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1. 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。

2. 发明申请

US20110046218A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 审中-公开
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20110046218A1
公开(公告)日：2011-02-24
申请号：US12916750
申请日：2010-11-01
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： A61K31/343 , C07D307/87 , A61P25/24
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。

3. 发明授权

US07723533B2 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：US07723533B2
公开(公告)日：2010-05-25
申请号：US12046999
申请日：2008-03-12
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-isobenzo-furancarbonitrile, 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-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。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

US20080161388A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20080161388A1
公开(公告)日：2008-07-03
申请号：US12046984
申请日：2008-03-12
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： A61K31/343 , 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-isobenzo-furancarbonitrile, 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-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。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。

5. 发明授权

US07560576B2 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：US07560576B2
公开(公告)日：2009-07-14
申请号：US12046984
申请日：2008-03-12
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： C07D307/00 , A61K31/34
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-isobenzo-furancarbonitrile, 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-异苯并呋喃腈的结晶碱，其制剂的所述碱的方法，使用碱，通过所述方法获得的盐以及含有这些盐的制剂来制备依他普仑的纯化盐如草酸盐的方法，以及制备纯化的依他普仑游离碱或其盐的方法使用氢溴酸盐，通过所述方法获得的盐和含有这些盐的制剂，例如草酸盐。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。

6. 发明申请

US20080161584A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
公开(公告)号：US20080161584A1
公开(公告)日：2008-07-03
申请号：US12046999
申请日：2008-03-12
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-isobenzo-furancarbonitrile, 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.

7. 发明申请

US20070021499A1 CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
标题翻译：包括ESCITALOPRAM基板的晶圆和可折叠片
公开(公告)号：US20070021499A1
公开(公告)日：2007-01-25
申请号：US11425522
申请日：2006-06-21
申请人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Rock , Helle Eliasen , Ken Liljegren
发明人： Robert Dancer , Hans Petersen , Ole Nielsen , Michael Rock , Helle Eliasen , Ken Liljegren
IPC分类号： A61K31/343 , C07D307/02
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。

8. 发明授权

US07112686B2 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-西酞普兰混合物制备外消旋西酞普兰和/或S-或R-西酞普兰的方法
公开(公告)号：US07112686B2
公开(公告)日：2006-09-26
申请号：US10482000
申请日：2002-06-25
申请人： Rikke E. Humble , Troels V. Christensen , Michael H. Rock , Ole Nielsen , Hans Petersen , Robert Dancer
发明人： Rikke E. Humble , Troels V. Christensen , Michael H. Rock , Ole Nielsen , Hans Petersen , Robert Dancer
IPC分类号： C07D307/78 , C07D307/87 , C07D307/93
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 addition salt thereof.
摘要翻译：本发明涉及一种通过分离R和S-的混合物来制备外消旋西酞普兰游离碱或其酸加成盐和/或R-或S-西酞普兰作为游离碱或其酸加成盐的方法，西酞普兰与超过50％的一种对映异构体组成由外消旋西酞普兰和/或S-西酞普兰或R-西酞普兰的部分组成的部分，其特征在于i）西酞普兰作为游离碱或作为酸从溶剂中沉淀出来其加成盐; ii）形成的沉淀物与母液分离; 如果沉淀物是结晶的，则任选地重结晶一次或多次以形成外消旋西酞普兰，然后任选地转化成其酸加成盐; iib）如果沉淀物不结晶，则任选地重复步骤i）和ii），直到获得结晶沉淀物，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，然后任选地转化为其酸加成盐; iii）任选地将母液进一步纯化，并从母液中分离S-西酞普兰或R-西酞普兰，并任选地转化成其加成盐。

9. 发明授权

US08076320B2 Crystalline forms of a pharmaceutical compound 有权
标题翻译：药物化合物的结晶形式
公开(公告)号：US08076320B2
公开(公告)日：2011-12-13
申请号：US10597977
申请日：2005-02-24
申请人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
发明人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
IPC分类号： A61P25/16 , A61K31/7056 , C07H19/23
CPC分类号： C07H19/23 , C07D491/22
摘要： Described are crystalline forms of the pharmaceutical compound “[9S-(9α,10β,12α)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9, 12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
摘要翻译：描述了药物化合物“[9S-（9α，10α，12α）] -5,16-双[（乙硫基）甲基] -2,3,9,10,11,12-六氢-10- -4-羟基-9-甲基-1-氧代-9,12-环氧基-1H-二吲哚并[1,2,3-fg：3'，2'，1'-k]吡咯并[3,4-i] 6]苯并二氮辛-10-羧酸甲酯“，以及它们的使用和制备方法。

10. 发明授权

US08729065B2 Crystalline forms of a pharmaceutical compound 有权
标题翻译：药物化合物的结晶形式
公开(公告)号：US08729065B2
公开(公告)日：2014-05-20
申请号：US12983558
申请日：2011-01-03
申请人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
发明人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
IPC分类号： A61P25/16 , A61K31/553 , C07D498/12
CPC分类号： C07H19/23 , C07D491/22
摘要： Described are crystalline forms of the pharmaceutical compound “[9S-(9α,10β,12α)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
摘要翻译：描述了药物化合物“[9S-（9α，10α，12α）] -5,16-双[（乙硫基）甲基] -2,3,9,10,11,12-六氢-10- 羟基-9-甲基-1-氧代-9,12-环氧基-1H-二吲哚并[1,2,3-fg：3'，2'，1'-k]吡咯并[3,4-i] 6]苯并二氮辛-10-羧酸甲酯“，以及它们的使用和制备方法。

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