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    REGULATION OF THE STABILITY OF RECOMBINANT PROTEINS AND ANTIBOODIES
    12.
    发明申请
    REGULATION OF THE STABILITY OF RECOMBINANT PROTEINS AND ANTIBOODIES 审中-公开
    调节重组蛋白和抗体的稳定性

    公开(公告)号：WO0050089A3

    公开(公告)日：2001-03-29

    申请号：PCT/US0004749

    申请日：2000-02-25

    Applicant: MINDSET BIOPHARMACEUTICALS USA ,  CHAIN DANIEL G

    Inventor： CHAIN DANIEL G

    IPC: A61K47/48 ,  C12N15/62 ,  C12N15/85

    CPC classification number: B82Y5/00 ,  A61K47/6897

    Abstract: An antibody to a drug of interest is caused to be expressed in a target cell of interest by genetic therapy. This antibody is expressed along with a promoter and modulator for the antibody. The drug is administered to the patient, where it binds to the antibody for the drug until a critical concentration of drug is reached at the target site. Once this critical concentration of drug is achieved, the antibody is released from the drug/antibody conjugate, and the drug is available at the target site in concentrations sufficient to treat the condition for which the drug is administered. In order to ensure that the antibodies are degraded at the proper time, the antibodies are designed to have built-in signals for degradation.

    Abstract translation: 使感兴趣的药物的抗体通过遗传治疗在靶细胞中表达。 该抗体与抗体的启动子和调节剂一起表达。 将药物施用于患者，其中其与药物的抗体结合，直到在靶位点达到临界浓度的药物。 一旦药物的这种临界浓度达到，抗体就会从药物/抗体结合物中释放出来，药物可以在靶位点以足以治疗药物给药条件的浓度获得。 为了确保抗体在适当的时间降解，设计抗体具有降解的内在信号。

    KIT FOR PRETARGETING AND NOVEL PRETARGETING CONJUGATES
    15.
    发明申请
    KIT FOR PRETARGETING AND NOVEL PRETARGETING CONJUGATES 审中-公开
    预付款和新款预付款套餐

    公开(公告)号：WO9600087A3

    公开(公告)日：1996-03-07

    申请号：PCT/EP9502425

    申请日：1995-06-22

    Applicant: AKZO NOBEL NV ,  BOS EBO SYBREN ,  KASPERSEN FRANCISCUS MICHAEL

    Inventor： BOS EBO SYBREN ,  KASPERSEN FRANCISCUS MICHAEL

    IPC: A61K47/48 ,  A61K51/10

    CPC classification number: B82Y5/00 ,  A61K47/665 ,  A61K47/6897 ,  A61K51/1093

    Abstract: The invention relates to a method of pretargeting therapeutic or diagnostic compounds to target cells in the body and a kit for such a method. The targeting is preferably through a specific antibody. The binding between the preinjected targeting moiety and the effector moiety is established by a zinc finger and its cognate nucleotide sequence, conjugated to the targeting or effector moiety. Also part of the invention are conjugates of zinc fingers and therapeutic or diagnostic compounds.

    Abstract translation: 本发明涉及将治疗或诊断化合物预靶向靶向体内细胞的方法和用于这种方法的试剂盒。 靶向优选通过特异性抗体。 预注射的靶向部分和效应部分之间的结合由锌指及其与靶向或效应子部分缀合的同源核苷酸序列建立。 本发明的一部分是锌指和治疗或诊断化合物的缀合物。

    ANTIBODIES REACTIVE WITH AN EPITOPE LOCATED IN THE N-TERMINAL REGION OF MUC5AC COMPRISING CYSTEINE-RICH SUBDOMAIN 2 (CYS2)
    17.
    发明申请
    ANTIBODIES REACTIVE WITH AN EPITOPE LOCATED IN THE N-TERMINAL REGION OF MUC5AC COMPRISING CYSTEINE-RICH SUBDOMAIN 2 (CYS2) 审中-公开
    位于包含CYSTEINE-RICH SUBDOMAIN 2（CYS2）的MUC5AC的N-末端区域的抗原决定簇的抗体反应

    公开(公告)号：WO2016003869A1

    公开(公告)日：2016-01-07

    申请号：PCT/US2015/038252

    申请日：2015-06-29

    Applicant: IMMUNOMEDICS, INC.

    Inventor： LIU, Donglin ,  CHANG, Chien-Hsing ,  GOLDENBERG, David, M.

    IPC: A61K39/00 ,  A61K39/395 ,  A61K51/10

    CPC classification number: A61K51/1057 ,  A61K31/7068 ,  A61K31/7105 ,  A61K38/00 ,  A61K45/06 ,  A61K47/6859 ,  A61K47/6897 ,  A61P35/00 ,  C07K16/303 ,  C07K16/3092 ,  C07K2317/72 ,  G01N33/57438 ,  G01N2333/4725 ,  A61K2300/00

    Abstract: The present invention concerns compositions and methods of use of antibodies or antibody fragments that bind to an epitope located within the second cysteine-rich domain (Cys2, amino acid residues 1575-1725) of MUC5AC. The antibodies bind with high specificity and selectivity to pancreatic cancer and are of use for therapy, detection and/or diagnosis of pancreatic cancer. In preferred embodiments, therapeutic antibody may be conjugated to at least one therapeutic agent, such as 90 Y. Both in vivo and in vitro detection of pancreatic cancer may be performed with the subject methods and compositions. Specific dosages of radiolabeled antibody and/or gemcitabine, of use in human pancreatic cancer patients, are disclosed herein.

    Abstract translation: 本发明涉及结合位于MUC5AC的第二富含半胱氨酸结构域（Cys2，氨基酸残基1575-1725）内的表位的抗体或抗体片段的组合物和方法。 该抗体以高特异性和对胰腺癌的选择性结合，并且可用于胰腺癌的治疗，检测和/或诊断。 在优选的实施方案中，治疗性抗体可以缀合至至少一种治疗剂，例如90Y。 胰腺癌的体内和体外检测都可以用本发明方法和组合物进行。 本文公开了在人胰腺癌患者中使用的放射性标记的抗体和/或吉西他滨的特定剂量。

    BIOORTHOGONAL TWO-COMPONENT DELIVERY SYSTEMS FOR ENHANCED INTERNALIZATION OF NANOTHERAPEUTICS
    18.
    发明申请
    BIOORTHOGONAL TWO-COMPONENT DELIVERY SYSTEMS FOR ENHANCED INTERNALIZATION OF NANOTHERAPEUTICS 审中-公开
    生物多功能双组分输送系统，用于增强纳米技术的内在化

    公开(公告)号：WO2014138186A1

    公开(公告)日：2014-09-12

    申请号：PCT/US2014/020620

    申请日：2014-03-05

    Applicant: THE JOHNS HOPKINS UNIVERSITY

    Inventor： HAPUARACHCHIGE, Sudath ,  ARTEMOV, Dmitri

    IPC: A61K9/16 ,  A61K49/06 ,  A61K49/08 ,  A61K47/48

    CPC classification number: A61K49/0056 ,  A61K47/60 ,  A61K47/643 ,  A61K47/6851 ,  A61K47/6889 ,  A61K47/6897 ,  A61K49/0002 ,  A61K49/0021 ,  A61K49/0041 ,  A61K49/0054

    Abstract: In accordance with one or more embodiments, the present invention provides a new strategy for an improved target-specific drug delivery that utilizes enhanced internalization of therapeutic conjugates by in situ complexation driven by bioorthogonal click chemistry, which is defined herein as "click therapy". This novel two-step/two-component system for intracellular delivery of therapeutics is based on the induced internalization of cross-linked and clustered mAb to target receptors of interest, including, for example, HER2 receptors. The system provides target-specific, and optionally, image-guided drug delivery, and highly efficient internalization and accumulation of chemotherapeutics in the target cells of interest. The present invention provides in situ complexation of two or more delivery components by the bioorthogonal click reactions between multiple azido-functionalized or tetrazine functionalized mAb and multiple cyclooctyne-functionalized nanocarriers, or trans- cyclooctene functionalization, and bovine serum albumin (BSA) substituted with chemotherapeutics, such as paclitaxel. The present invention provides copper-free, strained- promoted, bioorthogonal click chemistry for therapy.

    Abstract translation: 根据一个或多个实施方案，本发明提供了改进的靶特异性药物递送的新策略，其通过由本文定义为“点击治疗”的生物正交点击化学驱动的原位络合使用治疗性缀合物的增强内化。 这种用于细胞内递送治疗剂的新型两步/双组分系统是基于诱导的目的受体目标受体（包括例如HER2受体）的交联和聚集的mAb的内化。 该系统提供目标特异性和可选择的图像引导的药物递送，以及化学治疗剂在目标细胞中的高效内化和积累。 本发明通过多重叠氮官能化或四嗪功能化的单克隆抗体和多环辛烯功能化纳米载体之间的生物正交点击反应或反式环辛烯官能化和用化学治疗剂取代的牛血清白蛋白（BSA），提供两种或多种递送成分的原位络合 ，如紫杉醇。 本发明提供了用于治疗的无铜，应变促进的生物正交点击化学。

    BIO-ORTHOGONAL DRUG ACTIVATION
    19.
    发明申请
    BIO-ORTHOGONAL DRUG ACTIVATION 审中-公开
    生物正醛药物活化

    公开(公告)号：WO2014081301A1

    公开(公告)日：2014-05-30

    申请号：PCT/NL2013/050848

    申请日：2013-11-22

    Applicant: TAGWORKS PHARMACEUTICALS B.V.

    Inventor： ROBILLARD, Marc Stefan

    IPC: A61K47/48 ,  C07C13/00

    CPC classification number: A61K47/48246 ,  A61K31/704 ,  A61K47/48061 ,  A61K47/545 ,  A61K47/555 ,  A61K47/60 ,  A61K47/64 ,  A61K47/6897 ,  B82Y5/00 ,  C07K16/30 ,  C07K2317/626 ,  C07K2317/76

    Abstract: Disclosed is a kit for the administration and activation of a Prodrug. The kit comprises a Masking Moiety linked, directly or indirectly, to a Trigger moiety, which in turn is linked to a Drug, and an Activator for the Trigger moiety. The Trigger moiety comprises a dienophile and the Activator comprises a diene, whereby the dienophile is an eight-membered non- aromatic cyclic alkenylene group, preferably a cyclooctene group, and more preferably a trans-cyclooctene group. The Trigger and the Activator undergo a fast, bio-orthogonal reaction resulting in the release of the Masking Moiety, and activation of the drug.

    Abstract translation: 公开了用于给药和激活前药的试剂盒。 该试剂盒包括直接或间接连接到触发部分的掩蔽部分，触发部分又连接到药物和触发器部分的激活剂。 触发剂部分包含亲二烯体，活化剂包含二烯，其中亲双酯是八元非芳族环亚烯基，优选环辛烯基，更优选反式环辛烯基。 触发剂和活化剂经历快速，生物正交反应，导致掩蔽部位的释放和药物的活化。

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