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    Abuse-resistant amphetamine compounds
    1.
    发明授权
    Abuse-resistant amphetamine compounds 有权
    滥用安非他明类化合物

    公开(公告)号：US07105486B2

    公开(公告)日：2006-09-12

    申请号：US10858526

    申请日：2004-06-01

    申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Scott Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    IPC分类号： A61K38/00

    CPC分类号： A61K31/165 ,  A61K47/542

    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： 本发明描述了使用其的化合物，组合物和方法，其包含与苯丙胺共价连接的化学部分。 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。

    Stabilized thyroxine compounds
    3.
    发明申请
    Stabilized thyroxine compounds 审中-公开
    稳定的甲状腺素化合物

    公开(公告)号：US20040116391A1

    公开(公告)日：2004-06-17

    申请号：US10630650

    申请日：2003-07-31

    申请人： New River Pharmaceuticals Inc.

    发明人： Thomas Piccariello ,  Anne-Frederique Le Clercq

    IPC分类号： A61K031/695 ,  A61K031/66 ,  A61K031/24

    CPC分类号： A61K31/198

    摘要： Throxinyldimethylphosphinate was invented as a prodrug to stabilize thyroxine, a drug widely used to treat hypothyroidism and depression. The presence of the dimethylphosphinate group at the phenolic hydroxyl of thyroxine is key to preventing thyroxine from decomposing through the proposed pathway. The prodrug will be hydrolyzed in the stomach or the gut into thyroxine and the biologically inert dimethylphosphinic acid. Related products may be stabilized with the same or similar protecting groups.

    摘要翻译： 发明了作为用于稳定甲状腺素（一种广泛用于治疗甲状腺功能减退和抑郁症的药物）的前药的甲状腺素二甲基膦酸盐。 甲状腺素酚羟基上二甲基次膦酸盐的存在是防止甲状腺素通过拟议途径分解的关键。 前药将在胃或肠中水解成甲状腺素和生物惰性的二甲基次膦酸。 相关产品可能与相同或相似的保护基团稳定。

    Iodothyronine compositions
    8.
    发明授权
    Iodothyronine compositions 有权
    碘甲腺氨酸组成

    公开(公告)号：US07163918B2

    公开(公告)日：2007-01-16

    申请号：US10136433

    申请日：2002-05-02

    申请人： Thomas Piccariello ,  Lawrence Peter Olon ,  Alex Saunders Goldstein ,  James Scott Moncrief ,  Nancy Johnston Boerth

    发明人： Thomas Piccariello ,  Lawrence Peter Olon ,  Alex Saunders Goldstein ,  James Scott Moncrief ,  Nancy Johnston Boerth

    IPC分类号： A61K38/04 ,  A61K38/05 ,  A61K38/06 ,  C07K4/00 ,  C07K5/087

    CPC分类号： A61K47/645 ,  A61K47/62

    摘要： The present invention relates to compositions comprising thyroxine (T4) and triiodothyronine (T3). More specifically, the invention relates to thyroxine (T4) and triiodothyronine (T3) compositions that include a peptide carrier and thyroxine (T4) and triiodothyronine (T3) covalently attached to at least one of the N-terminus, the C-terminus, a side chain of the peptide carrier, and/or interspersed within the peptide chain; methods for protecting and administering thyroxine (T4) and triiodothyronine (T3); and methods for treating thyroid disorders.

    摘要翻译： 本发明涉及包含甲状腺素（T4）和三碘甲状腺原氨酸（T3）的组合物。 更具体地，本发明涉及包含肽载体和甲状腺素（T4）和三碘甲状腺原氨酸（T3）的甲状腺素（T4）和三碘甲状腺原氨酸（T3）组合物，其共价连接至N-末端，C-末端， 肽载体的侧链和/或散布在肽链内; 保护和服用甲状腺素（T4）和三碘甲状腺原氨酸（T3）的方法; 和治疗甲状腺疾病的方法。

    Abuse-resistant amphetamine compounds
    9.
    发明申请
    Abuse-resistant amphetamine compounds 有权
    滥用安非他明类化合物

    公开(公告)号：US20050054561A1

    公开(公告)日：2005-03-10

    申请号：US10858526

    申请日：2004-06-01

    申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    IPC分类号： A61K31/165 ,  A61K31/7008 ,  A61K38/16 ,  A61K47/48 ,  A61K48/00

    CPC分类号： A61K31/165 ,  A61K47/542

    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： 本发明描述了使用其的化合物，组合物和方法，其包含与苯丙胺共价连接的化学部分。 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。

    Abuse resistant lysine amphetamine compounds
    10.
    发明申请
    Abuse resistant lysine amphetamine compounds 有权
    滥用抗性赖氨酸苯丙胺化合物

    公开(公告)号：US20050038121A1

    公开(公告)日：2005-02-17

    申请号：US10857619

    申请日：2004-06-01

    申请人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    发明人： Travis Mickle ,  Suma Krishnan ,  Barney Bishop ,  Christopher Lauderback ,  James Moncrief ,  Rob Oberlender ,  Thomas Piccariello

    IPC分类号： A61K31/165 ,  A61K31/198 ,  A61K38/00 ,  A61K47/48

    CPC分类号： A61K31/165 ,  A61K47/542 ,  C07C237/06 ,  Y02A50/415 ,  Y10S436/901 ,  Y10T436/173845

    摘要： The present invention describes compounds, compositions and methods of using the same comprising lysine 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： 本发明描述了使用其包含与苯丙胺共价连接的赖氨酸的化合物，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。