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1. 发明申请

WO2009109608A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2009109608A1
公开(公告)日：2009-09-11
申请号：PCT/EP2009/052567
申请日：2009-03-05
申请人： GLAXO GROUP LIMITED , BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BETTATI, Michela , BONANOMI, Giorgio , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04 , A61K31/435 , A61P25/00
CPC分类号： C07D401/04 , C07D413/04 , C07D417/04 , C07D491/04
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。

2. 发明申请

WO2007113232A1 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：WO2007113232A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053074
申请日：2007-03-30
申请人： Glaxo Group Limited , BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , BONANOMI, Giorgio , CAPELLI, Anna Maria , CHECCHIA, Anna , DI FABIO, Romano , GENTILE, Gabriella , MICHELI, Fabrizio , PASQUARELLO, Alessandra , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14 , A61K31/513 , A61P25/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/14
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; A is a group P1 or a group P2 Wherein 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 5 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 5 is a phenyl group, a 5-14 membered heterocyclic group; and any of such phenyl or heterocyclic 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 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; wherein at least one of R 4 and R 5 is hydrogen; and wherein only one R 2 group may be different from hydrogen; 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元杂芳基双环基团 A是基团P1或基团P2，其中p是0至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烷基，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 6; 并且当p是2至5的整数时，每个R 1可以相同或不同; R 2是氢或C 1-4烷基; n为3,4,5或6; R 6是选自以下的部分：异恶唑基，-CH 2 - N-吡咯基，1,1-二氧代-2-异噻唑烷基，噻吩基，噻唑基，吡啶基，2-吡咯烷酮基和这样的R 6 C 6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 - >一

3. 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。

4. 发明申请

WO2008031772A1 AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE 审中-公开
标题翻译：单一化合物作为单体反应的抑制剂
公开(公告)号：WO2008031772A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059381
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： BERTANI, Barbara , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： C07D221/04 , A61K31/435 , A61P25/00
CPC分类号： C07D221/04
摘要： The present invention relates to novel compounds of formula (I)´, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R 1 is hydrogen or C 1-4 alkyl; R 2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R 18 , each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R 15 ) p , which can be the same or different; p is an integer from 0 to 5; R 3 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 4 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to a group X or X 1 ; R 5 is hydrogen or C 1-4 alkyl; R 7 is hydrogen or C 1-4 alkyl; or is a group X, X 1 , X 2 or X 3 ; wherein X is (IV) X 1 is (V) X 2 is (VI) and X 3 is (VII) R 6 is hydrogen or C 1-4 alkyl; or is a group X or X 1 ; R 9 is C 1-4 alkyl; R 10 is selected from a group consisting of: hydrogen, 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 8 ; R 8 is a 5-6 membered heterocycle group, which may be 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 11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 13 is selected from a group consisting of: hydrogen, 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 8 ; R 14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C 1-4 alkyl, haloC 1-4 alkyl, C 1-4 aIkoxy, haloC 1-4 alkoxy, C 1-4 alkanoyl and SF 5 ; or corresponds to a group R 8 ; R 15 is 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 8 ; R 16 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 17 is hydrogen or C 1-4 alkyl; R 18 is selected from a group consisting of: halog
摘要翻译：本发明涉及新的式（I）化合物，其药学上可接受的盐，前药或溶剂合物：其中R 1是氢或C 1-4烷基; R 2是基团A，K或W，其中A是（II）K是任选被1或2个基团R 18取代的a或β萘基，每个他们是相同或不同的; 并且W是（III），并且其中G是5,6-元单环杂芳基或8至11元杂芳基双环基团; 这样的G可以被相同或不同的（R 15） p是0至5的整数; R 3 3选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 4选自：氢，氟和C 1-4烷基; 或对应于组X或X 1 1; R 5是氢或C 1-4烷基; R 7是氢或C 1-4烷基; 或者为X，X 1，X 2或X 3; 其中X是（Ⅳ）ⅩⅢ是（Ⅴ）ⅩⅥ是（Ⅵ），ⅩⅢ是（Ⅶ） 6是氢或C 1-4烷基; 或者是X或X 1族; R 9是C 1-4烷基; R 10选自：氢，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 8; R 8是5-6元杂环基团，其可以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 1-4烷氧基和C 1-4烷酰基; R 11选自：氢，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 8; R 12选自：氢，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 8; R 13选自：氢，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 8; R 14选自：氢，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 8; R 15选自：卤素，羟基，氰基，C 1-4烷基，卤代C 1-4烷基，C 1-4个碳原子的烷氧基，卤代C 1-4烷氧基，C 1-4烷酰基和SF 5。或对应于基团R 8; R 16是氢，C 1-4烷基，C 3-6环烷基或C 3-6环烷基C _{1-3 烷基; R 17是氢或C 1-4烷基; R 18选自：卤素}

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

WO2008031771A3 3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION 审中-公开
公开(公告)号：WO2008031771A3
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059380
申请日：2007-09-07
申请人： GLAXO GROUP LIMITED , DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
发明人： DI FABIO, Romano , MICHELI, Fabrizio , TEDESCO, Giovanna , TERRENI, Silvia
IPC分类号： A61K31/435 , A61P25/24 , C07D221/04
摘要： The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: formula (I), 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; such G may be substituted by (R 2 ) p , which can be the same or different; R 1 is hydrogen or C 1-4 alkyl; R 2 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 R 8 ; R 5 is hydrogen or C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; R 7 is selected in the group consisting of: hydrogen, fluorine, and C 1-4 alkyl; or corresponds to X, X 1 , X 2 or X 3 ; wherein X corresponds to: formula (a) X 1 corresponds to: formula (b) X 2 corresponds to: formula (c) X 3 corresponds to: formula (d) R 3 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 4 is hydrogen or C 1-4 alkyl; or corresponds to X or X 1 ; R 8 is a 5-6 membered heterocycle group, which may be 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 9 is C 1-4 alkyl; R 10 is hydrogen, C 1-4 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-3 alkyl; R 11 is haloC 1-2 alkyl; p is an integer from 0 to 5; n is 1 or 2. processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as as serotonin (5-HT), dopamine (DA) and norepinephrine (NE), re-uptake inhibitors.

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

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。

9. 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。

10. 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。

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