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    Methods for treating cognitive/attention deficit disorders using tetrahydroindolone analogues and derivatives
    2.
    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：US06982269B2

    公开(公告)日：2006-01-03

    申请号：US10193550

    申请日：2002-07-09

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

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

    IPC分类号： A61K31/52 ,  A61K31/495 ,  A61K43/54 ,  A61K31/33

    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（Y 1 H）-D的部分，其中Y 1可以是多种取代基之一，包括氢或烷基， 并且D是增强药理作用，促进衍生物或类似物的吸收或血脑屏障穿透的部分。 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
    3.
    发明申请
    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/注意缺陷性疾病的方法

    公开(公告)号：US20090192319A1

    公开(公告)日：2009-07-30

    申请号：US12414539

    申请日：2009-03-30

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

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

    IPC分类号： C07D209/08

    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.
    发明申请
    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：US20050096317A1

    公开(公告)日：2005-05-05

    申请号：US11002329

    申请日：2004-12-01

    申请人： Alvin Glasky ,  David Fick ,  David Helton

    发明人： Alvin Glasky ,  David Fick ,  David Helton

    IPC分类号： A61P25/28 ,  C07D209/88 ,  A61K31/541 ,  A61K31/404 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377

    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（Y 1 H）-D的部分，其中Y 1可以是多种取代基之一，包括氢或烷基， 并且D是增强药理作用，促进衍生物或类似物的吸收或血脑屏障穿透的部分。 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。

    EMESIS TREATMENT
    9.
    发明申请
    EMESIS TREATMENT 审中-公开
    EMESIS治疗

    公开(公告)号：US20120208892A1

    公开(公告)日：2012-08-16

    申请号：US13501531

    申请日：2010-10-15

    申请人： David Helton ,  James Lucot

    发明人： David Helton ,  James Lucot

    IPC分类号： A61K31/135 ,  C07C215/64 ,  A61P1/08

    CPC分类号： A61K31/135 ,  A61K31/13

    摘要： A method of treating or preventing emesis through the administration of an effective dosage of a 2-(amino) tetralin compound in which one of the S or R enantiomers of the 2-(amino) tetralin compound is present in the composition in excess of the other enantiomer, and compositions comprising such a 2-(amino) tetralin compound in which the ratio of the S and R enantiomers is at least 2:1.

    摘要翻译： 通过施用有效剂量的2-（氨基）四氢化萘化合物治疗或预防呕吐的方法，其中2-（氨基）四氢化萘化合物的S或R对映异构体之一存在于组合物中超过 其它对映异构体和包含其中S和R对映异构体的比例至少为2:1的这种2-（氨基）四氢化萘化合物的组合物。