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    Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors
    3.
    发明授权
    Azabicyclo (3.1.0.) hexane derivatives useful as modulators of dopamine D3 receptors 有权
    可用作多巴胺D3受体调节剂的氮杂双环（3.1.0。）己烷衍生物

    公开(公告)号：US07855298B2

    公开(公告)日：2010-12-21

    申请号：US10598200

    申请日：2005-02-21

    申请人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： C07D215/38

    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: 1. wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; or a salt thereof which are useful as modulators of dopamine D3 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：1.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; 或其盐，其可用作多巴胺D3受体的调节剂，例如， 治疗药物依赖或作为抗精神病药。

    Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors
    4.
    发明申请
    Azabicyclo (3.1.0) Hexane Derivatives Useful As Modulators Of Dopamine D3 Receptors 有权
    可用作多巴胺D3受体调节剂的氮杂双环（3.1.0）己烷衍生物

    公开(公告)号：US20100160336A1

    公开(公告)日：2010-06-24

    申请号：US12639282

    申请日：2009-12-16

    申请人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Luca Arista ,  Giorgio Bonanomi ,  Anna Maria Capelli ,  Federica Damiani ,  Romano Di Fabio ,  Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Luca Tarsi ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： A61K31/50 ,  C07D403/14

    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; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, 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 D3 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。

    Compounds having activity at 5ht2c receptor and uses thereof
    5.
    发明申请
    Compounds having activity at 5ht2c receptor and uses thereof 审中-公开

    公开(公告)号：US20060205788A1

    公开(公告)日：2006-09-14

    申请号：US10548118

    申请日：2004-02-24

    申请人： Federica Damiani ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Giovanna Tedesco

    发明人： Federica Damiani ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Alessandra Pasquarello ,  Giovanna Tedesco

    IPC分类号： A61K31/454 ,  C07D403/02

    CPC分类号： C07D207/26 ,  C07D207/273 ,  C07D207/38

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 is hydrogen, fluoro, chloro, hydroxy, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy or haloC1-6alkoxy; m is 0 when ═ is a double bond and m is 1 when ═ is a single bond; R2 is hydrogen, halogen, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; X is —(CH2—CH2)—, —(CH═CH)—, —(CH2)3—, —C(CH3)2—, —(CH═CH—CH2)—, —(CH2-CH═CH)— or a group —(CHR5)— wherein R5 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R3 is halogen, cyano, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, C1-6alkoxy, C1-6alkylthio, hydroxy, amino, mono- or di-C1-6alkylamino, an N-linked 4 to 7 membered heterocyclic group, nitro, haloC1-6alkyl, haloC1-6alkoxy, aryl, arylC1-6alkyl, arylC1-6alkyloxy, arylC1-6alkylthio or COOR6, CONR7R8 or COR9 wherein R6, R7, R8 and R9 are independently hydrogen or C1-6alkyl; p is 0, 1 or 2 or 3; R4 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C1-6alkanoyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; Y is oxygen, sulfur, —CH2— or NR10 wherein R10 is hydrogen or C1-6alkyl; D is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is —NR11R12 where R11 and R12 are independently hydrogen or C1-6alkyl, or an optionally substituted N-linked or C-linked 4 to 7 membered heterocyclic group. Method of preparation and uses of the compounds in therapy, for example depression and anxiety, are also disclosed.