MULTI-ARM POLYMER PRODRUGS
    2.
    发明申请
    MULTI-ARM POLYMER PRODRUGS 有权
    多臂聚合物原料

    公开(公告)号:US20170056514A1

    公开(公告)日:2017-03-02

    申请号:US15144440

    申请日:2016-05-02

    IPC分类号: A61K47/48 A61K31/4709

    摘要: Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

    摘要翻译: 本文提供的是水溶性前药,包含这些前药的组合物,以及制备和施用该前药的相关方法。 本发明的前药包含具有三个或更多个臂的水溶性聚合物,其中至少三个通常共价连接到活性剂例如小分子上。 本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载,因为本发明的缀合物具有可释放地连接到多臂水溶性聚合物上的三种或更多种活性剂。 与未修饰的母体药物相比,本发明的前药在治疗上是有效的,并且在体内表现出改善的性质。

    MULTI-ARM POLYMER PRODRUGS
    3.
    发明申请
    MULTI-ARM POLYMER PRODRUGS 有权
    多臂聚合物原料

    公开(公告)号:US20140323514A1

    公开(公告)日:2014-10-30

    申请号:US14323993

    申请日:2014-07-03

    IPC分类号: A61K47/48

    摘要: Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

    摘要翻译: 本文提供的是水溶性前药,包含这些前药的组合物,以及制备和施用该前药的相关方法。 本发明的前药包含具有三个或更多个臂的水溶性聚合物,其中至少三个通常共价连接到活性剂例如小分子上。 本发明的共轭物提供聚合物尺寸和结构的最佳平衡以实现改善的药物负载,因为本发明的缀合物具有可释放地连接到多臂水溶性聚合物上的三种或更多种活性剂。 与未修饰的母体药物相比,本发明的前药在治疗上是有效的,并且在体内表现出改善的性质。