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    Dosing form for a polymer support, use of said dosing form in organic chemical synthesis and method for production of said dosing form
    82.
    发明申请
    Dosing form for a polymer support, use of said dosing form in organic chemical synthesis and method for production of said dosing form 审中-公开
    用于聚合物载体的剂量形式，在有机化学合成中使用所述加料形式以及用于生产所述加料形式的方法

    公开(公告)号：US20030138847A1

    公开(公告)日：2003-07-24

    申请号：US10245839

    申请日：2002-09-16

    Applicant: H. Lundbeck A/S

    Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

    IPC: G01N033/53 ,  C08G063/91 ,  G01N033/543 ,  C08G063/48

    CPC classification number: C07K1/042 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  B01J2219/0072 ,  C07B2200/11 ,  C40B60/14

    Abstract: A dosing form for a polymer support for organic chemical synthesis in a solvent medium comprising a fixed weight amount of beads of a polymer containing functional groups, which polymer is insoluble in the solvent for the intended synthesis, is provided as compressed tablets of essentially equal weight and composition wherein the polymer beads are essentially intact and are released as such when the tablets are disintegrated in said solvent. Use of the dosing form is made in conventional synthesis, in parallel synthesis, in split and mix synthesis and/or combinatorial chemistry. In a method for producing the dosing form, beads of a polymer having functional gropusgroups is compressed into tablets after pre-treatment with an aprotic organic solvent groups are compressed into tablets after pre-treatment with an aprotic organic solvent.

    Abstract translation: 提供用于溶剂介质中有机化学合成的聚合物载体的剂型，其包含固定重量的含有官能团的聚合物珠，该聚合物不溶于用于预期合成的溶剂中，作为基本相等重量的压片 和组合物，其中当片剂在所述溶剂中崩解时，聚合物珠基本上是完整的并且如此释放。 在分批和混合合成和/或组合化学中，在常规合成，并行合成中使用配料形式。 在制备给药形式的方法中，具有功能性组蛋白的聚合物的珠粒在用非质子有机溶剂基团预处理后被压缩成片剂，在用非质子有机溶剂预处理后被压缩成片剂。

    Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form
    83.
    发明申请
    Dosing form for reagents, use of said dosing form in organic chemical synthesis and production of said dosing form 审中-公开
    用于试剂的剂量形式，在有机化学合成中使用所述给药形式并生产所述给药形式

    公开(公告)号：US20030138376A1

    公开(公告)日：2003-07-24

    申请号：US10245836

    申请日：2002-09-16

    Applicant: H. Lundbeck A/S

    Inventor： Thomas Ruhland ,  Per Holm ,  Kirsten Schultz ,  Jannie Egeskov Holm ,  Kim Andersen

    IPC: A61K049/00 ,  G01N033/543

    CPC classification number: C07K1/023 ,  B01J4/02 ,  B01J19/0046 ,  B01J2219/00351 ,  B01J2219/00459 ,  B01J2219/00497 ,  B01J2219/005 ,  B01J2219/00585 ,  B01J2219/0059 ,  B01J2219/00592 ,  C07K1/04 ,  C07K1/1077 ,  C40B60/14

    Abstract: A dosing form for at least one solid reagent for use in conventional organic and inorganic synthesis, in parallel synthesis, and in split and mix synthesis in combinatorial chemistry is provided as compressed tablets each containing the same predetermined amount of said at least one reagent embedded in a polymer matrix comprising beads of a polymer insoluble in the solvents for the intended synthesis, which tablets are capable of disintegrating in said solvent for release of the at least one reagent and disperse the matrix as polymer beads into the solvent. The polymer beads forming the matrix and the reagents of the dosing form can easily be removed by filtration in order to separate these from a formed soluble product. In a method for producing the dosing form, beads of one or more polymers are mixed with the reagents and compressed into tablets after pre-treatment with an aprotic organic solvent.

    Abstract translation: 提供用于常规有机和无机合成，并行合成和组合化学中的分离和混合合成中的至少一种固体试剂的给药形式，其为包含相同预定量的所述至少一种试剂 聚合物基质，其包含不溶于用于预期合成的溶剂中的聚合物的珠粒，该片剂能够在所述溶剂中分解以释放至少一种试剂并将基质作为聚合物珠分散到溶剂中。 形成基质的聚合物珠粒和剂型的试剂可以通过过滤容易地除去，以将它们与形成的可溶性产物分离。 在制备给药形式的方法中，将一种或多种聚合物的珠粒与试剂混合，并用非质子有机溶剂预处理后压制成片剂。

    Method for the preparation of pure citalopram
    86.
    发明申请
    Method for the preparation of pure citalopram 失效
    纯西酞普兰的制备方法

    公开(公告)号：US20020120005A1

    公开(公告)日：2002-08-29

    申请号：US10046126

    申请日：2002-01-08

    Applicant: H. Lundbeck A/S

    Inventor： Marco Villa ,  Federico Sbrogio ,  Robert Dancer

    IPC: A61K031/36 ,  C07D37/81

    CPC classification number: C07D307/87

    Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) 1 in which a compound of formula (II) 2 wherein Z is iodo, bromo, chloro or CF3null(CF2)nnullSO2nullOnull, 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.

    Abstract translation: 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。

    Treatment of neurotic disorders
    87.
    发明申请
    Treatment of neurotic disorders 有权
    治疗神经性疾病

    公开(公告)号：US20020086899A1

    公开(公告)日：2002-07-04

    申请号：US10021126

    申请日：2001-12-12

    Applicant: H. Lundbeck A/S

    Inventor： Connie Sanchez ,  Sandra Hogg

    IPC: A61K031/343

    CPC classification number: A61K31/343 ,  Y10S514/962

    Abstract: Use of escitalopram (the S-(null)-enantiomer of citalopram) or a pharmaceutically acceptable salt thereof for the preparation of a medicament useful in the treatment of neurotic disorders is provided, including anxiety states, in particular generalised anxiety disorder and social anxiety disorder, post traumatic stress disorder, obsessive compulsive disorder and panic attacks.

    Abstract translation: 提供了依他普仑（西酞普兰的S-（+） - 对映异构体）或其药学上可接受的盐在制备用于治疗神经性疾病的药物中的应用，包括焦虑状态，特别是广泛性焦虑症和社会焦虑症 ，创伤后应激障碍，强迫症和恐慌发作。

    Method for the preparation of citalopram
    88.
    发明申请
    Method for the preparation of citalopram 审中-公开
    西酞普兰制备方法

    公开(公告)号：US20020077353A1

    公开(公告)日：2002-06-20

    申请号：US10012054

    申请日：2001-11-06

    Applicant: H. Lundbeck A/S

    Inventor： Hans Petersen ,  Michael Harold Rock ,  Henrik Svane

    IPC: C07D307/78 ,  A61K031/343

    CPC classification number: C07D307/87 ,  C07D307/81

    Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) 1 wherein R is halogen, or CF3null(CF2)nnullSO2null, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cnull or Zn2null, or with Zn(CN)2 in the presence of a palladium catalyst.

    Abstract translation: 制备西酞普兰的方法，其包括其中R为卤素的式（IV）化合物或CF 3 - （CF 2）n -SO 2 - ，n为0至8的化合物与氰化物源在钯催化剂存在下反应， 催化量的C +或Zn 2+，或与Zn（CN）2在钯催化剂存在下反应。

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