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公开(公告)号：EP1971585A1
公开(公告)日：2008-09-24
申请号：EP06842191.6
申请日：2006-12-08
发明人： TRINKA, Péter , REITER, József , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ, Donáth, Györgyi , NAGY, Kálmán , PONGÓ, László , MEZEI, Tibor
IPC分类号： C07D295/088
CPC分类号： C07D295/088
摘要： The present invention relates to a process for the preparation of {2-[4-(α-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide of the Formula (I) and enantiomers thereof. The compound of the Formula (I) or enantiomers thereof are important pharmaceutical intermediates suitable for direct transformation into non-sedating antihistamine type pharmaceutical active ingredients cetirizine and levocetirizine.
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公开(公告)号：EP1971585B1
公开(公告)日：2011-03-09
申请号：EP06842191.6
申请日：2006-12-08
发明人： TRINKA, Péter , REITER, József , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ, Donáth, Györgyi , NAGY, Kálmán , PONGÓ, László , MEZEI, Tibor
IPC分类号： C07D295/088
CPC分类号： C07D295/088
摘要： The present invention relates to a process for the preparation of {2-[4-(α-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide of the Formula (I) and enantiomers thereof. The compound of the Formula (I) or enantiomers thereof are important pharmaceutical intermediates suitable for direct transformation into non-sedating antihistamine type pharmaceutical active ingredients cetirizine and levocetirizine.
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公开(公告)号：EP1963335A2
公开(公告)日：2008-09-03
申请号：EP06808805.3
申请日：2006-11-10
发明人： KOVANYINE LAX, Györgyi , NEMETH, Gábor , KRASZNAI, György , MESTERHAZY, Norbert , NAGY, Kálmán , VERECZKEYNE DONATH, Györgyi , SZENT-KIRALLYI, Zsuzsanna
IPC分类号： C07D495/04 , A61K31/5513
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of 2 -methyl-4 - (4-methylpiperazin- 1-yl) - 10H- thieno- [2 , 3 -b] [1 , 5] benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3- b] [1/5] benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1, 3-dimethyl-2- imidazolidinone . The invention also encompasses new 2-methyl-4- (4-methylpiperazin-l-yl) -10H-thieno [2,3- b] [1,5] benzodiazepine dihydrochloride trihydrate of the formula (IB) , the preparation thereof and pharmaceutical compositions comprising said new compound.
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4.发明授权OPTICALLY ACTIVE CARBAMATES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS PHARMACEUTICAL INTERMEDIATES 有权光学活性氨基甲酸酯，方法及其及其作为医药中间体
公开(公告)号：EP1963296B1
公开(公告)日：2012-02-15
申请号：EP06831510.0
申请日：2006-12-08
发明人： MEZEI, Tibor , MOLNÁR, Enikö , TRINKA, Péter , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ DONÁTH, Györgyi , NAGY, Kálmán , PONGÓ, László , LUKÁCS, Gyula , PORCS-MAKKAY, Márta , ÉVINGER, Zsuzsanna , SIMIG, Gyula
IPC分类号： C07D295/06 , C07D295/18
CPC分类号： C07D295/073 , C07D295/185
摘要： The present invention is related to l-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
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5.发明公开OPTICALLY ACTIVE CARBAMATES, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS PHARMACEUTICAL INTERMEDIATES 有权光学活性氨基甲酸酯，方法及其及其作为医药中间体
公开(公告)号：EP1963296A2
公开(公告)日：2008-09-03
申请号：EP06831510.0
申请日：2006-12-08
发明人： MEZEI, Tibor , MOLNÁR, Enikö , TRINKA, Péter , BARTHA, Ferenc , KATONA, Zoltán , VERECZKEYNÉ DONÁTH, Györgyi , NAGY, Kálmán , PONGÓ, László , LUKÁCS, Gyula , PORCS-MAKKAY, Márta , ÉVINGER, Zsuzsanna , SIMIG, Gyula
IPC分类号： C07D295/06 , C07D295/18
CPC分类号： C07D295/073 , C07D295/185
摘要： The present invention is related to l-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. l-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.
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公开(公告)号：EP1963335B1
公开(公告)日：2011-05-04
申请号：EP06808805.3
申请日：2006-11-10
发明人： KOVANYINE LAX, Györgyi , NEMETH, Gábor , KRASZNAI, György , MESTERHAZY, Norbert , NAGY, Kálmán , VERECZKEYNE DONATH, Györgyi , SZENT-KIRALLYI, Zsuzsanna
IPC分类号： C07D495/04 , A61K31/5513
CPC分类号： C07D495/04
摘要： The invention relates to a process for the preparation of 2 -methyl-4 - (4-methylpiperazin- 1-yl) - 10H- thieno- [2 , 3 -b] [1 , 5] benzodiazepine (olanzapine) of the formula (I) by reacting 4-amino-2-methyl-10H-thieno [2,3- b] [1/5] benzodiazepine hydrochloride of the formula (II) with N-methylpiperazine in an organic solvent, which comprises carrying out the reaction in the mixture of toluene and 1, 3-dimethyl-2- imidazolidinone . The invention also encompasses new 2-methyl-4- (4-methylpiperazin-l-yl) -10H-thieno [2,3- b] [1,5] benzodiazepine dihydrochloride trihydrate of the formula (IB) , the preparation thereof and pharmaceutical compositions comprising said new compound.
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