Prodrugs comprising an exendin linker conjugate
    38.
    发明授权
    Prodrugs comprising an exendin linker conjugate 有权
    包含毒蜥外泌肽连接子缀合物的前药

    公开(公告)号:US09133276B2

    公开(公告)日:2015-09-15

    申请号:US13822170

    申请日:2011-09-16

    摘要: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an exendin linker conjugate D-L1, wherein D represents an exendin moiety; and -L1 is represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the exendin moiety by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by exendin.

    摘要翻译: 本发明涉及前药或其药学上可接受的盐,其包含毒蜥外泌肽连接体缀合物D-L1,其中D表示毒蜥外泌肽部分; -L1由式(I)表示,其中虚线表示通过形成酰胺键与毒蜥蜴蛋白部分的一个氨基的连接。 本发明进一步涉及包含所述前体药物的药物组合物及其作为治疗或预防可被毒蜥外泌肽治疗的疾病或病症的药物的用途。

    High-Loading Water-Soluable Carrier-Linked Prodrugs
    39.
    发明申请
    High-Loading Water-Soluable Carrier-Linked Prodrugs 审中-公开
    高负载水溶性载体连接前体药物

    公开(公告)号:US20140296257A1

    公开(公告)日:2014-10-02

    申请号:US14237429

    申请日:2012-08-10

    摘要: The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment.

    摘要翻译: 本发明涉及式(I)的水溶性载体连接的前药,其中B,A和Hyp形成载体,B是支化核心,每个A独立地是基于聚(乙二醇)的聚合物链,每个 Hyp独立地是支链部分,每个SP独立地是间隔基部分,每个L独立地是可逆的前药接头部分,每个D独立地是生物活性部分,每个x独立地为0或1,每个m独立地为 2〜64,n为3〜32的整数, 或其药学上可接受的盐。 它还涉及包含所述水溶性载体连接的前药的药物组合物,它们作为药物或诊断用途以及治疗方法。