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    Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives
    3.
    发明授权
    Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives 有权
    使用四氢吲哚酮类似物和衍生物治疗认知/注意力缺陷障碍的方法

    公开(公告)号：US08063233B2

    公开(公告)日：2011-11-22

    申请号：US12414539

    申请日：2009-03-30

    申请人： Alvin J. Glasky ,  David B. Fick ,  David R. Helton

    发明人： Alvin J. Glasky ,  David B. Fick ,  David R. Helton

    IPC分类号： C07D209/04

    CPC分类号： C07D209/08 ,  C07D209/88

    摘要： Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided. The compounds used to treat and/or palliate cognitive/attention deficit disorders in general include a tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y1)-D, where Y1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.

    摘要翻译： 公开了通常使用四氢吲哚酮衍生物和类似物，特别是其中四氢吲哚酮衍生物或类似物共价连接到另一部分以形成双功能缀合物的四氢吲哚酮衍生物或类似物的治疗认知/注意力缺陷障碍的方法。 更具体地，提供了用于治疗成人和儿童的注意力缺陷障碍和注意缺陷多动障碍以及轻度认知障碍和痴呆的方法和组合物。 用于治疗和/或缓解认知/注意力缺陷障碍的化合物通常包括四氢吲哚酮衍生物或类似物包含通过连接体L与B部分连接的9位双环部分A部分，其中B是羧酸， 羧酸酯或结构N（Y1）-D的部分，其中Y1可以是各种取代基之一，包括氢或烷基，D是增强药理作用，促进吸收或血液中的部分， 衍生物或类似物的脑屏障穿透。 部分A具有与五元环稠合的六元环。 部分A可以在五元环中具有一个，两个或三个氮原子。 部分A可以是四氢吲哚酮部分。 部分B可以是多种部分之一，包括具有向异性活性或其他生物或生理活性的部分。

    Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives
    5.
    发明授权
    Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives 失效
    使用四氢吲哚酮类似物和衍生物治疗认知/注意力缺陷障碍的方法

    公开(公告)号：US07531670B2

    公开(公告)日：2009-05-12

    申请号：US11002329

    申请日：2004-12-01

    申请人： Alvin Jerald Glasky ,  David B. Fick ,  David R. Helton

    发明人： Alvin Jerald Glasky ,  David B. Fick ,  David R. Helton

    IPC分类号： C07D209/04

    CPC分类号： C07D209/08 ,  C07D209/88

    摘要： Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided. The compounds used to treat and/or palliate cognitive/attention deficit disorders in general include a tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y1)-D, where Y1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption or blood-brain barrier penetration of the derivative or analogue. The moiety A has a six-membered ring fused to a five-membered ring. The moiety A can have one, two, or three nitrogen atoms in the five membered ring. The moiety A can be a tetrahydroindolone moiety. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.

    摘要翻译： 公开了通常使用四氢吲哚酮衍生物和类似物，特别是其中四氢吲哚酮衍生物或类似物共价连接到另一部分以形成双功能缀合物的四氢吲哚酮衍生物或类似物的治疗认知/注意力缺陷障碍的方法。 更具体地，提供了用于治疗成人和儿童的注意力缺陷障碍和注意缺陷多动障碍以及轻度认知障碍和痴呆的方法和组合物。 用于治疗和/或缓解认知/注意力缺陷障碍的化合物通常包括四氢吲哚酮衍生物或类似物包含通过连接体L与B部分连接的9位双环部分A部分，其中B是羧酸， 羧酸酯或结构N（Y1）-D的部分，其中Y1可以是各种取代基之一，包括氢或烷基，D是增强药理作用，促进吸收或血液中的部分， 衍生物或类似物的脑屏障穿透。 部分A具有与五元环稠合的六元环。 部分A可以在五元环中具有一个，两个或三个氮原子。 部分A可以是四氢吲哚酮部分。 部分B可以是多种部分之一，包括具有向异性活性或其他生物或生理活性的部分。

    Tetrahydroindolone and purine derivatives linked to arylpiperazines
    7.
    发明授权
    Tetrahydroindolone and purine derivatives linked to arylpiperazines 有权
    连接到芳基哌嗪的四氢吲哚酮和嘌呤衍生物

    公开(公告)号：US06770638B2

    公开(公告)日：2004-08-03

    申请号：US10209451

    申请日：2002-07-30

    申请人： David B. Fick ,  Mark M. Foreman ,  Alvin J. Glasky ,  David R. Helton

    发明人： David B. Fick ,  Mark M. Foreman ,  Alvin J. Glasky ,  David R. Helton

    IPC分类号： A61K3133

    CPC分类号： C07D403/12 ,  A61K31/496 ,  A61K31/506 ,  C07D209/08 ,  C07D209/88 ,  C07D403/14 ,  C07D413/12 ,  C07D417/12

    摘要： Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.

    摘要翻译： 公开了包含与芳基哌嗪及其衍生物连接的四氢吲哚酮的药物复合组合物。 具体地，公开了可用于治疗抗精神病药物的复合组合物。 本文公开的复合组合物可以有效地改善症状并治疗精神病，而不引起认知功能的降低。 通常，复合化合物由两个部分A和B组成，其中四氢吲哚酮包含通过连接体L与B部分连接的部分A，其中B是芳基哌嗪基部分。 复合化合物通过与GABA，血清素和多巴胺受体的相互作用积极地提供抗精神病药物。 具有组合活性的复合分子将提供治疗精神和神经疾病而没有认知障碍。