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1. 发明授权

US06365747B1 Method for the preparation of citalopram 有权
标题翻译：西酞普兰制备方法
公开(公告)号：US06365747B1
公开(公告)日：2002-04-02
申请号：US09830109
申请日：2001-06-01
申请人： Leone Dall'Asta , Umberto Casazza , Hans Petersen
发明人： Leone Dall'Asta , Umberto Casazza , Hans Petersen
IPC分类号： C07D30787
CPC分类号： C07D307/87 , C07D263/14 , C07D413/04
摘要： The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising treatment of a compound of formula (IV), wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring, with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring, or treatment in presence of a radical initiator, to form citalopram. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.
摘要翻译：本发明涉及一种制备西酞普兰或其任何对映异构体及其酸加成盐的方法，包括处理式（IV）化合物，其中X为O或S; R 1 -R 2各自独立地选自氢和C 1-6烷基，或者R 1和R 2一起形成C 2-5亚烷基链，从而形成螺环; R3选自氢和C 1-6烷基，因此R4选自氢，C 1-6烷基，羧基或前体基，或者R 3和R 4一起形成C 2-5亚烷基链，从而形成螺环，用脱水剂或者其中X是S，噻唑啉环的热裂解，或在自由基引发剂的存在下进行处理以形成西酞普兰。本发明还涉及用于制备西酞普兰的新方法的中间体以及根据新方法制备的西酞普兰。

2. 发明申请

US20110065938A1 METHOD FOR THE PREPARATION OF ESCITALOPRAM 审中-公开
标题翻译：用于制备ESCITALOPRAM的方法
公开(公告)号：US20110065938A1
公开(公告)日：2011-03-17
申请号：US12781048
申请日：2010-05-17
申请人： Michael B. Sommer , Ole Nielsen , Hans Petersen , Haleh Ahmadian , Henrik Pedersen , Peter Brosen , Fiona Geiser , James Lee , Geoffrey Cox , Olivier Dapremont , Christina Suteu , Sebastian P. Assenza , Shankar Hariharan , Usha Nair
发明人： Michael B. Sommer , Ole Nielsen , Hans Petersen , Haleh Ahmadian , Henrik Pedersen , Peter Brosen , Fiona Geiser , James Lee , Geoffrey Cox , Olivier Dapremont , Christina Suteu , Sebastian P. Assenza , Shankar Hariharan , Usha Nair
IPC分类号： C07D307/87 , C07C215/32
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 Chiralpak™ AD or Chiralcel™ OD. Novel chiral intermediates for the synthesis of Escitalopram made by said method are also provided.
摘要翻译：提供了一种制备依他普仑的新方法。该方法包括使用手性固定相如Chiralpak TM AD或Chiralcel TM OD，对西酞普兰对映异构体或西酞普兰生产中的中间体进行色谱分离。还提供了通过所述方法制备的用于合成依他普仑的新型手性中间体。

3. 发明授权

US07834201B2 Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
标题翻译：依他普仑和包含依他普仑碱的分散片的结晶基
公开(公告)号：US07834201B2
公开(公告)日：2010-11-16
申请号：US11425522
申请日：2006-06-21
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Harold Rock , Helle Eliasen , Ken Liljegren
IPC分类号： C07D307/87
CPC分类号： C07D307/81
摘要： The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.
摘要翻译：本发明涉及众所周知的抗抑郁药物依他普仑S-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃甲腈的结晶碱，所述制剂为碱，使用碱，草酸盐的纯化盐的制备方法，通过所述方法获得的盐和含有这些盐的制剂的方法，以及制备纯化的依他普仑游离碱或依他普仑的盐的方法，例如草酸盐，使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。最后，本发明涉及硬度至少为22N，口服崩解时间小于120秒的可分散片剂，其包含吸附在水溶性填料上的活性药物成分，其中活性药物成分的熔点为 40-100℃的范围，以及制造这种可分散片剂的方法。

4. 发明申请

US20060229459A1 CRYSTALLINE BASE OF CITALOPRAM 审中-公开
标题翻译： CITALOPRAM的晶体碱基
公开(公告)号：US20060229459A1
公开(公告)日：2006-10-12
申请号：US11425308
申请日：2006-06-20
申请人： Hans Petersen , Klaus Bogeso , Per Holm
发明人： Hans Petersen , Klaus Bogeso , Per Holm
IPC分类号： C07D307/02
CPC分类号： C07D307/81 , H01M8/04156 , H01M8/04171 , H01M8/04186 , H01M8/1009 , H01M8/1011 , H01M8/241 , H01M8/2455 , H01M8/246 , Y02E60/523
摘要： The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.
摘要翻译：本发明涉及众所周知的抗抑郁药物西酞普兰，1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，所述碱的制剂，制备西酞普兰纯化盐的方法，例如使用碱的氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。

5. 发明申请

US20050165244A1 Crystalline base of citalopram 审中-公开
标题翻译：西酞普兰的结晶基
公开(公告)号：US20050165244A1
公开(公告)日：2005-07-28
申请号：US11090337
申请日：2005-03-24
申请人： Hans Petersen , Klaus Bogeso , Per Holm
发明人： Hans Petersen , Klaus Bogeso , Per Holm
IPC分类号： C07D307/87 , A61J3/10 , A61K9/20 , A61K31/00 , A61K31/34 , A61K31/343 , A61P25/00 , A61P25/24 , C07C209/86 , C07C253/14 , C07D20060101 , C07D307/84
CPC分类号： C07D307/87
摘要： The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-dimethylanino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.
摘要翻译：本发明涉及公知的抗抑郁药物西酞普兰，1- [3-二甲基氨基丙基]丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈的结晶碱，所述碱的配方，制备西酞普兰纯化盐的方法，例如使用碱的氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂。

6. 发明申请

US20050137255A1 Crystalline escitalopram hydrobromide and methods for preparing the same 审中-公开
标题翻译：结晶的依依泊溴铵氢溴酸盐及其制备方法
公开(公告)号：US20050137255A1
公开(公告)日：2005-06-23
申请号：US11025532
申请日：2004-12-29
申请人： Hans Petersen , Peter Ellegaard , Lawrence Martel , Robert Dancer
发明人： Hans Petersen , Peter Ellegaard , Lawrence Martel , Robert Dancer
IPC分类号： A61K31/343 , C07D307/87 , C07D307/78
CPC分类号： C07D307/87 , A61K31/343
摘要： The present invention provides crystalline escitalopram hydrobromide ((S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzo-furan carbonitrile hydrobromide), and a novel crystalline form of escitalopram hydrobromide referred to herein as Form I. Form I is stable, water soluble, and not hygroscopic at a relative humidity less than 70%.
摘要翻译：本发明提供结晶的依他普仑氢溴酸盐（（S）-1- [3-（二甲基氨基）丙基] -1-（4-氟苯基）-1,3-二氢-5-异苯并呋喃腈氢溴酸盐）本文称为形式I的依他普仑氢溴酸盐的形式。在相对湿度小于70％时，I型是稳定的，水溶性的，并且不吸湿。

7. 发明申请

US20050020670A1 Stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran 审中-公开
标题翻译： 5-取代的1-（4-氟苯基）-1,3-二氢异苯并呋喃的逐步烷基化
公开(公告)号：US20050020670A1
公开(公告)日：2005-01-27
申请号：US10917667
申请日：2004-08-13
申请人： Hans Petersen , Haleh Ahmadian
发明人： Hans Petersen , Haleh Ahmadian
IPC分类号： A61K31/343 , A61P9/10 , A61P25/24 , A61P25/28 , A61P43/00 , C07D20060101 , C07D307/87 , C07D307/78
CPC分类号： C07D307/87
摘要： Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.
摘要翻译：公开了通过5-取代的1-（4-氟苯基）-1,3-二氢异苯并呋喃的逐步烷基化制备西酞普兰的方法。

8. 发明授权

US06762308B2 Method for the preparation of citalopram 失效
标题翻译：西酞普兰制备方法
公开(公告)号：US06762308B2
公开(公告)日：2004-07-13
申请号：US10237145
申请日：2002-09-05
申请人： Hans Petersen
发明人： Hans Petersen
IPC分类号： C07D30787
CPC分类号： C07D307/87
摘要： The present invention relates to a method for the preparation of citalopram by alkylation of a 1-(4-fluorophenyl)-1,3-dihydroisobenzofurane derivative.
摘要翻译：本发明涉及通过1-（4-氟苯基）-1,3-二氢异苯并呋喃衍生物的烷基化制备西酞普兰的方法。

9. 发明授权

US06717000B2 Method for the preparation of citalopram 失效
标题翻译：西酞普兰制备方法
公开(公告)号：US06717000B2
公开(公告)日：2004-04-06
申请号：US10238843
申请日：2002-09-09
申请人： Hans Petersen
发明人： Hans Petersen
IPC分类号： C07D30778
CPC分类号： C07D307/87
摘要： The present invention relates to a method for the preparation of citalopram comprising reduction of a compound of formula wherein X is a cyano group or a group which can be converted to a cyano group, and if X is not a cyano group followed by conversion of X to a cyano group.
摘要翻译：本发明涉及一种制备西酞普兰的方法，包括还原糠醛的化合物X是氰基或可以转化成氰基的基团，如果X不是氰基，随后将X转化为氰基。

10. 发明授权

US06229026B1 Method for the preparation of citalopram 有权
标题翻译：西酞普兰制备方法
公开(公告)号：US06229026B1
公开(公告)日：2001-05-08
申请号：US09479832
申请日：2000-01-07
申请人： Hans Petersen
发明人： Hans Petersen
IPC分类号： C07D30783
CPC分类号： C07D307/87 , C07C229/38 , C07C235/84 , C07C237/30
摘要： A method for the preparation of citalopram comprising the steps of reacting a compound of Formula (IV) wherein R1 is C1-6 alkyl and X is O or NH, successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, respectively, effecting ring-closure of the resulting compound of Formula (V) wherein R1 and X are as defined above, and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.
摘要翻译：一种制备西酞普兰的方法，包括以下步骤：使R 1为C 1-6烷基且X为O或NH的式（Ⅳ）化合物依次与4-卤代 - 氟苯基的格氏试剂和3位的格利雅试剂 - 卤素-N，N-二甲基丙胺，使所得到的式（Ⅴ）化合物闭环，其中R 1和X如上定义，并将所得1,3-二氢异苯并呋喃化合物转化为相应的5-氰基衍生物，即西酞普兰。

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