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    ABUSE-RESISTANT AMPHETAMINE PRODRUGS
    37.
    发明申请
    ABUSE-RESISTANT AMPHETAMINE PRODRUGS 审中-公开
    耐药AMPHETAMINE PRODRUGS

    公开(公告)号：US20110009669A1

    公开(公告)日：2011-01-13

    申请号：US12701483

    申请日：2010-02-05

    申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

    发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Robert Oberlender ,  Thomas Piccariello ,  Bernhard J. Paul ,  Christopher A. Verbicky

    IPC分类号： C07C231/12

    CPC分类号： A61K31/27 ,  A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y10S436/901 ,  Y10T436/173845

    摘要： The invention describes compounds, compositions, and methods of using the same comprising a chemical moiety covalently attached to amphetamine. These compounds and compositions are useful for reducing or preventing abuse and overdose of amphetamine. These compounds and compositions find particular use in providing an abuse-resistant alternative treatment for certain disorders, such as attention deficit hyperactivity disorder (ADHD), ADD, narcolepsy, and obesity. Oral bioavailability of amphetamine is maintained at therapeutically useful doses. At higher doses bioavailability is substantially reduced, thereby providing a method of reducing oral abuse liability. Further, compounds and compositions of the invention decrease the bioavailability of amphetamine by parenteral routes, such as intravenous or intranasal administration, further limiting their abuse liability.

    摘要翻译： 本发明描述了使用包含与苯丙胺共价连接的化学部分的化合物，组合物和方法。 这些化合物和组合物可用于减少或预防滥用和过量安非他明。 这些化合物和组合物特别用于提供某些障碍（例如注意力缺陷多动障碍（ADHD），ADD，发作性睡病和肥胖）的耐药性替代治疗。 苯丙胺的口服生物利用度维持在治疗有用的剂量。 在较高剂量下，生物利用度显着降低，从而提供减少口服滥用责任的方法。 此外，本发明的化合物和组合物通过肠胃外途径（例如静脉内或鼻内给药）降低苯丙胺的生物利用度，进一步限制其滥用责任。