专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009130231A1 PYRROLO [1, 2-A] PYRAZINE DERIVATIVES AS VASOPRESSIN VIB RECEPTOR ANTAGONISTS 审中-公开
标题翻译： PYRROLO [1,2-A]吡嗪衍生物作为VASOPRESSIN VIB受体拮抗剂
公开(公告)号：WO2009130231A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054777
申请日：2009-04-22
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
发明人： DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
IPC分类号： C07D519/00 , C07D487/04 , A61K31/4985 , A61P25/22 , A61P25/24
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or salts thereof; wherein R is -X-[CH 2 ] n CR 4 R 5 -Y; or a group G; R 1 is H or C1 -C4 alkyl; R 2 is aryl, heteroaryl or C3-C7 cycloalkyl, which may be substituted with one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, - CN; R 3 is -CH 2 -C(=O)-NH-R 6 ; X is -CR 7 R 8 -, -O-, -NR 9 -, -S-; Y is-NR 10 R 11 R 4 is H or C1 -C4 alkyl; R 5 is H or C1 -C4 alkyl; R 6 is C1-C6 alkyl, C3-C6 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 7 is H or C1 -C4 alkyl; R 8 is H or C1 -C4 alkyl; R 9 is H or C1 -C4 alkyl; R 10 is H or C1-C4 alkyl, or together with R 11 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 12 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 11 is H or C1 -C4 alkyl; R 12 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; G is one of the groups selected from the list consisting of G1, G2, G3, G4, G5, G6, G7, G8, G9, G10, G11 and G12; R 13 is H or C1-C4 alkyl, or together with R 14 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 24 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 14 R 16 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 15 , R 17 correspond to H or C1-C4 alkyl and may assume different meanings; R 18 is H or C1-C4 alkyl, or together with R 17 forms a 4-8 saturated or unsaturated heterocycle ring which may comprise a further heteroatom selected from O, S and -NR 25 ; such heterocycle may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 19 , R 20 , R 21 , R 22 , R 23 , R 24 , R 25 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; R 26 , R 27 , R 28 , R 29 is H, C1-C6 alkyl, C3-C7 cycloalkyl; C3-C6 cycloalkyl- (C1 -C2 alkyl); which may be substituted by one or more halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; I, I' correspond to 1 or 2 and may assume different meanings; m, m', m", m"', m ιv , m v correspond to 0, 1 or 2 and may assume different meanings; n is 1, 2 or 3; q is 1, 2 or 3; p, p', p", p'" correspond to 0, 1, 2 or 3 and may assume different meanings; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as antagonists of V1b receptors, e.g. to treat depression and anxiety.
摘要翻译：本发明涉及新的式（I）化合物或其盐; 其中R是-X- [CH2] nCR4R5-Y; 或G组; R1是H或C1-C4烷基; R 2是可以被一个或多个取代基取代的芳基，杂芳基或C 3 -C 7环烷基：卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基，-CN; R3是-CH2-C（= O）-NH-R6; X为-CR 7 R 8 - ， - O - ， - NR 9 - ， - S- Y是-NR 10 R 11 R 4是H或C 1 -C 4烷基; R5是H或C1-C4烷基; R6是C1-C6烷基，C3-C6环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R7是H或C1-C4烷基; R8是H或C1-C4烷基; R 9为H或C 1 -C 4烷基; R 10是H或C 1 -C 4烷基，或与R 11一起形成4-8个饱和或不饱和杂环，其可包含选自O，S和-NR 12的另外的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R 11是H或C 1 -C 4烷基; R 12是H，C 1 -C 6烷基，C 3 -C 7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; G是从由G1，G2，G3，G4，G5，G6，G7，G8，G9，G10，G11和G12组成的列表中选择的组之一; R 13是H或C 1 -C 4烷基，或与R 14一起形成4-8个饱和或不饱和的杂环，其可以包含另外的选自O，S和-NR 24的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R14R16是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R 15，R 17对应于H或C 1 -C 4烷基，并且可以具有不同的含义; R 18是H或C 1 -C 4烷基，或与R 17一起形成4-8个饱和或不饱和杂环，其可包含选自O，S和-NR 25的另外的杂原子; 这样的杂环可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基， R19，R20，R21，R22，R23，R24，R25是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; R26，R27，R28，R29是H，C1-C6烷基，C3-C7环烷基; C 3 -C 6环烷基 - （C 1 -C 2烷基）; 其可以被一个或多个卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基取代; 我，我对应1或2，可能会有不同的含义; m，m'，m“，m”'，m？v，mv对应于0,1或2，可以具有不同的含义; n为1,2或3; q为1,2或3; p，p'，p“，p'”对应于0,1,2或3，可以具有不同的含义; 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V1b受体的拮抗剂，例如。治疗抑郁症和焦虑症。

2. 发明申请

WO2009130232A1 PYRAZOLO [1, 5 -A] PYRAZINE DERIVATIVES AS ANTAGONISTS OF V1B RECEPTORS 审中-公开
标题翻译：吡咯并[1,5-A]吡嗪衍生物作为V1B受体的拮抗剂
公开(公告)号：WO2009130232A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054780
申请日：2009-04-22
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
发明人： DI FABIO, Romano , GENTILE, Gabriella , POZZAN, Alfonso , TARSI, Luca , TERRENI, Silvia , TONELLI, Federica
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel compounds of formula (I) or salts thereof: wherein R is -X-[CH 2 ] n CR 4 R 5 -Y; or a group G; G is one of the groups selected form the list consisting of G1, G2, G3, G4, G5, G6, G7, G8, G9, G10, G11 and G12, and the rest of the variables are as specified in the claims, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as antagonists of V1b receptors, e.g. to treat depression and anxiety.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中R是-X- [CH2] nCR4R5-Y; 或G组; G是从由G1，G2，G3，G4，G5，G6，G7，G8，G9，G10，G11和G12组成的列表中选择的组之一，其余变量如权利要求中所述，对于它们的制备，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V1b受体的拮抗剂，例如治疗抑郁症和焦虑症。

3. 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。

4. 发明申请

WO2005080382A1 AZABICYCLO (3.1.0) HEXANE DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： AZ Y Y O O O O S S S S S S S S S S S S S S S S S S S S S S S S S S
公开(公告)号：WO2005080382A1
公开(公告)日：2005-09-01
申请号：PCT/EP2005/001940
申请日：2005-02-21
申请人： GLAXO GROUP LIMITED , ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： ARISTA, Luca , BONANOMI, Giorgio , CAPELLI, Anna Maria , DAMIANI, Federica , DI FABIO, Romano , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D403/12
CPC分类号： C07D495/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/08
摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups 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; R 5 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 a 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; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1; 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 or as antipsychotic agents.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐，其中G选自：苯基，吡啶基，苯并噻唑基，吲唑基; p为0〜5的整数; R 1独立地选自：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; 或对应于R5组; R2是氢或C1-4烷基; R3是C1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被1,2,3或4个取代基取代选自：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; R5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，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; 当R1为氯且p为1时，该R1不存在于与分子的其余部分的连接键的邻位; 当R1对应于R5时，p为1; 它们的制备方法，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受体的调节剂。治疗药物依赖或作为抗精神病药。

5. 发明申请

WO2007022933A1 TRIAZOLE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译：作为DOPAMINE D3受体的调节剂的三唑衍生物
公开(公告)号：WO2007022933A1
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008200
申请日：2006-08-18
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DI FABIO, Romano , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D413/14 , C07D403/14 , A61K31/4196 , A61P25/18
CPC分类号： C07D403/14 , C07D413/14
摘要： The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: G is a 5- or 6-membered heteroaromatic group, or is a 9- or 10-membered bicyclic heteroaromatic group containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein G is not pyridyl, indazolyl or benzothiazolyl; p is an integer ranging from 0 to 4; R 1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl or SF 5 ; or corresponds to a group R 5 ; R 2 is hydrogen or C 1-4 alkyl; n is 2 or 3; X is S or -CH 2 -; R 3 is C 1-4 alkyl; R 4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups 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 and C 1-4 alkanoyl; R 5 is isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein each group is optionally substituted by one or two substituents selected from: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1- 4alkoxy and C 1-4 alkanoyl; 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 substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其盐：其中：G是5-或6-元杂芳族基团，或是含有一个或两个独立选择的杂原子的9或10元双环杂芳族基团氮和氧，其中G不是吡啶基，吲唑基或苯并噻唑基; p为0〜4的整数。 R 1独立地选自：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烷酰基或SF 5 N; 或对应于基团R 5; R 2是氢或C 1-4烷基; n为2或3; X是S或-CH 2 - ; R 3是C 1-4烷基; R 4是氢或苯基，杂环基，5或6元杂芳族基团或8至11元双环基团，其中任何基团任选被 1,2,3或4个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1 -4个烷氧基和C 1-4烷酰基; R 5是异恶唑基，-CH 2 N-吡咯基，1,1-二氧化-2-异噻唑烷基，噻吩基，噻唑基，吡啶基或2-吡咯烷基，其中各基团任选地被一个或两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 - 烷氧基和C 1-4烷酰基; 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D 3受体的调节剂，例如。治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

6. 发明申请

WO2005118549A2 COMPOUNDS HAVING AFFINITY FOR DOPAMINE D3 RECEPTOR AND USES THEREOF 审中-公开
标题翻译：具有DOPAMINE D3受体的亲和性的化合物及其用途
公开(公告)号：WO2005118549A2
公开(公告)日：2005-12-15
申请号：PCT/EP2005/005965
申请日：2005-05-31
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BONANOMI, Giorgio , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter Wolfgang , MICHELI, Fabrizio , TARSI, Luca , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D223/16
CPC分类号： C07D513/04 , C07D487/04
摘要： Compounds of formula (I) and salts thereof are disclosed: wherein A, R 1 , m, R 2 , n, R 3 , R 4 , q, W 1 , W 2 , R 5 and R 6 are as defined in the description. Methods of preparing the compounds and uses thereof in medicine, for example in the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物及其盐：其中A，R1，m，R2，n，R3，R4，q，W1，W2，R5和R6如说明书中所定义。还公开了制备化合物的方法及其在医药中的用途，例如治疗精神分裂症或药物依赖性。

7. 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。

8. 发明申请

WO2009027293A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2009027293A1
公开(公告)日：2009-03-05
申请号：PCT/EP2008/060911
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： C07D209/52 , A61K31/403 , A61P25/00
CPC分类号： C07D209/52
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。

9. 发明申请

WO2006108701A1 3- (1,2,4-TRIAZOL-3YLALKYL) AZABRICLO (3.1.0) HEXANE DERIVATIVES AS MODULATORS OF DOPAMINE D3 RECEPTORS 审中-公开
标题翻译： 3-（1,2,4-TRIAZOL-3YLALKYL）AZABRICLO（3.1.0）作为DOPAMINE D3受体的调节剂的HEXANE衍生物
公开(公告)号：WO2006108701A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003554
申请日：2006-04-12
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
发明人： BONANOMI, Giorgio , CHECCHIA, Anna , FAZZOLARI, Elettra , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca , TERRENI, Silvia
IPC分类号： C07D403/06 , C07D403/14 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4196 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/501 , A61K31/497 , A61P25/00 , C07D409/14
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein " G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; " p is an integer ranging from 0 to 5; " R 1 is independently selected from a group consisting of: 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 5; " each R 2 is independently hydrogen, fluorine or C 1-4 alkyl; " n is 2, 3, 4, or 5; " R 3 is C 1-4 alkyl; " R 4 is hydrogen, or a C 1-4 alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups 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, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ;or R 4 is a -SR 6 group; " R 5 is selected from a group consisting of: isoxazolyl, -CH 2 -N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl and 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from a group consisting of: halogen, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 alkoxy and C 1-4 alkanoyl; " R 6 is C 1-4 alkyl or -CH 2 C 3-4 cycloalkyl; and when R 1 is chlorine and p is 1, such R 1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R 1 corresponds to R 5 , p is 1. 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 cognition impairment.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐：其中“G选自：苯基，吡啶基，苯并噻唑基和吲唑基”; p是0-5的整数; “R 1”独立地选自：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R 5;每个R 2独立地是氢，氟或C 1-4烷基; “n为2,3,4或5;”R 3为C 1-4烷基; “R”4是氢或C 1-4烷基，苄基，苯基，杂环基，5或6元杂芳基或8至11元双环基团，其中任何基团任选被1,2,3或4个选自以下的取代基取代：卤素，氰基，C 1-4烷基，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烷基，烷酰基和SF 5;或R 4是-SR 6 C 6;选择“R 5” 由以下组成的组：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，吡啶基和2-吡咯烷基，并且这种基团任选被取代通过一个或两个选自以下的取代基：卤素，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4 - 烷氧基和C 1-4烷酰基; “R 6”是C 1-4烷基或-CH 2 -SO 3 -S-环烷基;当R 相对于与分子的其余部分的连接键，R 1不在氯原子的邻位存在这样的R 1，并且当R _{1 对应于R 5，p为1.它们的制备方法，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D的调节剂 > 3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，早泄或认知障碍。}

10. 发明申请

WO2006002928A1 COMPOUNDS HAVING AFFINITY FOR THE DOPAMINE D3 RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：多巴胺D3受体具有重要性的化合物及其在医药中的应用
公开(公告)号：WO2006002928A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/007069
申请日：2005-06-29
申请人： GLAXO GROUP LIMITED , BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
发明人： BONANOMI, Giorgio , CARDULLO, Francesca , DAMIANI, Federica , GENTILE, Gabriella , HAMPRECHT, Dieter , MICHELI, Fabrizio , TARSI, Luca
IPC分类号： C07D498/04
CPC分类号： C07D513/04
摘要： Compounds of formula (I) or a salt thereof are disclosed, wherein A, m R 1 , R 2 , R 3 , q, W 1 , W 2 , R 4 and R 5 are as defined in the description. Processes for preparation and uses of the compounds in medicine, for example for the treatment of schizophrenia or drug dependency, are also disclosed.
摘要翻译：公开了式（I）化合物或其盐，其中A，m R 1，R 2，R 3，q，W W 1，W 2，R 4和R 5如说明书中所定义。还公开了用于药物中化合物的制备和用途的方法，例如用于治疗精神分裂症或药物依赖性。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式