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    Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages
    2.
    发明申请
    Carrier-Linked Prodrugs Having Reversible Carboxylic Ester Linkages 审中-公开
    具有可逆羧酸酯连接的载体相关前体药物

    公开(公告)号：US20140249093A1

    公开(公告)日：2014-09-04

    申请号：US14238447

    申请日：2012-08-10

    申请人： Dirk Vetter ,  Harald Rau

    发明人： Dirk Vetter ,  Harald Rau

    IPC分类号： A61K47/48 ,  A61K31/216

    CPC分类号： A61K31/216 ,  A61K31/25 ,  A61K47/60 ,  A61K47/64

    摘要： The invention provides a carrier-linked prodrugs, wherein the biologically active moieties comprise at least one carboxylic acid and wherein the linkage between the drug moiety and linker is in the form of an ester wherein the hydroxyl group required for ester formation is provided by the linker moiety and the carboxyl group required for ester formation is provided by the drug moiety. The hydroxyl group of the linker is sterically hindered by the presence of an alkyl or aryl group on the carbon directly bound to or adjacent to the carbon carrying the hydroxyl group (α-carbon). The steric effect of the alkyl or aryl group enables greater control of the rate of hydrolytic degradation of such carrier-linked prodrugs.

    摘要翻译： 本发明提供载体连接的前药，其中生物活性部分包含至少一种羧酸，并且其中药物部分和接头之间的连接是酯的形式，其中酯形成所需的羟基由连接体提供 部分和酯形成所需的羧基由药物部分提供。 在直接与携带羟基（α-碳）的碳上键合或相邻的碳上存在烷基或芳基，连接体的羟基被空间位阻。 烷基或芳基的立体效应能够更好地控制这种载体连接的前药的水解降解速率。

    Biodegradable polyethylene glycol based water-insoluble hydrogels
    4.
    发明授权
    Biodegradable polyethylene glycol based water-insoluble hydrogels 有权

    公开(公告)号：US11559482B2

    公开(公告)日：2023-01-24

    申请号：US13387971

    申请日：2010-07-30

    申请人： Harald Rau ,  Ulrich Hersel ,  Mathias Krusch ,  Dirk Vetter ,  Tobias Voigt

    发明人： Harald Rau ,  Ulrich Hersel ,  Mathias Krusch ,  Dirk Vetter ,  Tobias Voigt

    IPC分类号： A61K47/10 ,  C08J3/075 ,  A61K47/60 ,  A61K47/69 ,  A61K9/00

    摘要： The present invention relates to biodegradable polyethylene glycol based water-insoluble hydrogels comprising backbone moieties which are interconnected by hydrolytically degradable bonds, the backbone moieties further comprising reactive functional groups, wherein the water-insoluble hydrogel is further characterized in that the ratio between the time period for the complete degradation of the hydrogel by hydrolysis of the degradable bonds into water-soluble degradation products comprising one or more backbone moieties and the time period for the release of the first 10 mol-% of water-soluble degradation products comprising one or more backbone moieties based on the total amount of backbone moieties in the hydrogel is greater than 1 and equal to or less than 2. The invention further relates to conjugates of such hydrogels with ligands or ligating groups, prodrugs and pharmaceutical compositions as well as their use in a medicament.

    Aliphatic prodrug linker
    6.
    发明授权
    Aliphatic prodrug linker 有权
    脂肪族前药接头

    公开(公告)号：US08980242B2

    公开(公告)日：2015-03-17

    申请号：US11993645

    申请日：2006-06-21

    申请人： Dirk Vetter ,  Harald Rau ,  Thomas Wegge ,  Ulrich Hersel

    发明人： Dirk Vetter ,  Harald Rau ,  Thomas Wegge ,  Ulrich Hersel

    IPC分类号： A61K31/74 ,  A61K47/48

    CPC分类号： A61K47/48215 ,  A61K47/60

    摘要： A polymeric prodrug is described which comprises at least one polymer attached via at least one permanent bond to a bicine linker. The bicine linker is attached via a temporary linkage to an amine containing biologically active moiety. The amine containing biologically active moiety—such as a drug—can be released by cleaving the temporary linkage.

    摘要翻译： 描述了包含至少一种通过至少一个永久键连接到双链接头的聚合物的聚合物前药。 双连接体通过临时连接连接到含胺的生物活性部分上。 含有生物活性部分的胺（如药物）可通过切断临时连接而释放。

    High-Loading Water-Soluable Carrier-Linked Prodrugs
    9.
    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

    申请人： Ulrich Hersel ,  Guillaume Maitro ,  Harald Rau ,  Dirk Vetter

    发明人： Ulrich Hersel ,  Guillaume Maitro ,  Harald Rau ,  Dirk Vetter

    IPC分类号： A61K31/519 ,  A61K31/428 ,  A61K47/48

    CPC分类号： A61K31/519 ,  A61K31/428 ,  A61K47/60

    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。