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    Bivalent linkers and conjugates thereof
    4.
    发明授权
    Bivalent linkers and conjugates thereof 有权

    公开(公告)号：US10647676B2

    公开(公告)日：2020-05-12

    申请号：US16444786

    申请日：2019-06-18

    申请人： Endocyte, Inc.

    发明人： Iontcho R. Vlahov ,  Christopher P. Leamon ,  Apparao Satyam ,  Stephen J. Howard

    IPC分类号： C07D213/71 ,  C07D401/12 ,  C07D475/04 ,  A61K49/00 ,  A61K47/55 ,  A61K47/68

    摘要： This invention pertains to bivalent linkers, and the synthesis and use thereof. In particular, this invention pertains to the synthesis and use of bivalent linkers in preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates. The present invention includes divalent linkers, which are alternatively referred to as bivalent linkers, that may be used to couple, link, bond, attach, or otherwise associate two or more chemical entities. This coupling, linking, attachment, or association may be used in the formation of conjugates of such chemical entities. Those chemical entities include targeting ligands and receptor-binding ligands, such as vitamins. Those chemical entities also include drugs for treating various diseases or disease states, and imaging and diagnostic agents for diagnosing, detecting, or otherwise monitoring various diseases or disease states.

    VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES
    7.
    发明申请
    VITAMIN RECEPTOR BINDING DRUG DELIVERY CONJUGATES 审中-公开
    维生素B受体结合药物联合用药

    公开(公告)号：US20140058063A1

    公开(公告)日：2014-02-27

    申请号：US13785523

    申请日：2013-03-05

    申请人： ENDOCYTE, INC.

    发明人： Iontcho R. Vlahov ,  Christopher P. Leamon ,  Matthew A. Parker ,  Stephen J. Howard ,  Hari Krishna R. Santhapuram ,  Apparao Satyam ,  Joseph A. Reddy

    IPC分类号： A61K47/48

    CPC分类号： A61K47/55 ,  A61K47/551 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/55

    摘要： The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety includes vitamins, and vitamin receptor binding analogs and derivatives thereof, and the drug includes analogs and derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) includes components such as spacer linkers, releasable linkers, and heteroatom linkers, and combinations thereof. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

    摘要翻译： 本发明描述了维生素受体结合药物递送缀合物及其制备方法。 药物递送缀合物由维生素受体结合部分，二价连接体（L）和药物组成。 维生素受体结合部分包括维生素和维生素受体结合类似物及其衍生物，并且该药物包括其类似物及其衍生物。 维生素受体结合部分与二价连接体共价连接，药物或其类似物或衍生物与二价连接体共价连接，其中二价连接体（L）包括组分如间隔连接子，可释放接头， 和杂原子接头，及其组合。 还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。