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    Triazolyl derivatives of azabicyclo [3.1.0] hexane as dopamine D3 receptor modulators
    1.
    发明授权
    Triazolyl derivatives of azabicyclo [3.1.0] hexane as dopamine D3 receptor modulators 失效
    氮杂双环[3.1.0]己烷的三唑基衍生物作为多巴胺D3受体调节剂

    公开(公告)号：US07863299B2

    公开(公告)日：2011-01-04

    申请号：US12064118

    申请日：2006-08-18

    申请人： Anna Maria Capelli ,  Elettra Fazzolari ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    发明人： Anna Maria Capelli ,  Elettra Fazzolari ,  Fabrizio Micheli ,  Giovanna Tedesco ,  Silvia Terreni

    IPC分类号： A61K31/428 ,  A61K31/4196 ,  A61K31/4439 ,  C07D403/14 ,  C07D417/14

    CPC分类号： C07D413/14

    摘要： The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; 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 and C1-4alkanoyl; R5 is isoxazolyl, —CH2—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, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; with the proviso that when m5=m6=1, R7 is not chlorine; 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 substance related disorders, as antipsychotic agents, premature ejaculation or cognition impairment.

    摘要翻译： 本发明涉及新型式（IC）化合物或其盐：其中：p为0至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; 或对应于R5组; m1，m2，m3，m4为0; m5，m6和m7各自独立地为0,1或2，其中m5，m6和m7的和为1或2; R6是C1-6烷基; R7是卤素，C1-6烷基或卤代C 1-6烷基; R2是氢或C1-4烷基; n为2或3; X是S或-CH 2 - ; 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烷氧基和C 1-4烷酰基; R5是异恶唑基，-CH2-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，其中每个基团任选被一个或两个选自以下的取代基取代：卤素，氰基，C1 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基和C 1-4烷酰基; 条件是当m5 = m6 = 1时，R7不是氯; 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。 治疗与物质相关的疾病，作为抗精神病药，早泄或认知障碍。

    Azabicyclo [3.1.0] hexylphenyl derivatives as modulators of dopamine D3 receptors
    3.
    发明授权
    Azabicyclo [3.1.0] hexylphenyl derivatives as modulators of dopamine D3 receptors 失效
    氮杂双环[3.1.0]己基苯基衍生物作为多巴胺D3受体的调节剂

    公开(公告)号：US07776904B2

    公开(公告)日：2010-08-17

    申请号：US12064121

    申请日：2006-08-18

    申请人： Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Adolfo Prandi ,  Silvia Terreni

    发明人： Gabriella Gentile ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Adolfo Prandi ,  Silvia Terreni

    IPC分类号： A61K31/403 ,  C07D209/52

    CPC分类号： C07D209/52

    摘要： The present invention relates to novel compounds of formula (IA) or a salt thereof: wherein: A is attached to the phenyl group at the meta position or the para position relative to the cyclopropyl group, and is selected from the group consisting of: —SO2NR5—, —SO2CR2R3—, —CR2R3SO2— and —NR5SO2—; R1 is hydrogen, C1-6alkyl, haloC1-6alkyl or C2-6alkylene; R2 and R3 are independently hydrogen or C1-6alkyl; R4 is hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; R5 is hydrogen, C1-6alkyl, or a phenyl optionally substituted by R4; and R6 is hydrogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; 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 substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.

    摘要翻译： 本发明涉及新的式（IA）化合物或其盐：其中：A相对于环丙基在间位或对位与苯基连接，并且选自： - SO 2 NR 5 - ， - SO 2 CR 2 R 3 - ， - CR 2 R 3 SO 2 - 和-NR 5 SO 2 - ; R1是氢，C1-6烷基，卤代C 1-6烷基或C 2-6亚烷基; R2和R3独立地是氢或C1-6烷基; R 4是氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R5是氢，C1-6烷基或任选被R4取代的苯基; 并且R 6是氢，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基或卤代C 1-6烷氧基; 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。 治疗物质相关疾病，作为抗精神病药物早泄或认知障碍。

    Compounds having activity at 5ht2c receptor and uses thereof
    6.
    发明申请
    Compounds having activity at 5ht2c receptor and uses thereof 审中-公开

    公开(公告)号：US20070191457A1

    公开(公告)日：2007-08-16

    申请号：US10551904

    申请日：2004-04-05

    申请人： Giorgio Bonanomi ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Silvia Terreni

    发明人： Giorgio Bonanomi ,  Dieter Hamprecht ,  Fabrizio Micheli ,  Silvia Terreni

    IPC分类号： A61K31/454 ,  C07D401/02

    CPC分类号： C07D209/46

    摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein R1 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, —COOR3, —COR4, wherein R3 and R4 are independently hydrogen or C1-6alkyl, or —COR5, wherein R5 is amino, mono- or di-C1-6alkylamino or an N-linked 4 to 7 membered heterocyclic group; p is 0, 1, 2 or 3; Q is a 6-membered aromatic group or a 6-membered heteroaromatic group; A is —(CH2—CH2)—, —(CH═CH)—, or a group —(CHR7)— wherein R7 is hydrogen, halogen, hydroxy, cyano, nitro, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkyloxy, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy or C1-6alkylthio; R2 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; X is oxygen, sulfur, —CH2— or NR8 wherein R8 is hydrogen or C1-6alkyl; Y is a single bond, —CH2—, —(CH2)2— or —CH═CH—; and Z is an optionally substituted N-linked heterocyclic group or a C-linked 4 to 7 membered heterocyclic group containing at least one nitrogen, or Z is —NR9R10 where R9 and R10 are independently hydrogen or C1-6alkyl. Methods of preparation and uses thereof in therapy, such as for depression or anxiety, are also disclosed.