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10 条记录 (耗时 0.021 秒)

    Treatment of psychostimulant addiction
    1.
    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
    2.
    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.

    Process for brominating ergot alkaloids
    6.
    发明授权
    Process for brominating ergot alkaloids 失效
    溴化麦角生物碱的工艺

    公开(公告)号：US4609731A

    公开(公告)日：1986-09-02

    申请号：US141304

    申请日：1980-04-18

    申请人： Milan Jurgec ,  Rudolf Rucman ,  Branko Stanovnik ,  Miha Tisler

    发明人： Milan Jurgec ,  Rudolf Rucman ,  Branko Stanovnik ,  Miha Tisler

    IPC分类号： C07D457/04 ,  C07D457/06 ,  C07D519/02

    CPC分类号： C07D457/06 ,  C07D457/04 ,  C07D519/02

    摘要： The present invention provides an improved process for the production of a compound of formula I ##STR1## wherein R.sub.1 is carboxyl, alkoxy(C.sub.1-5)carbonyl, amido, alkyl(C.sub.1-5)amido, di(alkyl(C.sub.1-5)amido or an amido radical of formula II ##STR2## wherein R.sub.a is alkyl(C.sub.1-4),R.sub.b is alkyl(C.sub.1-4) or benzyl, andR.sub.2 is hydrogen or alkyl(C.sub.1-4), andeitherR.sub.3 is hydrogen and R.sub.4 is hydrogen or alkoxy(C.sub.1-4)orR.sub.3 and R.sub.4 together are a single bond,characterized in that a compound of formula III ##STR3## wherein R.sub.1 to R.sub.4 are as defined above,is brominated with a bromine complex of 3-bromo-6-chloro-2-methyl-imidazo[1,2-b]pyridazine.

    摘要翻译： 本发明提供了制备式I化合物I的改进方法，其中R 1是羧基，烷氧基（C 1-5）羰基，酰氨基，烷基（C 1-5）酰氨基，二（烷基（C 1-5） ）酰氨基或式II的酰胺基其中R a是烷基（C 1-4），R b是烷基（C 1-4）或苄基，并且R 2是氢或烷基（C 1-4），并且R 3是 氢和R4是氢或烷氧基（C1-4）或R3和R4一起是单键，其特征在于其中R 1至R 4如上定义的式III化合物III与溴络合物溴化 3-溴-6-氯-2-甲基 - 咪唑并[1,2-b]哒嗪。

    Process for the removal of a silyloxy protecting group from 4-silyloxy-tetrahydro-pyran-2-ones
    7.
    发明授权
    Process for the removal of a silyloxy protecting group from 4-silyloxy-tetrahydro-pyran-2-ones 失效
    从4-甲硅烷氧基 - 四氢 - 吡喃-2-酮中除去甲硅烷氧基保护基的方法

    公开(公告)号：US06509479B1

    公开(公告)日：2003-01-21

    申请号：US09869372

    申请日：2001-09-21

    申请人： Marko Zlicar ,  Rudolf Rucman

    发明人： Marko Zlicar ,  Rudolf Rucman

    IPC分类号： C07D30930

    CPC分类号： C07D309/30 ,  Y02P20/55

    摘要： This invention relates to a novel method for the removal of a silyl protecting group from the 4-hydroxy group of tetrahydropyran-2-ones, which method is particularly suitable in the process for the preparation of simvastatin and derivatives and analogs thereof.

    摘要翻译： 本发明涉及从四氢吡喃-2-酮的4-羟基除去甲硅烷基保护基的新方法，该方法特别适用于制备辛伐他汀及其衍生物和类似物的方法。

    Process for the preparation of perindopril using tetramethyluronium salts as coupling reagents
    8.
    发明申请
    Process for the preparation of perindopril using tetramethyluronium salts as coupling reagents 审中-公开
    使用四甲基脲盐作为偶联剂制备培哚普利的方法

    公开(公告)号：US20070173637A1

    公开(公告)日：2007-07-26

    申请号：US10555848

    申请日：2004-05-07

    申请人： Rudolf Rucman

    发明人： Rudolf Rucman

    IPC分类号： C07K5/10 ,  C07D209/42

    CPC分类号： C07K5/06026 ,  C07D209/42 ,  Y02P20/55

    摘要： The present invention relates to the process for the preparation of the ACE inhibitor perindopril starting from stereospecific amino acid N-/1-(S)-ethoxy-carbonyl-butyl/-(S)-alanine which is activated with tetramethyluronium salts in the presence of tertiary organic base, following the reaction with (2S,3aS,7aS)-octahydroindolo-2-carboxylic acid or an ester thereof, and after completing the reaction followed by elimination of protective group by hydrogenation, phase transfer hydrogenation or extraction.

    摘要翻译： 本发明涉及从立体特异性氨基酸N- / 1-（S） - 乙氧基 - 羰基 - 丁基 - （S） - 丙氨酸制备ACE抑制剂培哚普利的方法，该方法在存在下用四甲基脲鎓盐活化 （2S，3aS，7aS） - 八氢吲哚-2-羧酸或其酯反应后，在完成反应之后，通过氢化，相转移氢化或萃取除去保护基。

    Process for the preparation of N-substituted esters of 9,10-dihydrolysergicacids
    10.
    发明授权
    Process for the preparation of N-substituted esters of 9,10-dihydrolysergicacids 失效
    制备9,10-二氢赖氨酸的N-取代酯的方法

    公开(公告)号：US4230859A

    公开(公告)日：1980-10-28

    申请号：US922692

    申请日：1978-07-07

    申请人： Rudolf Rucman

    发明人： Rudolf Rucman

    IPC分类号： C07D457/02 ,  A61K31/48 ,  B01J31/00 ,  C07B61/00 ,  C07D457/04

    CPC分类号： C07D457/04

    摘要： A process for the preparation of N-substituted esters of 9,10-dihydrolysergic acids of the formula: ##STR1## wherein R.sub.1 is an alkyl group of 1-5 carbon atoms, an alkenyl group of 2-5 carbon atoms or a cycloalkyl group of 3-5 carbon atoms,R.sub.2 is hydrogen or an alkoxy group of 1-3 carbon atoms andX' is hydrogen or halogen,characterized in that esterified 9,10-dihydrolysergic acids of the formula: ##STR2## wherein R is hydrogen or a hydrolyzable organic group,X' is hydrogen or halogen, andR.sub.2 has the meaning as stated above,are reacted with a compound of the formula:R.sub.1 Y (III)whereinR.sub.1 has the meaning as stated above,Y is halogen or sulphate,in the presence of a catalyst for phase transition in the presence of aqueous alkali medium in an inert organic solvent immiscible with water, and certain novel esters obtained thereby.

    摘要翻译： 制备下式的9,10-二氢赖氨酸的N-取代酯的方法：其中R1是1-5个碳原子的烷基，2-5个碳原子的链烯基或 3-5个碳原子的环烷基，R2是氢或1-3个碳原子的烷氧基，X'是氢或卤素，其特征在于下式的酯化的9,10-二氢赖氨酸：（II ）其中R是氢或可水解的有机基团，X'是氢或卤素，并且R 2具有如上所述的含义，与下式的化合物反应：其中R 1具有如上所述的含义，Y 在碱性水溶液存在下，在与水不混溶的惰性有机溶剂的存在下，在存在催化剂的情况下，是卤素或硫酸盐，以及由此得到的某些新的酯。