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28 条记录 (耗时 0.065 秒)

    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
    22.
    发明申请
    COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
    潜在的谷氨酸受体的化合物及其在医药中的应用

    公开(公告)号：US20090170902A1

    公开(公告)日：2009-07-02

    申请号：US12278604

    申请日：2007-02-06

    申请人： Daniele Andreotti ,  Simon Edward Ward

    发明人： Daniele Andreotti ,  Simon Edward Ward

    IPC分类号： A61K31/443 ,  C07D307/02 ,  C07D405/00 ,  A61K31/34

    CPC分类号： C07D401/10 ,  C07D307/22 ,  C07D409/10

    摘要： Compounds of formula (I), salts and solvates thereof are provided: wherein Ar is selected from phenyl, pyridyl, furanyl and thienyl, each optionally substituted with one or more groups Y; and each Y group is independently selected from the group consisting of: halo, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, cyano, C(O)C1-4alkyl, NHSO2C1-4alkyl, NMeSO2C1-4alkyl, NHCOC1-4alkyl, NMeCOC1-4alkyl, SOC1-4alkyl, SO2C1-4alkyl, and CO2C1-4alkyl, or two Y groups together form a cyclic group —O(CH2)O—. Processes for preparation, and uses thereof in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.

    摘要翻译： 提供式（I）化合物，其盐和溶剂化物：其中Ar选自苯基，吡啶基，呋喃基和噻吩基，各自任选被一个或多个Y基团取代; 并且每个Y基团独立地选自：卤素，C 1-4烷基，卤代C 1-4烷基，C 1-4烷氧基，氰基，C（O）C 1-4烷基，NHSO 2 C 1-4烷基，NMeSO 2 C 1-4烷基，NHCOC 1-4烷基，NMeCOC 1 - 烷基，SO1-4烷基，SO2C1-4烷基和CO2C1-4烷基，或两个Y基团一起形成环状基团-O（CH 2）O-。 还公开了制备方法及其用于治疗谷氨酸受体功能如精神分裂症或认知障碍的还原或不平衡介导的疾病或病症的用途。

    3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands
    25.
    发明授权
    3-triazolylthiaalkyl-3-azabicyclo (3-1-O) hexanes and their use as dopamine D3 receptor ligands 失效
    3-三唑基硫杂烷基-3-氮杂双环（3-1-O）己烷及其作为多巴胺D3受体配体的用途

    公开(公告)号：US07803820B2

    公开(公告)日：2010-09-28

    申请号：US11911035

    申请日：2006-04-12

    申请人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A61K31/41 ,  C07D249/08 ,  C07D257/00

    CPC分类号： C07D413/12 ,  C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 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 and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; 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, 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R 1是氢或C 1-4烷基; R2是C1-4烷基; R 3为氢或苯基，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烷酰基和SF 5; p是0，1，2，3或4; R 4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烷氧基和C 1-4烷酰基; n为0或1; 其中当R 4为氯并且p为1时，相对于与分子的其余部分的连接键，该R 4不存在于邻位; 并且其中，如果n为0，则R 3包含至少一个SF 5基团作为取代基; 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。

    3-Triazolylthiaalkyl-3-Azabicyclo (3-1-O) Hexanes and Their Use as Dopamine D3 Receptor Ligands
    27.
    发明申请
    3-Triazolylthiaalkyl-3-Azabicyclo (3-1-O) Hexanes and Their Use as Dopamine D3 Receptor Ligands 失效
    3-三唑基硫杂烷基-3-氮杂双环（3-1-O）己烷及其作为多巴胺D3受体配体的用途

    公开(公告)号：US20080176917A1

    公开(公告)日：2008-07-24

    申请号：US11911035

    申请日：2006-04-12

    申请人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    发明人： Daniele Andreotti ,  Anna Checchia ,  Dieter Hamprecht ,  Fabrizio Micheli

    IPC分类号： A61K31/4196 ,  C07D209/52 ,  A61K31/403 ,  A61P25/18 ,  C07D249/12

    CPC分类号： C07D413/12 ,  C07D403/12

    摘要： The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 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 and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; 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, 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R 1是氢或C 1-4烷基; R 2是C 1-4烷基; R 3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，C 1-4烷酰基和SF 5; p是0，1，2，3或4; R 4和R 4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烷氧基和C 1-4烷酰基; n为0或1; 其中当R 4为氯且p为1时，相对于与分子其余部分的连接键，该R 4不在邻位; 并且其中，如果n为0，则R 3 3包含至少一个SF 5基团作为取代基; 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。