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    Method for the preparation of pure citalopram
    1.
    发明授权
    Method for the preparation of pure citalopram 失效
    纯西酞普兰的制备方法

    公开(公告)号：US06455710B1

    公开(公告)日：2002-09-24

    申请号：US10046126

    申请日：2002-01-08

    申请人： Marco Villa ,  Federico Sbrogiò ,  Robert Dancer

    发明人： Marco Villa ,  Federico Sbrogiò ,  Robert Dancer

    IPC分类号： C01D30787

    CPC分类号： C07D307/87

    摘要： The present invention relates to the process for the preparation and purification of citalopram (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF3—(CF2)n—SO2—O—, n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and subsequently treated with an amide or an amide-like group forming agent; the reaction mixture is then subjected to an acid/base wash and/or crystallisation and recrystallisation of citalopram in order to remove the amides formed from the crude citalopram mixture; and the resulting citalopram product is optionally further purified, worked up and isolated as the base or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及西酞普兰（I）的制备和纯化方法，其中Z为碘，溴，氯或CF 3 - （CF 2）n -SO 2 -O-的式（II）化合物，n为0 ，1，2，3，4，5，6，7或8，与氰化物源进行氰化物交换反应; 所得粗制西酞普兰产品任选进行一些初始纯化，随后用酰胺或类酰胺形成剂处理; 然后将反应混合物进行酸/碱洗涤和/或结晶并重结晶西酞普兰以除去由西酞普兰粗制混合物形成的酰胺; 任选地进一步纯化，后处理和分离得到的西酞普兰产物作为碱或其药学上可接受的盐。

    CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE
    2.
    发明申请
    CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 审中-公开
    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。

    METHOD FOR MANUFACTURE OF ESCITALOPRAM
    3.
    发明申请
    METHOD FOR MANUFACTURE OF ESCITALOPRAM 有权
    制造方法

    公开(公告)号：US20090069582A1

    公开(公告)日：2009-03-12

    申请号：US12202522

    申请日：2008-09-02

    申请人： Carla De Faveri ,  Florian Anton Martin Huber ,  Robert Dancer

    发明人： Carla De Faveri ,  Florian Anton Martin Huber ,  Robert Dancer

    IPC分类号： C07D307/87 ,  C07C209/86

    CPC分类号： C07D307/87 ,  C07C253/34 ,  C07C255/59

    摘要： This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4′-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4′-fluoro-phenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)—(S,S)— or (−)—(R,R)-enantiomer of O,O′-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.

    摘要翻译： 该专利公开了将4- [4-（二甲基氨基）-1-（4'-氟苯基）-1-羟基丁基] -3-（羟基甲基） - 苄腈作为外消旋或非外消旋对映异构体混合物分离成其分离的方法 所述方法包括将4- [4-（二甲基氨基）-1-（4'-氟 - 苯基）-1-羟基丁基] -3-（羟甲基） - 苄腈以（+） - - 在包含1-丙醇，乙醇或乙腈的溶剂体系中的O，O-二对甲苯酰 - 酒石酸的（S，S） - 或（ - ） - （R，R） - 对映异构体。

    CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE
    4.
    发明申请
    CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE 有权
    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。

    Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
    5.
    发明授权
    Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
    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。

    CRYSTALLINE BASE OF ESCITALOPRAM AND ORODISPERSIBLE TABLETS COMPRISING ESCITALOPRAM BASE
    6.
    发明申请
    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.

    Process for the preparation of racemic citalopram diol and/or S- or R-citalopram diols and the use of such diols for the preparation of racemic citalopram, R-citalopram and/or S-citalopram
    7.
    发明授权
    Process for the preparation of racemic citalopram diol and/or S- or R-citalopram diols and the use of such diols for the preparation of racemic citalopram, R-citalopram and/or S-citalopram 失效
    用于制备外消旋西酞普兰二醇和/或S-或R-西酞普兰二醇的方法以及用于制备外消旋西酞普兰，西酞普兰和/或西酞普兰的这些二醇的用途

    公开(公告)号：US07390913B2

    公开(公告)日：2008-06-24

    申请号：US10540300

    申请日：2003-12-18

    申请人： Hans Petersen ,  Brian Christiansen ,  Robert Dancer ,  Rikke E. Humble

    发明人： Hans Petersen ,  Brian Christiansen ,  Robert Dancer ,  Rikke E. Humble

    IPC分类号： C07D307/78 ,  C07D307/87 ,  C07D307/93

    CPC分类号： C07D307/87 ,  C07C253/34

    摘要： In the following, citalopram diol means 4-(4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl)-3-(hydroxymethyl)-benzonitrile, as free base and/or acid addition salt. The invention relates to a process for the preparation of racemic citalopram diol and/or R- or S-citalopram diol, comprising the separation of a non-racemic mixture of R- and S-citalopram diol with more than 50% of one of the enantiomers into a fraction being enriched with S- or R-citalopram diol and a fraction comprising RS-citalopram diol wherein the ratio of R-citalopram diol:S-citalopram diol is equal to 1:1 or closer to 1:1 than in the initial mixture. The method is characterized in that (i) RS-citalopram diol is precipitated from a solution of the initial non-racemic mixture, or R- or S-citalopram diol is dissolved into a solvent from the initial non-racemic mixture, leaving a residue of RS-citalopram diol, and in that (ii) the residue/precipitate formed is separated from the final solution phase, followed by optional steps of repetition, recrystallisation, purification, isolation and conversion between free base and salts. The invention also relates to a process for the preparation of RS-citalopram, S-citalopram or R-citalopram (all as free base and/or acid addition salt) comprising the method described above followed by ring closure.

    摘要翻译： 在下文中，西酞普兰二醇是指作为游离碱和/或酸加成盐的4-（4-（二甲基氨基）-1-（4-氟苯基）-1-羟基丁基）-3-（羟甲基） - 苄腈。 本发明涉及一种制备外消旋西酞普兰二醇和/或R-或S-西酞普兰二醇的方法，包括将R-和S-西酞普兰二醇的非外消旋混合物与50％以上的 对映异构体转化成富含S-或R-西酞普兰二醇的级分和包含RS-西酞普兰二醇的级分，其中R-西酞普兰二醇：西西酞普兰二醇的比例等于1:1比或接近1比1 初始混合物。 该方法的特征在于（i）RS-西酞普兰二醇从初始非外消旋混合物的溶液中沉淀，或将R-或S-西酞普兰二醇从初始非外消旋混合物中溶解到溶剂中，留下残余物 的RS-西酞普兰二醇，并且（ii）所形成的残余物/沉淀物与最终溶液相分离，随后重复，重结晶，纯化，分离和转化游离碱和盐之间的任选步骤。 本发明还涉及一种制备RS-西酞普兰，西酞普兰或R-西酞普兰（均为游离碱和/或酸加成盐）的方法，包括上述方法，然后闭环。

    Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
    9.
    发明授权
    Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base 有权
    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。