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    Treatment of psychostimulant addiction
    5.
    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。

    Novel Process
    7.
    发明申请
    Novel Process 审中-公开
    小说流程

    公开(公告)号：US20090234139A1

    公开(公告)日：2009-09-17

    申请号：US11992212

    申请日：2006-09-19

    申请人： Lovro Selic ,  Gregor Vilfan ,  Uros Urleb

    发明人： Lovro Selic ,  Gregor Vilfan ,  Uros Urleb

    IPC分类号： C07D205/04

    CPC分类号： C07F7/1892 ,  Y02P20/55

    摘要： A novel process for the preparation of 1′-hydroxy-2′-substituted cyclohexyl azetidin-2-one compound of formula 2, which is important intermediate in the synthesis of trinems, is described by epoxide ring opening of (3S,4R)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-4-[(1′R,2′S,3′R)-1′,2′-epoxycyclohexan-3′-yl]azetidin-2-one of formula 1 with the nucleophile compound of formula RYH, where nucleophile may act as solvent itself if the nucleophile is in the liquid form, in a suitable solvent and in the presence of a suitable catalyst from the group of salt of trifluoromethane sulfonic acid, preferably ytterbium (III) trifluoromethanesulfonate, stannous (II) trifluoromethanesulfonate or dysprosium (III) trifluoromethanesulfonate, under a) ultrasonic irradiation or b) under microwave irradiation of the reaction mixture following by isolation and purification of the desired compound. A variant of the novel process describes ring epoxide opening of the starting compound of formula 1 with the compound of formula NH4X in a suitable solvent under a) microwave irradiation or b) without microwave irradiation to obtain the desired compound of formula 2. Instead of compound of formula 1 a compound of formula 6 may be used as starting compound where any other suitable hydroxy protecting group known in the art may be used in the formula of the starting compound.

    摘要翻译： （3S，4R） - 环糊精的环氧化物开环描述了制备式（2）的1'-羟基-2'-取代的环己基氮杂环丁烷-2-酮化合物的新方法，其是三聚氰胺合成中的重要中间体。 3 - [（1R）-1-（叔丁基二甲基甲硅烷氧基）乙基] -4 - [（1'R，2'S，3'R）-1'，2'-环氧环己烷-3'-基]氮杂环丁-2-酮 式1与式RYH的亲核化合物反应，其中如果亲核试剂为液体形式，亲核试剂可以在合适的溶剂中和在三氟甲烷磺酸盐的合适的催化剂存在下，作为溶剂本身，优选 （a）三氟甲磺酸镱（II），三氟甲磺酸亚锡（II），三氟甲磺酸镝（III），或b）在微波照射反应混合物之后，分离和纯化所需化合物。 新方法的变体描述了式Ⅰ的起始化合物与式NH 4 X的化合物在合适的溶剂中在a）微波照射下或b）没有微波照射得到所需的式2化合物的环氧化物开环。代替化合物 式1的化合物可以用作起始化合物，其中本领域已知的任何其它合适的羟基保护基可以用于起始化合物的式中。

    Crystalline form of omeprazole
    8.
    发明授权
    Crystalline form of omeprazole 有权
    奥美拉唑的结晶形式

    公开(公告)号：US07553856B2

    公开(公告)日：2009-06-30

    申请号：US11248461

    申请日：2005-10-12

    申请人： Natasa H Milac ,  Anton Copar ,  Barbara Podobnik ,  Andreja C Belcic ,  Alenka Kosak ,  Brina Ornik ,  Uros Urleb

    发明人： Natasa H Milac ,  Anton Copar ,  Barbara Podobnik ,  Andreja C Belcic ,  Alenka Kosak ,  Brina Ornik ,  Uros Urleb

    IPC分类号： A61K31/4439

    CPC分类号： C07D401/12

    摘要： A novel crystalline form of the substrate known under the chemical name 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfiny]-1H-benzimidazole, and having the generic name omeprazole, hereinafter referred to as omeprozole form C, is disclosed. Further, a process for the preparation of omeprazole form C, a pharmaceutical formulation containing omeprazole form C in admixture with pharmaceutically acceptable excipients and the use of omeprazole form C for treatment of gastrointestinal disorders are disclosed.

    摘要翻译： 以化学名称为5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑的新颖的底物结晶形式，具有通用名奥美拉唑 ，以下称为奥美曲唑C型。 此外，公开了制备奥美拉唑C型的方法，一种含有与药学上可接受的赋形剂混合的奥美拉唑C形式的药物制剂以及奥美拉唑C型用于治疗胃肠道疾病的用途。

    Use of Aza-Phenylalanine Compounds For Treating Cardiac Arrhythmia
    10.
    发明申请
    Use of Aza-Phenylalanine Compounds For Treating Cardiac Arrhythmia 审中-公开
    用于治疗心律失常的氮杂苯丙氨酸化合物

    公开(公告)号：US20080306047A1

    公开(公告)日：2008-12-11

    申请号：US12093974

    申请日：2006-11-16

    申请人： Manica Cerne ,  Uros Urleb ,  Metka V. Budihna ,  Gorazd Drevensek ,  Luka Peternel

    发明人： Manica Cerne ,  Uros Urleb ,  Metka V. Budihna ,  Gorazd Drevensek ,  Luka Peternel

    IPC分类号： A61K31/55 ,  A61P9/00

    CPC分类号： A61K31/55

    摘要： The present invention relates to the use of certain aza-phenylalanine compounds of formula (I) wherein R1 denotes amino, alkylamino, dialkylamino, amidino, alkylamidino, N-hydroxyamidino, or N-alkoxyamidino, Y denotes sulfonyl or carbonyl and R2 and R4 independently represent various organic residues, in the treatment or prevention of cardiac arrhythmia and/or in treatment or prevention of diseases in association with ischemic heart conditions.

    摘要翻译： 本发明涉及式（I）的某些氮杂 - 苯丙氨酸化合物的用途，其中R1表示氨基，烷基氨基，二烷基氨基，脒基，烷基脒基，N-羟基脒基或N-烷氧基脒基，Y表示磺酰基或羰基，R2和R4独立地 代表各种有机残留物，用于治疗或预防心律失常和/或治疗或预防与缺血性心脏病有关的疾病。