Medicinal compositions and method for the preparation thereof
    4.
    发明授权
    Medicinal compositions and method for the preparation thereof 失效
    药物组合物及其制备方法

    公开(公告)号:US07597897B2

    公开(公告)日:2009-10-06

    申请号:US10596836

    申请日:2004-12-10

    摘要: Methods for the manufacture of medicinal compositions are described. A method for the manufacture of a medicinal composition according to the invention comprises: (a) Providing a biocompatible polymer of the general formula —[O—R1—C(O)]n— wherein: “R1” is a linear, branched, or cyclic organic group, “n” is at least three, (b) Acylating the biocompatible polymer to provide an acylated biocompatible polymer and a mixed anhydride; (c) Reacting the mixed anhydride with a nucleophile to provide an acylated biocompatible polymer with a terminal carboxylic acid derivative capable of being chemically converted to an acid in the absence of water, (d) Converting the terminal carboxylic acid derivative to an acylated biocompatible polymer with a terminal carboxylic acid; and (e) Combining the acylated biocompatible polymer with a drug to provide the medicinal composition.

    摘要翻译: 描述了药物组合物的制造方法。 制备根据本发明的药用组合物的方法包括:(a)提供通式为[O-R 1 -C(O)] n - 的生物相容性聚合物,其中:“R 1”为直链,支链, 或环状有机基团,“n”为至少三个,(b)酰化生物相容性聚合物以提供酰化生物相容性聚合物和混合酸酐; (c)用亲核试剂反应混合酸酐以提供酰化的生物相容性聚合物,其具有能够在不存在水的情况下化学转化为酸的末端羧酸衍生物; (d)将末端羧酸衍生物与末端羧酸转化成酰化生物相容性聚合物; 和(e)将酰化的生物相容性聚合物与药物组合以提供药物组合物。

    Biocompatible Polymer Compounds For Medicinal Formulations
    5.
    发明申请
    Biocompatible Polymer Compounds For Medicinal Formulations 审中-公开
    药用配方的生物相容性高分子化合物

    公开(公告)号:US20080112894A1

    公开(公告)日:2008-05-15

    申请号:US11816883

    申请日:2006-03-14

    IPC分类号: A61K9/12 A61K47/32

    摘要: Stability of biocompatible polymers of the formula: wherein Z is —C(O)R1; each R1 is independently selected from a linear, branched, or cyclic alkyl, alkoxy, or aryl with 1 to 18 carbon atoms optionally substituted by carbonyl, oxy, thio, and/or nitrogen; each R2 is independently selected from hydrogen or a linear or branched hydrocarbon with 1 to 4 carbon atoms; X is selected from the group consisting of —OR1, —SR1, —N(R1)2 and divalent or trivalent headgroups terminated in oxygen, nitrogen, or sulfur; y is greater than or equal to 1 and less than or equal to 3; is enhanced by providing compositions where there is a low level of —OH end group impurity, i.e., where Z is —H instead of —C(O)R1 and/or X is —OH instead of —OR1, —SR1, —N(R1)2 or divalent or trivalent headgroups terminated in —O—, —N—, or —S—, such that there are no more than 10 of these —OH end groups for every 100 intended biocompatible polymer molecules.

    摘要翻译: 下式的生物相容性聚合物的稳定性:其中Z为-C(O)R 1; 每个R 1独立地选自具有任选被羰基,氧基,硫基和/或氮取代的具有1至18个碳原子的直链,支链或环状烷基,烷氧基或芳基; 每个R 2独立地选自氢或具有1至4个碳原子的直链或支链烃; X选自-OR 1,-SR 1 N, - N(R 1)2, - SUB >和二价或三价头基终止于氧,氮或硫; y大于或等于1且小于或等于3; 通过提供其中存在低水平的-OH端基杂质的组合来增强,即其中Z是-H而不是-C(O)R 1和/或X是-OH而不是 -OR 1,-SR 1,-N(R 1)2,或二价或三价头基终止于 -O-,-N-或-S-,使得每100个预期的生物相容性聚合物分子中不超过10个这些-OH端基。

    Novel Formulations
    6.
    发明申请
    Novel Formulations 审中-公开
    新型配方

    公开(公告)号:US20090123391A1

    公开(公告)日:2009-05-14

    申请号:US12293205

    申请日:2007-03-21

    IPC分类号: A61K9/12 A61P11/00

    CPC分类号: A61K9/008

    摘要: A pharmaceutical aerosol formulation includes a therapeutically effective amount of particulate medicament of formula (I) or a solvate thereof, a propellant selected from the group consisting of 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoro-n-propane or mixtures thereof, and a biocompatible polymer comprising one or more compounds of formula (II)

    摘要翻译: 药物气溶胶制剂包括治疗有效量的式(I)的颗粒药物或其溶剂合物,推荐剂选自1,1,1,2-四氟乙烷,1,1,1,2,3, 3,3-七氟正丙烷或其混合物,以及包含一种或多种式(II)化合物的生物相容性聚合物,

    Medicinal Compositions and Method for the Preparation Thereof
    10.
    发明申请
    Medicinal Compositions and Method for the Preparation Thereof 失效
    药用组合物及其制备方法

    公开(公告)号:US20080267885A1

    公开(公告)日:2008-10-30

    申请号:US10596836

    申请日:2004-12-10

    IPC分类号: A61K47/48 A61K9/12

    摘要: Methods for the manufacture of medicinal compositions are described. A method for the manufacture of a medicinal composition according to the invention comprises: (a) Providing a biocompatible polymer of the general formula —[O—R1—C(O)]n— wherein: “R1” is a linear, branched, or cyclic organic group, “n” is at least three, (b) Acylating the biocompatible polymer to provide an acylated biocompatible polymer and a mixed anhydride; (c) Reacting the mixed anhydride with a nucleophile to provide an acylated biocompatible polymer with a terminal carboxylic acid derivative capable of being chemically converted to an acid in the absence of water, (d) Converting the terminal carboxylic acid derivative to an acylated biocompatible polymer with a terminal carboxylic acid; and (e) Combining the acylated biocompatible polymer with a drug to provide the medicinal composition.

    摘要翻译: 描述了药物组合物的制造方法。 制备根据本发明的药物组合物的方法包括:(a)提供具有通式的生物相容性聚合物 - [OR 1 -C 2 -C(O)] n 其中:“R 1”是直链,支链或环状有机基团,“n”为至少三个,(b)酰化生物相容性聚合物以提供酰化生物相容性聚合物和混合 酐; (c)用亲核试剂反应混合酸酐以提供酰化的生物相容性聚合物,其具有能够在不存在水的情况下化学转化为酸的末端羧酸衍生物; (d)将末端羧酸衍生物与末端羧酸转化成酰化生物相容性聚合物; 和(e)将酰化的生物相容性聚合物与药物组合以提供药物组合物。