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    CONJUGATES INCLUDING AN ANTIBODY MOIETY, A POLYPEPTIDE THAT TRAVERSES THE BLOOD-BRAIN BARRIER, AND A CYTOTOXIN
    84.
    发明公开
    CONJUGATES INCLUDING AN ANTIBODY MOIETY, A POLYPEPTIDE THAT TRAVERSES THE BLOOD-BRAIN BARRIER, AND A CYTOTOXIN 审中-公开
    包括抗体片段的缀合物，穿过血脑屏障的多肽和细胞毒素

    公开(公告)号：EP3218414A1

    公开(公告)日：2017-09-20

    申请号：EP15859337.6

    申请日：2015-11-13

    申请人： Angiochem Inc.

    发明人： DEMEULE, Michel ,  CHE, Christian ,  DAS, Sanjoy ,  YANG, Gaoqiang

    IPC分类号： C07K19/00 ,  A61K47/50 ,  A61P35/00 ,  C07K14/81 ,  C07K16/28

    CPC分类号： A61K39/395 ,  A61K39/39558 ,  A61K47/6803 ,  A61K47/6855 ,  A61K47/6869 ,  A61K47/6883 ,  A61K47/6885 ,  C07K14/8117 ,  C07K16/32 ,  C07K2319/00

    摘要： The present invention relates to antibody-polypeptide-cytotoxin conjugates and methods of making, packaging, and using the conjugates. The polypeptide can be a Kunitz-type protease inhibitor or a derivative thereof that facilitates transport of the conjugate across the blood-brain barrier and/or into cancer cells outside the CNS, and the antibody moiety selectively binds a target within the CNS or in peripheral tumors to direct the cytotoxic agent to that target (e.g., a tumor or cancer cell). The conjugates can be further defined by the inclusion of a linker between the antibody moiety and the polypeptide; by the number of polypeptides and cytotoxic agents conjugated thereto; by the positions at which the entities within the conjugates are bound to one another; and by the larger configuration of the conjugate. Modified polypeptides (e.g., polypeptides conjugated to cytotoxic agents but not to an anti-body moiety), pharmaceutical compositions, kits (e.g., including a modified polypeptide and an as-yet unconjugated antibody), and methods of making and using the conjugates are also features of the invention.

    摘要翻译： 本发明涉及抗体 - 多肽 - 细胞毒素缀合物以及制造，包装和使用缀合物的方法。 多肽可以是Kunitz型蛋白酶抑制剂或其衍生物，其有助于缀合物穿过血脑屏障和/或进入CNS外的癌细胞，并且抗体部分选择性地结合CNS内或外周 肿瘤将细胞毒素剂引导至该靶标（例如肿瘤或癌细胞）。 缀合物可以通过包含抗体部分和多肽之间的接头进一步定义; 通过与其缀合的多肽和细胞毒性剂的数量; 由共轭物中的实体相互结合的位置决定; 并通过缀合物的较大配置。 经修饰的多肽（例如与细胞毒剂偶联但不与抗体部分缀合的多肽），药物组合物，试剂盒（例如，包括修饰的多肽和尚未偶联的抗体）以及制备和使用缀合物的方法也是 本发明。

    SHORT AND D-AMINO ACID-CONTAINING POLYPEPTIDES FOR THERAPEUTIC CONJUGATES AND USES THEREOF
    85.
    发明授权
    SHORT AND D-AMINO ACID-CONTAINING POLYPEPTIDES FOR THERAPEUTIC CONJUGATES AND USES THEREOF 有权
    短期和D-氨基酸，多肽含治疗性偶联物及其用途

    公开(公告)号：EP2588490B1

    公开(公告)日：2017-02-22

    申请号：EP11800042.1

    申请日：2011-07-04

    申请人： Angiochem Inc.

    发明人： CASTAIGNE, Jean-Paul ,  DEMEULE, Michel ,  CHE, Christian ,  THIOT, Carine ,  PESLHERBE, Laurence

    IPC分类号： C07K7/06 ,  C07K7/08 ,  C07K14/81

    CPC分类号： A61K47/6811 ,  A61K38/10 ,  A61K38/185 ,  A61K38/2264 ,  A61K38/2278 ,  A61K47/64 ,  C07K14/8117 ,  C07K2319/00 ,  Y02A50/463

    摘要： The present invention relates to short polypeptides (e.g., fewer than 19 amino acids in length) and longer polypeptides (e.g., 19 or more amino acids in length) having one or more D-amino acids as targeting moieties. These polypeptides, when conjugated to agents (e.g., therapeutic agents or transport vectors) are capable of transporting the agents across the BBB or into particular cell types. In particular, the short polypeptides can include one or more D-amino acids. These compounds are therefore particularly useful in the treatment of neurological diseases or diseases associated with particular cell types, organs, or tissues.

    摘要翻译： 本发明涉及短多肽（E. G.，长度小于19个氨基酸）和更长的多肽（E. G.，19或在长度多个氨基酸），其具有一个或多个D-氨基酸作为靶向部分。 这些多肽当缀合至药物（E. G.，治疗剂或运输载体）能够运输穿过BBB或进入特定细胞类型的试剂。 特别地，所述短多肽可以包括一个或多个D-氨基酸。 这些化合物可用于治疗。因此与特定细胞类型，器官或组织有关的神经性疾病或疾病特别有用。