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11 条记录 (耗时 0.044 秒)

    MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
    1.
    发明申请
    MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT 审中-公开
    含有药物诱导剂的熔融挤出固体分散体

    公开(公告)号：US20120108590A1

    公开(公告)日：2012-05-03

    申请号：US13253727

    申请日：2011-10-05

    申请人： Esther Birtalan ,  Peter Hoelig ,  David J. Lindley ,  Yeshwant D. Sanzgiri ,  Ping Tong

    发明人： Esther Birtalan ,  Peter Hoelig ,  David J. Lindley ,  Yeshwant D. Sanzgiri ,  Ping Tong

    IPC分类号： A61K31/496 ,  A61P35/02 ,  A61P37/00 ,  A61K31/5377 ,  A61P35/00

    CPC分类号： A61K31/496 ,  A61K9/0053 ,  A61K9/1635 ,  A61K9/1694 ,  A61K9/2027 ,  A61K9/2095 ,  A61K31/5377 ,  A61K31/541 ,  A61K47/02 ,  A61K47/26 ,  A61K47/32

    摘要： A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease.

    摘要翻译： 促凋亡固体分散体以基本上非结晶形式包含分散在固体基质中的如本文定义的式I的Bcl-2家族蛋白质抑制化合物，其包含（a）药学上可接受的水溶性聚合物载体和（ b）药学上可接受的表面活性剂。 制备这种固体分散体的方法包括使升高的温度使式I化合物，水溶性聚合物载体和表面活性剂提供可挤出的半固体混合物; 挤出半固体混合物; 并将所得的挤出物冷却以提供包含聚合物载体和表面活性剂的固体基质，并使化合物以基本上非结晶形式分散在其中。 固体分散体适合于有需要的受试者口服给药以治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症或免疫或自身免疫性疾病）过表达为特征的疾病。

    SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT
    9.
    发明申请
    SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT 审中-公开
    含有病毒诱导剂的固体分散体

    公开(公告)号：US20120277210A1

    公开(公告)日：2012-11-01

    申请号：US13282773

    申请日：2011-10-27

    申请人： Nathaniel Catron ,  David Lindley ,  Jonathan M. Miller ,  Eric A. Schmitt ,  Ping Tong

    发明人： Nathaniel Catron ,  David Lindley ,  Jonathan M. Miller ,  Eric A. Schmitt ,  Ping Tong

    IPC分类号： A61K31/496 ,  A61K31/517 ,  A61P37/00 ,  A61P35/00 ,  A61P35/02 ,  A61K31/5377 ,  A61K31/541

    CPC分类号： A61K31/5377 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/4866 ,  A61K31/437 ,  A61K31/496 ,  Y02A50/411

    摘要： A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

    摘要翻译： 促凋亡固体分散体以基本上非结晶形式包含分散在固体基质中的如本文定义的式I的Bcl-2家族蛋白质抑制化合物，其包含（a）药学上可接受的水溶性聚合物载体和（ b）药学上可接受的表面活性剂。 制备这种固体分散体的方法包括将化合物，聚合物载体和表面活性剂溶解在合适的溶剂中，并除去溶剂以提供包含聚合物载体和表面活性剂的固体基质，并使化合物分散在基本上不结晶 形成。 该固体分散体适合于需要其的受试者口服给药以治疗以一种或多种抗凋亡Bcl-2家族蛋白（例如癌症）过表达为特征的疾病。