(公告)号：WO2009043884A1
公开(公告)日：2009-04-09
申请号：PCT/EP2008/063168
申请日：2008-10-01
申请人： Glaxo Group Limited , BERTANI, Barbara , CREMONESI, Susanna , FONTANA, Stefano , PASQUARELLO, Alessandra
发明人： BERTANI, Barbara , CREMONESI, Susanna , FONTANA, Stefano , PASQUARELLO, Alessandra
IPC分类号： C07D207/36 , C07D209/02 , C07D401/14 , C07D403/06 , C07D417/14 , A61K31/53 , A61P25/18
CPC分类号： C07D403/06 , C07D207/36 , C07D209/02 , C07D401/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof, wherein G is selected from a group consisting of: phenyl, a 5- or 6-membered monocyclic heteroaryl group, or a 8- to 11-membered heteroaryl bicyclic group; p is an integer ranging from 0 to 5; R 1 is halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 6 ; and when p is an integer ranging from 2 to 5, each R 1 may be the same or different; R 2 is hydrogen or C 1-4 alkyl; n is 3, 4, 5 or 6; R 6 is a moiety selected from the group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such R 6 group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl; R 4 is selected in the group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, C 3-7 cycloalkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and NR'R"; or R 4 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic group is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyl, haloC 1-4 alkoxy and SF 5 ; R 7 is hydrogen or C 1-2 alkyl; R' is H, C 1-4 alkyl or C 1-4 alkanoyl; R" is defined as R'; R' and R" taken together with the interconnecting nitrogen atom may form a 5-, 6-membered saturated or unsaturated heterocyclic ring; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D 3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, or premature ejaculation.
摘要翻译：本发明涉及新的式（I）化合物或其盐，其中G选自：苯基，5-或6-元单环杂芳基或8至11元杂芳基双环组; p为0〜5的整数。 R 1是卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5; 或对应于基团R6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R2是氢或C1-4烷基; n为3,4,5或6; R6是选自以下的部分：异恶唑基，-CH 2 -N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基，这些R 6基团任选地被一个或多个选自以下的两个取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，C 1-4烷酰基; R4选自：氢，卤素，羟基，氰基，C 1-4烷基，C 3-7环烷基，卤代C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和NR'R“;或R 4是苯基，5-14元杂环基;任何这样的苯基或杂环基任选被1,2或3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，卤代C 1-4烷基 C 1-4烷氧基，C 1-4烷酰基，卤代C 1-4烷氧基和SF 5; R 7是氢或C 1-2烷基; R'是H，C 1-4烷基或C 1-4烷酰基; R“定义为R' R'和R“与互连氮原子一起可以形成5-，6-元饱和或不饱和杂环;其制备方法，在这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为调节剂多巴胺D3受体，例如治疗药物依赖性，作为抗精神病药，治疗强迫性强迫症或早泄。

10. 发明申请

WO2009027295A1 3-AZABICYCLO (4.1.0) HEPTANE DERIVATIVES USEFUL AS NOREPINEPHRINE, SEROTONIN OR DOPAMINE REUPTAKE INHIBITORS 审中-公开
标题翻译： 3-AZABICYCLO（4.1.0）HEPTANE衍生物有效用作肾上腺素，丝氨酸或多巴胺复制抑制剂
公开(公告)号：WO2009027295A1
公开(公告)日：2009-03-05
申请号：PCT/EP2008/060913
申请日：2008-08-21
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , MICHELI, Fabrizio , TARSI, Luca
发明人： BERTANI, Barbara , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , MICHELI, Fabrizio , TARSI, Luca
IPC分类号： C07D221/04 , A61K31/435 , A61P25/00
CPC分类号： C07D221/04
摘要： The present invention relates to compounds of formula (I), processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.
摘要翻译：本发明涉及式（I）化合物，其制备方法，这些方法中使用的中间体，含有它们的药物组合物及其在治疗中的用途，作为5-羟色胺（5-HT），多巴胺（DA）和去甲肾上腺素（NE），再吸收抑制剂。

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