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1. 发明授权

US07632843B2 Treatment of psychostimulant addiction 失效
标题翻译：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。

2. 发明申请

US20060014775A1 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.

3. 发明授权

US5288724A Ergoline derivatives of 2-propinylamine, a process for the manufacture thereof and the use thereof for medicaments 失效
标题翻译： 2-丙烯胺的二氢喹啉衍生物，其制备方法及其药物用途
公开(公告)号：US5288724A
公开(公告)日：1994-02-22
申请号：US901983
申请日：1992-06-22
申请人： Rudolf Rucman , Breda Bole-Vunduk , Magdalena Ocvirk , Bogomila Lavric , Igor Krisch
发明人： Rudolf Rucman , Breda Bole-Vunduk , Magdalena Ocvirk , Bogomila Lavric , Igor Krisch
IPC分类号： A61K31/48 , A61P3/04 , A61P9/12 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , C07D457/02 , C07D457/06 , A61K31/44 , C07D457/00
CPC分类号： C07D457/06 , C07D457/02
摘要： There are disclosed novel ergoline derivatives of 2-propinylamine of the general formula I ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group,X represents a hydrogen or a halogen atom,Z represents a carbonyl or methylene group andC.sub.9 C.sub.10 represents a single or a double bond, diastereomeric forms, racemates and acid addition salts thereof.There are also described a process for the manufacture of the compounds of the general formula I and a pharmaceutical composition containing the same.The compounds of the general formula I can be used in the pharmaceutical industry as active substances for the manufacture of medicaments used in the treatment of hypertension, migraine, anxiety states, depressions, obesity etc.
摘要翻译：公开了通式I的2-丙烯胺的新的麦角灵衍生物，其中R1，R2和R3独立地表示氢原子或直链或支链C1-C6烷基，X表示氢或卤素原子，Z表示羰基或亚甲基，C 9 C10表示单键或双键，非对映体形式，外消旋体及其酸加成盐。还描述了制备通式I化合物的方法和含有该化合物的药物组合物。通式I的化合物可用于制药工业中用作制备用于治疗高血压，偏头痛，焦虑状态，沮丧，肥胖等的药物的活性物质。

4. 发明授权

US5480885A Ergoline derivatives of 1-propinylamine, a process for the manufacture thereof and the use thereof for medicaments 失效
标题翻译： 2-丙烯胺的二氢喹啉衍生物，其制备方法及其药物用途
公开(公告)号：US5480885A
公开(公告)日：1996-01-02
申请号：US160271
申请日：1993-12-02
申请人： Rudolf Rucman , Breda Bole-Vunduk , Magdalena Ocvirk , Bogomila Lavric , Igor Krisch
发明人： Rudolf Rucman , Breda Bole-Vunduk , Magdalena Ocvirk , Bogomila Lavric , Igor Krisch
IPC分类号： C07D457/02 , C07D457/06 , A61K31/44
CPC分类号： C07D457/06 , C07D457/02
摘要： A method of treating psychosis including administering an antipsychotically effective amount of an ergolinyl derivative of 2-propinylamine of the formula I ##STR1## wherein, R.sub.1, R.sub.2, and R.sub.3 independently represent a hydrogen atom or a straight-chain or branched-chain C.sub.1 -C.sub.6 alkyl group, X represents a hydrogen or a halogen atom, Z represents a carbonyl or methylene group, and C.sub.9 - - - -C.sub.10 represents a single or a double, diastereomeric forms, racemates and acid addition salts thereof.
摘要翻译：一种治疗精神病的方法，包括施用抗精神病药有效量的式I的2-丙烯胺的麦角酰衍生物其中，R1，R2和R3独立地表示氢原子或直链或支链C1 C 6烷基，X表示氢或卤素原子，Z表示羰基或亚甲基，C 9 - -C 10表示单或双，非对映体形式，外消旋体及其酸加成盐。

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