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    STABLE POWDER FORMULATION CONTAINING AN ANTICHOLINGERIC AGENT
    6.
    发明申请
    STABLE POWDER FORMULATION CONTAINING AN ANTICHOLINGERIC AGENT 审中-公开
    含稳定粉剂的抗菌剂

    公开(公告)号：US20130164344A1

    公开(公告)日：2013-06-27

    申请号：US13706885

    申请日：2012-12-06

    Applicant: Michael TRUNK ,  Claudius WEILER ,  Werner PIEROTH

    Inventor： Michael TRUNK ,  Claudius WEILER ,  Werner PIEROTH

    IPC: A61K9/16

    CPC classification number: A61K31/5375 ,  A61K9/0075 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1647 ,  A61K9/1652 ,  A61K9/1682 ,  A61K9/4858 ,  C07D451/12

    Abstract: The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X− represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation.

    Abstract translation: 本发明涉及包含以下组分的颗粒的喷雾干燥粉末制剂：i）至iii）：i）抗胆碱剂，特别是至少一种式I化合物，其中X代表带负电荷的阴离子，ii） 至少一种选自单糖或二糖，低聚糖，聚合物，糖醇和胆固醇的嵌入材料，iii）有机，生理上可接受的空间要求酸，选自抗坏血酸，一价，二价 或三价羧酸，除了氨基羧酸，优选富马酸，草酸或二乙酸，以及果酸或烹饪酸，优选柠檬酸，酒石酸，苹果酸，乳酸，乙酸，α- 羟基辛酸或葡萄糖酸。 本发明还涉及制备所述制剂的方法。

    Stable powder formulation containing an anticholinergic agent
    8.
    发明申请
    Stable powder formulation containing an anticholinergic agent 审中-公开
    含有抗胆碱剂的稳定的粉末制剂

    公开(公告)号：US20100055193A1

    公开(公告)日：2010-03-04

    申请号：US12515780

    申请日：2007-11-06

    Applicant: Michael Trunk ,  Claudius Weiler ,  Werner Pieroth

    Inventor： Michael Trunk ,  Claudius Weiler ,  Werner Pieroth

    IPC: A61K9/14 ,  A61K31/5386 ,  A61P11/16

    CPC classification number: A61K31/5375 ,  A61K9/0075 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1647 ,  A61K9/1652 ,  A61K9/1682 ,  A61K9/4858 ,  C07D451/12

    Abstract: The invention relates to a spray-dried powder formulation comprising particles that contain the following components i) to iii): i) anticholinergic agents, in particular at least one compound of formula 1, in which X− represents a negatively charged anion, ii) at least one embedding material selected from the group consisting of mono- or disaccharides, oligosaccharides, polymers, sugar alcohols and cholesterol, iii) an organic, physiologically acceptable, sterically demanding acid, selected from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid. The invention also relates to a method for producing said formulation and to the use of an organic, physiologically acceptable, sterically demanding acid from the group consisting of ascorbic acid, a monovalent, divalent or trivalent carboxylic acid, with the exception of amino carboxylic acids, preferably fumaric acid, oxalic acid, or diacetic acid, and a fruit acid or culinary acid, preferably citric acid, tartaric acid, malic acid, lactic acid, acetic acid, α-hydroxycaprylic acid or gluconic acid, for stabilising a powder formulation produced by spray-drying containing the aforementioned compound of formula 1 according to i) and a suitable embedding material ii).

    Abstract translation: 本发明涉及包含以下组分的颗粒的喷雾干燥粉末制剂：i）至iii）：i）抗胆碱剂，特别是至少一种式I化合物，其中X代表带负电荷的阴离子，ii） 至少一种选自单糖或二糖，低聚糖，聚合物，糖醇和胆固醇的嵌入材料，iii）有机，生理上可接受的空间要求酸，选自抗坏血酸，一价，二价 或三价羧酸，除了氨基羧酸，优选富马酸，草酸或二乙酸，以及果酸或烹饪酸，优选柠檬酸，酒石酸，苹果酸，乳酸，乙酸， 羟基辛酸或葡萄糖酸。 本发明还涉及一种生产所述制剂的方法，以及使用由抗坏血酸，一价，二价或三价羧酸组成的组中的有机，生理上可接受的空间要求的酸，除了氨基羧酸， 优选富马酸，草酸或二乙酸，以及果酸或烹饪酸，优选柠檬酸，酒石酸，苹果酸，乳酸，乙酸，α-羟基辛酸或葡萄糖酸，用于稳定由 喷雾干燥含有上述根据i）的式1化合物和合适的包埋材料ii）。

    Tropane analogs and methods for inhibition of monoamine transport
    9.
    发明申请
    Tropane analogs and methods for inhibition of monoamine transport 审中-公开
    托烷类似物和抑制单胺转运的方法

    公开(公告)号：US20070244149A1

    公开(公告)日：2007-10-18

    申请号：US11731759

    申请日：2007-03-30

    Applicant: Peter Meltzer ,  Bertha Madras ,  Paul Blundell

    Inventor： Peter Meltzer ,  Bertha Madras ,  Paul Blundell

    IPC: A61K31/44 ,  A61P25/28 ,  C07D451/02

    CPC classification number: C07D451/02 ,  C07D451/06 ,  C07D451/12

    Abstract: New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.

    Abstract translation: 描述了结合单胺转运蛋白的新托品类似物，特别是具有6-或7-羟基或酮取代基的8-氮杂，8碳和8-氧代正丙酸。 本发明的化合物可以是外消旋的，纯的R-对映体或纯的S-对映异构体。 某些优选的本发明化合物对于DAT与SERT具有高选择性。 还描述了包含配制在药学上可接受的载体中的化合物的药物治疗组合物和通过使单胺转运蛋白与5-羟色胺重摄取抑制量的本发明化合物接触来抑制单胺转运蛋白的5-羟基 - 色胺再摄取的方法 。 用于实施本发明的优选的单胺转运蛋白包括多巴胺转运蛋白，5-羟色胺转运蛋白和去甲肾上腺素转运蛋白。

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