ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TUBULIN INHIBITOR INDIBULIN
    5.
    发明授权
    ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TUBULIN INHIBITOR INDIBULIN 有权
    口服固体TUBULINHEMMSTOFFS吲地布林药物剂型

    公开(公告)号:EP1922061B8

    公开(公告)日:2010-09-08

    申请号:EP06761981.7

    申请日:2006-06-07

    IPC分类号: A61K9/16 A61K31/4439

    摘要: The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

    ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TRIBULIN INHIBITOR INDIBULIN
    6.
    发明公开
    ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TRIBULIN INHIBITOR INDIBULIN 有权
    口服固体TRIBULINHEMMSTOFFS吲地布林药物剂型

    公开(公告)号:EP1922061A2

    公开(公告)日:2008-05-21

    申请号:EP06761981.7

    申请日:2006-06-07

    IPC分类号: A61K9/16 A61K31/4439

    摘要: The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

    Compounds and methods for the treatment of cancer
    7.
    发明授权
    Compounds and methods for the treatment of cancer 有权
    用于治疗癌症的化合物和方法

    公开(公告)号:EP2394702B1

    公开(公告)日:2014-12-31

    申请号:EP11180330.0

    申请日:2006-07-28

    IPC分类号: A61P35/00

    CPC分类号: A61K45/06 A61K31/285 C07F9/72

    摘要: The present invention provides an organic arsenicals of the formula (I) which is potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. wherein the melting point of the compound in its crystalline form is greater than 160 °C.

    Compounds and methods for the treatment of cancer
    8.
    发明公开
    Compounds and methods for the treatment of cancer 有权
    Verbindungen und Verfahren zur Behandlung von Krebs

    公开(公告)号:EP2394702A1

    公开(公告)日:2011-12-14

    申请号:EP11180330.0

    申请日:2006-07-28

    IPC分类号: A61P35/00

    CPC分类号: A61K45/06 A61K31/285 C07F9/72

    摘要: The present invention provides an organic arsenicals of the formula (I) which is potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.

    wherein the melting point of the compound in its crystalline form is greater than 160 °C.

    摘要翻译: 本发明提供了式(I)的有机砷,其对于固体和血液来源的许多人类肿瘤细胞系以及来自白血病患者的恶性血细胞都是有效的体外细胞毒性活性。 其中化合物的结晶形式的熔点大于160℃。

    ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TRIBULIN INHIBITOR INDIBULIN
    10.
    发明授权
    ORAL SOLID PHARMACEUTICAL FORMULATION OF THE TRIBULIN INHIBITOR INDIBULIN 有权
    口服TRIBULIN缓蚀剂的口服固体制剂

    公开(公告)号:EP1922061B1

    公开(公告)日:2008-12-17

    申请号:EP06761981.7

    申请日:2006-06-07

    IPC分类号: A61K9/16 A61K31/4439

    摘要: The present invention relates to a pharmaceutical formulation for oral administration of the poorly soluble and therefore hardly bioavailable microtubule polymerization inhibitor Indibulin and a process for its manufacture. In particular, there is provided a pharmaceutical formulation of Indibulin for oral administration comprising a granulate containing micronized Indibulin having a particle size of less than 20 mum for at least 99% of the volume of particles, at least one hydrophilic surfactant, and at least one capsulation excipient. The present invention also discloses a method of treating hyperproliferative disorders, malignancies and neoplasms with Indibulin.

    摘要翻译: 本发明涉及用于口服给药难溶性且因此难以生物利用的微管蛋白抑制剂Indibulin的药物制剂及其制造方法。 具体而言,提供了用于口服给药的吲地布林药物制剂,其包含含有对于至少99体积%的颗粒具有小于20μm的粒度的微粉化吲地布林的颗粒,至少一种亲水性表面活性剂和一种 更多的包装赋形剂。