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    Treatment of psychostimulant addiction
    3.
    发明授权
    Treatment of psychostimulant addiction 失效
    治疗精神兴奋剂成瘾

    公开(公告)号：US07632843B2

    公开(公告)日：2009-12-15

    申请号：US10539501

    申请日：2003-12-11

    申请人： Igor Krisch ,  Marko Zivin ,  Natasa Milivojevic ,  Rudolf Rucman ,  Breda Bole-Vunduk ,  Uros Urleb

    发明人： Igor Krisch ,  Marko Zivin ,  Natasa Milivojevic ,  Rudolf Rucman ,  Breda Bole-Vunduk ,  Uros Urleb

    IPC分类号： A61K31/135 ,  A61K31/33 ,  A61K31/395 ,  A61K31/56 ,  A61P25/30

    CPC分类号： A61K31/48 ,  Y10S514/81

    摘要： The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8β-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction. In addition to the treatment of cocaine addiction, the present invention also relates to the method for treatment of the addiction with amphetamine, methamphetamine, dextroamphetamine, 3,4-methylenedioxymethamphetamine and pemoline or acid addition salts thereof.

    摘要翻译： 本发明属于制药工业领域，涉及一种用于治疗精神兴奋剂成瘾的新方法，特别是可卡因成瘾或其药学上可接受的酸加成盐，其具有治疗有效量的9,10-二脱氮-N- 甲基-N-（2-丙基）-6-甲基-β-氨基甲基麦角线，其形式为游离碱或药学上可接受的加成盐形式，特别是二马来酸盐，以及含有所述 复合。 在文献中，该化合物也以代号LEK-8829所知。 更具体地，本发明涉及一种治疗可卡因戒断后禁欲症状的治疗方法，抑制可卡因戒断渴望症状，抑制可卡因加强渴求症状的新方法，以及所述活性物质用于 制备用于治疗可卡因成瘾的药物组合物。 除了治疗可卡因成瘾之外，本发明还涉及用苯丙胺，甲基苯丙胺，右旋安非他明，3,4-亚甲二氧基甲基安非他明和糠基苯甲酸或其酸加成盐治疗成瘾的方法。

    Treatment of psychostimulant addiction
    4.
    发明申请
    Treatment of psychostimulant addiction 失效

    公开(公告)号：US20060014775A1

    公开(公告)日：2006-01-19

    申请号：US10539501

    申请日：2003-11-12

    申请人： Igor Krisch ,  Marko Zivin ,  Natasa Milivojevic ,  Rudolf Rucman ,  Breda Bole-Vunduk ,  Uros Urleb

    发明人： Igor Krisch ,  Marko Zivin ,  Natasa Milivojevic ,  Rudolf Rucman ,  Breda Bole-Vunduk ,  Uros Urleb

    IPC分类号： A61K31/48

    CPC分类号： A61K31/48 ,  Y10S514/81

    摘要： The present invention belongs to the field of pharmaceutical industry and relates to a new method for the treatment of psychostimulant addiction, in particular cocaine addiction, or pharmaceutically acceptable acid addition salts thereof, with a therapeutically effective amount of 9,10-didehydro-N-methyl-N-(2-propy-nyl)-6-methyl-8β-aminomethylergo-line in the form of free base or in the form of pharmaceutically acceptable addition salt, in particular the bimaleate salt, as well as pharmaceutical compositions containing said compound. In literature, the compound is also known under code LEK-8829. More particularly, present invention relates to a novel method of treatment for reduction of abstinence symptoms after cocaine withdrawal and for suppression the symptoms of craving for cocaine withdrawal and for suppression the symptoms of craving for cocaine reinforcement, and to the use of said active substance for the preparation of the pharmaceutical composition for the treatment of cocaine addiction. In addition to the treatment of cocaine addiction, the present invention also relates to the method for treatment of the addiction with amphetamine, methamphetamine, dextroamphetamine, 3,4-methylenedioxymethamphetamine and pemoline or acid addition salts thereof.

    Inclusion complexes of racemic ibuproxam and of optically active ibuproxam with cyclodextrin derivatives, pharmaceutical preparations containing said inclusion complexes and methods for using same
    6.
    发明授权
    Inclusion complexes of racemic ibuproxam and of optically active ibuproxam with cyclodextrin derivatives, pharmaceutical preparations containing said inclusion complexes and methods for using same 失效
    外消旋布洛康和旋光布洛克星与环糊精衍生物的包合物，含有所述包合物的药物制剂及其使用方法

    公开(公告)号：US5840714A

    公开(公告)日：1998-11-24

    申请号：US602729

    申请日：1996-02-20

    申请人： Janko Zmitek ,  Katarina Verhnjak ,  Darja Fercej-Temeljotov ,  Mateja Kovacic ,  Anton Lavric ,  Breda Bole-Vunduk

    发明人： Janko Zmitek ,  Katarina Verhnjak ,  Darja Fercej-Temeljotov ,  Mateja Kovacic ,  Anton Lavric ,  Breda Bole-Vunduk

    IPC分类号： A61K9/00 ,  A61K31/165 ,  A61K47/48 ,  C07C51/00 ,  C07C57/00 ,  C07C259/06 ,  A61K47/40 ,  C07H21/00

    CPC分类号： B82Y5/00 ,  A61K31/165 ,  A61K47/48969 ,  C07C259/06 ,  Y10S514/965

    摘要： Inclusion Complexes of Racemic Ibuproxam and of Optically Active Ibuproxam with Cyclodextrin Derivatives, Process for the Preparation Thereof, Pharmaceutical Preparations Containing these Inclusion Complexes or Containing Optically Active S-(+)-Ibuproxam, and Use Thereof There are disclosed novel inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone. Further a process for preparing S-(+)-ibuproxam and inclusion complexes of racemic ibuproxam and of optically active S-(+)-ibuproxam with hydrophilic and hydrophobic derivatives of .beta.-cyclodextrin and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, is disclosed. Disclosed are also pharmaceutical compositions containing these inclusion complexes or optically active S-(+)-ibuproxam. Optically active S-(+)-ibuproxam and novel inclusion complexes of racemic ibuproxam and of optically active ibuproxam with cyclodextrin derivatives and, in the case of optically active S-(+)-ibuproxam, also with .beta.-cyclodextrin alone, are better soluble in water and have improved biopharmaceutical properties such as lesser toxicity, better antiinflammatory action and non-irritation of the gastric mucous membrane.

    摘要翻译： PCT No.PCT / SI94 / 00015 Sec。 371日期1996年2月20日 102（e）日期1996年2月20日PCT 1994年9月6日PCT PCT。 第WO95 / 07076号公报 日期1995年3月16日包含外消旋布洛康和光学活性布洛克星与环糊精衍生物的复合物，其制备方法，含有这些包合配合物或含有光学活性的S - （+） - 布洛克星姆的药物制剂及其用途已经公开了新颖的 外消旋布洛克星和光学活性的S - （+） - 布洛克星与亲水和疏水性环糊精衍生物的包合物，以及在光学活性的S - （+） - 布洛克星）的情况下，也仅与β-环糊精一起使用。 此外，制备S - （+） - 布洛克星和外消旋布洛克星与光学活性S - （+） - 布洛克星与β-环糊精的亲水和疏水衍生物的包合物的方法，在光学活性S - （+ ） - 吡罗昔康，也是单独使用β-环糊精。 还公开了含有这些包合物或光学活性的S - （+） - 布洛康的药物组合物。 光学活性的S - （+） - 布洛克星和外消旋布洛克星与光学活性布洛克星与环糊精衍生物的新型包合物，以及光学活性的S - （+） - 布洛克星，单独使用β-环糊精的情况较好 并具有改善的生物药物性质，如毒性较小，抗炎作用更好，胃粘膜无刺激性。