PEG LINKER COMPOUNDS AND BIOLOGICALLY ACTIVE CONJUGATES THEREOF
    2.
    发明申请
    PEG LINKER COMPOUNDS AND BIOLOGICALLY ACTIVE CONJUGATES THEREOF 审中-公开
    PEG连接子化合物及其生物活性偶联物

    公开(公告)号:US20090285780A1

    公开(公告)日:2009-11-19

    申请号:US12302238

    申请日:2007-05-24

    申请人: Chyi Lee

    发明人: Chyi Lee

    摘要: PEG linker compounds and biologically active conjugates thereof having mixed functional group linkages attached to at least one PEG moeity, and a coupling group for attaching a biologically active molecule. The PEG mixed linkages can be the combinations of stable, or labile, or releasable, or stable and labile, or stable and releasable, or releasable and labile covalent linkages. The mixed functional linkages of the PEG linker compounds consist of different organic functional groups, which have non-equivalent half-life in plasma and, hence, they have different release rates in blood. The present invention also provides for attachment of novel PEG linker compounds with mixed functional linkages for Pegylation of biologically active molecules to produce Probiomolecule-PEG constructs. The Probiomolecule-PEG construct is the prodrug of biomolecule-PEG conjugate or biomolecule. The Probiomolecule-PEG conjugate will gradually lose portions (or all) of its PEG polymers in vivo to convert into smaller size biomolecule-PEG conjugate (or biologically active molecule), thereby increasing their biological activity in vivo.

    摘要翻译: PEG连接体化合物及其与至少一种PEG摩尔系连接的混合官能团键的生物活性缀合物和用于连接生物活性分子的偶联基团。 PEG混合键可以是稳定的或不稳定的,或可释放的,或稳定的和不稳定的,或稳定的和可释放的,或可释放的和不稳定的共价键的组合。 PEG接头化合物的混合功能键由不同的有机官能团组成,其在血浆中具有非等效的半衰期,因此在血液中具有不同的释放速率。 本发明还提供了新型PEG连接体化合物与生物活性分子的聚乙二醇化混合功能键的连接以产生生物分子-PEG构建体。 生物分子-PEG构建体是生物分子-PEG轭合物或生物分子的前药。 生物分子-PEG缀合物将在体内逐渐失去部分(或全部)其PEG聚合物,以转化为更小尺寸的生物分子-PEG轭合物(或生物活性分子),从而增加其在体内的生物活性。

    SYNERGISTIC BIOMOLECULE-POLYMER CONJUGATES
    4.
    发明申请
    SYNERGISTIC BIOMOLECULE-POLYMER CONJUGATES 审中-公开
    协同生物分子聚合物共聚物

    公开(公告)号:US20130195799A1

    公开(公告)日:2013-08-01

    申请号:US13817702

    申请日:2011-08-19

    申请人: Chyi Lee

    发明人: Chyi Lee

    IPC分类号: C08G65/333

    摘要: The synergistic biomolecule-polymer conjugates are the long-acting, in vivo controlled continuous-release and hybrid synergy systems of biomolecules that provide increased biological activities and enhanced pharmacological properties for achieving greater therapeutic efficacies.

    摘要翻译: 协同生物分子 - 聚合物缀合物是生物分子的长效,体内受控的连续释放和混合协同系统,其提供增加的生物活性和增强的药理学性质以获得更大的治疗功效。