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公开(公告)号：EP1713771B1
公开(公告)日：2014-03-05
申请号：EP05700893.0
申请日：2005-01-13
发明人： RUCMAN, Rudolf
IPC分类号： C07D209/42 , A61K31/475 , A61P9/12
CPC分类号： C07D209/42
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公开(公告)号：EP1709066A1
公开(公告)日：2006-10-11
申请号：EP05700892.2
申请日：2005-01-13
发明人： RUCMAN, Rudolf
IPC分类号： C07K5/062 , C07D209/42 , A61K38/05 , A61P9/00
CPC分类号： C07K5/06026 , C07D209/42
摘要： Complexes of the ACE-inhibitor perindopril, a salt, an addition salt or a derivative thereof with cyclodextrins, polyvinylpyrrolidone or hydroxypropylcellulose, and processes for their preparation are described.
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3.发明授权A PROCESS FOR THE PREPARATION OF PERINDOPRIL USING TETRAMETHYLURONIUM SALTS AS COUPLING REAGENTS 有权用于生产培哚普利使用TETRAMETHYLURONIUMSALZEN作为偶联剂
公开(公告)号：EP1628995B1
公开(公告)日：2007-06-27
申请号：EP04731809.2
申请日：2004-05-07
发明人： RUCMAN, Rudolf
IPC分类号： C07K1/10 , C07K5/02 , C07K5/06 , C07D209/42 , C07D249/18 , C07D471/04 , C07C275/70
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.
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公开(公告)号：EP1581219A1
公开(公告)日：2005-10-05
申请号：EP03781272.4
申请日：2003-12-11
发明人： KRISCH, Igor , ZIVIN, Marko , MILIVOJEVIC, Natasa , RUCMAN, Rudolf , BOLE, Breda , URLEB, Uros
IPC分类号： A61K31/435 , 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-propynyl)-6-methyl8ß-aminomethylergoline 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 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.
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公开(公告)号：EP1581219B1
公开(公告)日：2008-12-31
申请号：EP03781272.4
申请日：2003-12-11
发明人： KRISCH, Igor , ZIVIN, Marko , MILIVOJEVIC, Natasa , RUCMAN, Rudolf , BOLE, Breda , URLEB, Uros
IPC分类号： A61K31/435 , 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-propynyl)-6-methyl8ß-aminomethylergoline 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 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.
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公开(公告)号：EP1709066B1
公开(公告)日：2008-08-27
申请号：EP05700892.2
申请日：2005-01-13
发明人： RUCMAN, Rudolf
IPC分类号： C07K5/062 , C07D209/42 , A61K38/05 , A61P9/00
CPC分类号： C07K5/06026 , C07D209/42
摘要： Complexes of the ACE-inhibitor perindopril, a salt, an addition salt or a derivative thereof with cyclodextrins, polyvinylpyrrolidone or hydroxypropylcellulose, and processes for their preparation are described.
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公开(公告)号：EP1713771A1
公开(公告)日：2006-10-25
申请号：EP05700893.0
申请日：2005-01-13
发明人： RUCMAN, Rudolf
IPC分类号： C07D209/42 , A61K31/475 , A61P9/12
CPC分类号： C07D209/42
摘要： The present invention relates to the process for a preparation of ACE inhibitor perindopril starting from the stereospecific amino acid N-[(S)-carbethoxy-1-butyl](S)-alanine, which is protected by trimethylsilyl group and converted to reactive acid chloride using thionylchloride or its complex with 1-H-benzotriazole (1:1), which reacts with (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid with a protected carboxyl group. This invention relates also to a new crystalline form of perindopril and to a new amorphous form of perindopril.
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8.发明公开A PROCESS FOR THE PREPARATION OF PERINDOPRIL USING TETRAMETHYLURONIUM SALTS AS COUPLING REAGENTS 有权用于生产培哚普利使用TETRAMETHYLURONIUMSALZEN作为偶联剂
公开(公告)号：EP1628995A1
公开(公告)日：2006-03-01
申请号：EP04731809.2
申请日：2004-05-07
发明人： RUCMAN, Rudolf
IPC分类号： C07K1/10 , C07K5/02 , C07K5/06 , C07D209/42 , C07D249/18 , C07D471/04 , C07C275/70
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.
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