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1. 发明授权

EP1412341B1 PROCESS FOR THE PREPARATION OF RACEMIC CITALOPRAM AND/OR S- OR R-CITALOPRAM BY SEPARATION OF A MIXTURE OF R- AND S-CITALOPRAM 有权
标题翻译：通过分离R-和S-CITALOPRAM的混合物来制备RACEMIC CITALOPRAM和/或S-R或C-RING的方法
公开(公告)号：EP1412341B1
公开(公告)日：2004-12-08
申请号：EP02742848.1
申请日：2002-06-25
申请人： H. Lundbeck A/S
发明人： HUMBLE, Rikke, Eva , CHRISTENSEN, Troels, Volsgaard , ROCK, Michael, Harold , NIELSEN, Ole , PETERSEN, Hans , DANCER, Robert
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The invention relates to a process for the preparation of racemic citalopram free base or an acid addition salt thereof and/or R- or S-citalopram as the free base or an acid addition salt thereof by separation of a mixture of R- and S-citalopram with more than 50% of one of the enantiomers into a fraction consisting of racemic citalopram and/or a fraction of S-citalopram or R-citalopram characterized in that i) citalopram is precipitated from a solvent as the free base or as an acid addition salt thereof; ii) the precipitate formed is separated from the mother liquor; iia) if the precipitate is crystalline it is optionally recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iib) if the precipitate is not crystalline, steps i) and ii) are optionally repeated until a crystalline precipitate is obtained and the crystalline precipitate is recrystallised one or more times to form racemic citalopram, and then optionally converted into an acid addition salt thereof; iii) the mother liquor is optionally subjected to further purification and S-citalopram or R-citalopram is isolated from the mother liquor and optionally converted into an acid addition salt thereof.
摘要翻译：本发明涉及一种制备外消旋西酞普兰游离碱或其酸加成盐和/或作为游离碱或其酸加成盐的R-或S-西酞普兰的方法，其通过分离R-和S- 西酞普兰与超过50％的一种对映体进入由外消旋西酞普兰和/或一部分S-西酞普兰或R-西酞普兰组成的部分，其特征在于i）西酞普兰以游离碱或酸形式从溶剂中沉淀出来其加成盐; ii）将形成的沉淀从母液中分离出来; 如果沉淀物是结晶的，则任选重结晶一次或多次以形成外消旋西酞普兰，然后任选转化为其酸加成盐; 如果沉淀物不是结晶的，则任选重复步骤i）和ii）直至获得结晶沉淀物，并将结晶沉淀物重结晶一次或多次以形成外消旋西酞普兰，然后任选转化成其酸加成盐; iii）任选地将母液进一步纯化，从母液中分离出S-西酞普兰或R-西酞普兰，并任选转化为其酸加成盐。

2. 发明授权

EP1044202B1 1'- 4- 1- (4-FLUOROPHENYL)- 1H-INDOLE-3-YL] -1-BUTYL]-SPIRO ISOBENZOFURAN- 1(3H),4'- PIPERIDINE] HYDROHALOGENIDES 有权
标题翻译： 1-（4-（1-（4- FLUORPHENYL）-1H-吲哚-3-基）-1-丁基） - 螺（异苯并呋喃-1（3H），4'-哌啶）-HYDROHALOGENIDE
公开(公告)号：EP1044202B1
公开(公告)日：2005-02-09
申请号：EP98952580.3
申请日：1998-11-06
申请人： H. LUNDBECK A/S
发明人： MORK, Niels , LOPEZ DE DIEGO, Heidi , NIELSEN, Ole
IPC分类号： C07D491/107 , C07D401/06 , A61K31/445
CPC分类号： C07D491/10
摘要： The present invention relates to a hydrohalogenide of 1'- [4-[1- (4-fluorophenyl) -1H-indole- 3-yl]-1- butyl]- spiro[isobenzofuran- 1(3H),4'-piperidine], pharmaceutical compositions containing the acid addition salts and the use thereof for the treatment of psychic and neurological disorders.

3. 发明公开

EP1318805A2 PHARMACEUTICAL COMPOSITION CONTAINING CITALOPRAM 审中-公开
标题翻译：西酞普兰的药物组合物
公开(公告)号：EP1318805A2
公开(公告)日：2003-06-18
申请号：EP01957768.3
申请日：2001-07-30
申请人： H. LUNDBECK A/S
发明人： LILJEGREN, Ken , HOLM, Per , NIELSEN, Ole , WAGNER, Sven
IPC分类号： A61K31/343 , A61K9/14
CPC分类号： C07D307/87 , A61K9/2054 , A61K9/4866 , A61K31/343
摘要： A solid unit dosage form comprising citalopram, which is prepared by direct compression of a mixture of citalopram base or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients, or by filling of said mixture in a hard gelatine capsule. Large crystals of a pharmaceutical acceptable salt of citalopram and method for the manufacture of said large crystals.

4. 发明公开

EP1658277A1 SUCCINATE AND MALONATE SALT OF TRANS-4-(IR,3S)-6-CHLORO-3-PHENYLINDAN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND THE USE AS A MEDICAMENT 有权
标题翻译：琥珀酸盐和反式-4-（1R，3S）-6-氯-3-苯基茚满-1-基）-1,2,2-三甲基哌嗪丙二酸盐和作为药物的用途
公开(公告)号：EP1658277A1
公开(公告)日：2006-05-24
申请号：EP04762772.4
申请日：2004-08-18
申请人： H. LUNDBECK A/S
发明人： LOPEZ DE DIEGO, Heidi , NIELSEN, Ole , RINGGARD, Lone, Munch , SVANE, Henrik , DAHL, Allan, Carsten , HOWELLS, Mark , BANG-ANDERSEN, Benny , LYNGSO, Lars Ole
IPC分类号： C07D295/06 , C07C35/32 , C07C25/22 , C12P7/02 , C12P41/00 , A61K31/495 , A61P25/18
CPC分类号： C07D295/073 , C07B2200/07 , C07C17/16 , C07C25/22 , C07C29/143 , C07C35/32 , C07C2602/08 , C07D241/04 , C12P7/22 , C12P41/004 , C07C35/52
摘要： 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen succinate or hadrogen malonat, pharmaceutical compositions containing these salts and the medical use thereof, including for the treatment of schizophrenia and other psychotic disorders. Also described are methods for the preparation of 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and medical uses thereof.
摘要翻译：的化合物，4 - （（1R，3S）-6-氯-3-苯基-1-基）-2,2-二甲基哌嗪和包含该化合物和它的盐，和医药用途，包括用于治疗的盐，药物组合物精神分裂症和其它精神障碍。

5. 发明公开

EP1409472A1 METHOD FOR THE PREPARATION OF ESCITALOPRAM 审中-公开
标题翻译：用于生产艾司西酞普兰
公开(公告)号：EP1409472A1
公开(公告)日：2004-04-21
申请号：EP02750836.5
申请日：2002-07-12
申请人： H. Lundbeck A/S
发明人： BECH SOMMER, Michael , NIELSEN, Ole , PETERSEN, Hans , AHMADIAN, Haleh , PEDERSEN, Henrik , BROSEN, Peter , GEISER, Fiona , LEE, James , COX, Geoffey , DAPREMONT, Olivier , SUTEU, Christina , ASSENZA, Sebastian, P. , HARIHARAN, Shankar , NAIR, Usha
IPC分类号： C07D307/87 , C07B57/00
CPC分类号： C07C215/32 , C07D307/87
摘要： A novel method is provided for the manufacture of escitalopram. The method comprises chromatographic separation of the enantiomers of citalopram or an intermediate in the production of citalopram using a chiral stationary phase such as ChiralpakTM AD or ChiralcelTM OD. Novel chiral intermediates for the synthesis of Escitalopram made by said method are also provided.

6. 发明公开

EP1044202A1 1'- 4- 1- (4-FLUOROPHENYL)- 1H-INDOLE-3-YL] -1-BUTYL]-SPIRO ISOBENZOFURAN- 1(3H),4'- PIPERIDINE] HYDROHALOGENIDES 有权
标题翻译： 1-（4-（1-（4-氟苯基）-1H-吲哚-3-基）-1-丁基）螺（异苯并呋喃-1（3H），4'-哌啶）-HYDROHALOGENIDE
公开(公告)号：EP1044202A1
公开(公告)日：2000-10-18
申请号：EP98952580.3
申请日：1998-11-06
申请人： H. LUNDBECK A/S
发明人： MORK, Niels , LOPEZ DE DIEGO, Heidi , NIELSEN, Ole
IPC分类号： C07D491/107 , C07D401/06 , A61K31/445
CPC分类号： C07D491/10
摘要： The present invention relates to a hydrohalogenide of 1'- [4-[1- (4-fluorophenyl) -1H-indole- 3-yl]-1- butyl]- spiro[isobenzofuran- 1(3H),4'-piperidine], pharmaceutical compositions containing the acid addition salts and the use thereof for the treatment of psychic and neurological disorders.

7. 发明公开

EP0994869A1 5-(2-ETHYL-2$i(H)-TETRAZOL-5-Y1)-1-METHYL-1,2,3,6-TETRAHYDROPYRIDINE MALEATE 失效
标题翻译： 5-（2-乙基-2H-（1H） - 四唑-5-基）-1-甲基-1,2,3,6-四氢吡啶马来酸盐
公开(公告)号：EP0994869A1
公开(公告)日：2000-04-26
申请号：EP98930655.0
申请日：1998-07-01
申请人： H. LUNDBECK A/S
发明人： BECH SOMMER, Michael , NIELSEN, Ole
IPC分类号： C07D401/04 , A61K31/44
CPC分类号： C07D401/04
摘要： The present invention relates to a maleate acid addition salt of 5-(2-ethyl-2H-tetrazol-5-yl)-1-methyl-1,2,3,6-tetrahydropyridine, pharmaceutical compositions containing the acid addition salt and the use thereof for the treatment of disorders caused by a malfunction of the acetylcholine (AcCh) or muscarinic system.
摘要翻译：本发明涉及5-（2-乙基-2H-四唑-5-基）-1-甲基-1,2,3,6-四氢吡啶的马来酸加成盐，含有该酸加成盐和用于治疗由乙酰胆碱（AcCh）或毒蕈碱系统故障引起的病症。

8. 发明公开

EP3230265A1 A PROCESS FOR THE MANUFACTURE OF IDALOPIRDINE 审中-公开
标题翻译：一种制造IDALOPIRDINE的方法
公开(公告)号：EP3230265A1
公开(公告)日：2017-10-18
申请号：EP15821029.4
申请日：2015-12-10
申请人： H. Lundbeck A/S
发明人： JACOBSEN, Mikkel, Fog , NIELSEN, Ole
IPC分类号： C07D209/04 , C07D209/16
CPC分类号： C07D209/14 , C07D209/04 , C07D209/08 , C07D209/16
摘要： Disclosed herein is a process for the preparation of idalopirdine and pharmaceutically acceptable salts thereof.
摘要翻译：本文公开了制备依达戈星及其药学上可接受的盐的方法。

9. 发明授权

EP1896439B2 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
标题翻译：依他普仑晶体碱和依他普仑-BASE CONTAINING口中崩解片剂IN
公开(公告)号：EP1896439B2
公开(公告)日：2014-10-15
申请号：EP06742481.2
申请日：2006-06-22
申请人： H. Lundbeck A/S
发明人： DANCER, Robert , PETERSEN, Hans , NIELSEN, Ole , ROCK, Michael, Harold , ELIASEN, Helle , LILJEGREN, Ken
IPC分类号： C07D307/87
CPC分类号： C07D307/87 , A61K31/343

10. 发明授权

EP1658277B1 SUCCINATE AND MALONATE SALT OF TRANS-4-(IR,3S)-6-CHLORO-3-PHENYLINDAN-1-YL)-1,2,2-TRIMETHYLPIPERAZINE AND THE USE AS A MEDICAMENT 有权
标题翻译：琥珀酸盐和反式-4-（1R，3S）-6-氯-3-苯基茚满-1-基）-1,2,2-三甲基哌嗪丙二酸盐和作为药物的用途
公开(公告)号：EP1658277B1
公开(公告)日：2012-04-04
申请号：EP04762772.4
申请日：2004-08-18
申请人： H. Lundbeck A/S
发明人： LOPEZ DE DIEGO, Heidi , NIELSEN, Ole , RINGGARD, Lone, Munch , SVANE, Henrik , DAHL, Allan, Carsten , HOWELLS, Mark , BANG-ANDERSEN, Benny , LYNGSO, Lars Ole
IPC分类号： C07D241/04 , C07C17/16 , C12P7/22 , C07C25/22 , C07C35/32 , C12P41/00 , A61K31/495 , A61P25/18 , C07C29/143
CPC分类号： C07D295/073 , C07B2200/07 , C07C17/16 , C07C25/22 , C07C29/143 , C07C35/32 , C07C2602/08 , C07D241/04 , C12P7/22 , C12P41/004 , C07C35/52
摘要： 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine hydrogen succinate or hadrogen malonat, pharmaceutical compositions containing these salts and the medical use thereof, including for the treatment of schizophrenia and other psychotic disorders. Also described are methods for the preparation of 4-((1R,3S)-6-Chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and medical uses thereof.

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