PARTICULATE DRUG DELIVERY METHODS
    5.
    发明申请
    PARTICULATE DRUG DELIVERY METHODS 有权
    颗粒药物递送方法

    公开(公告)号:US20150314006A1

    公开(公告)日:2015-11-05

    申请号:US14530174

    申请日:2014-10-31

    摘要: Methods for efficient preparation of drug-polymer (or oligomer) conjugates useful in the preparation of particles, including microparticles and nanoparticles, for delivery of the drug in vivo for therapeutic applications are provided. The invention also provides nanoparticles prepared by nanoprecipitation using drug-polymer/oligomer conjugates of the invention. The drug conjugates are formed during polymerization of the polymer or oligomer in which the drug is employed as an initiator of the polymerization of the monomers which form the polymer and/or oligomer. More specifically, the drug conjugates are formed by ring-opening polymerization of cyclic monomers in the presence of an appropriate ring-opening polymerization catalyst and the initiator (the drug). The method is particularly useful for formation of polymer/oligomer conjugates with drugs and other chemical species containing one or more hydroxyl groups or thiol groups.

    摘要翻译: 提供了用于有效制备药物 - 聚合物(或低聚物)共轭物的方法,其用于制备颗粒,包括微粒和纳米颗粒,用于在体内递送药物用于治疗应用。 本发明还提供了使用本发明的药物 - 聚合物/低聚物共轭物通过纳米沉淀制备的纳米颗粒。 在聚合物或低聚物的聚合过程中形成药物共轭物,其中药物被用作形成聚合物和/或低聚物的单体聚合的引发剂。 更具体地说,通过在合适的开环聚合催化剂和引发剂(药物)的存在下,环状单体的开环聚合形成药物偶联物。 该方法特别适用于与含有一个或多个羟基或硫醇基团的药物和其它化学物质形成聚合物/低聚物缀合物。

    Immunoconjugates and humanized antibodies specific for B-cell lymphoma and leukemia cells
    9.
    发明申请
    Immunoconjugates and humanized antibodies specific for B-cell lymphoma and leukemia cells 审中-公开
    B细胞淋巴瘤和白血病细胞的免疫偶联物和人源化抗体

    公开(公告)号:US20040013607A1

    公开(公告)日:2004-01-22

    申请号:US10446689

    申请日:2003-05-29

    IPC分类号: A61K051/00 C07K016/46

    摘要: A chimeric LL2 monoclonal antibody is described in which the complementarity determining regions (CDRs) of the light and heavy chains of the murine LL2 anti-B-lymphoma, anti-leukemia cell monoclonal antibody has been recombinantly joined to the human kappa and IgG1 constant region domains, respectively, which retains the immunospecificity and B-cell lymphoma and leukemia cell internalization capacity of the parental murine LL2 monoclonal antibody, and which has the potential of exhibiting reduced human anti-mouse antibody production activity. A humanized LL2 monoclonal antibody is described in which the CDRs of the light and heavy chains have been recombinantly joined to a framework sequence of human light and heavy chains variable regions, respectively, and subsequently linked to human kappa and IgG1 constant region domains, respectively, which retains the immunospecificity and B-lymphoma and leukemia cell internalization capacities of the parental murine and chimeric LL2 monoclonal antibodies, and which has the potential for exhibiting reduced human anti-mouse antibody production activity. Vectors for producing recombinant chimeric and humanized chimeric monoclonal antibodies are provided. Isolated DNAs encoding the amino acid sequences of the LL2 variable light and heavy chain and CDR framework regions are described. Conjugates of chimeric and humanized chimeric LL2 antibodies with cytotoxic agents or labels find use in therapy and diagnosis of B-cell lymphomas and leukemias.

    摘要翻译: 描述了嵌合LL2单克隆抗体,其中鼠LL2抗B淋巴瘤,抗白血病细胞单克隆抗体的轻链和重链的互补决定区(CDR)已经重组连接到人类κ和IgG1恒定区 分别保留亲本鼠LL2单克隆抗体的免疫特异性和B细胞淋巴瘤和白血病细胞内化能力,其具有降低的人抗小鼠抗体生产活性的潜力。 描述了一种人源化的LL2单克隆抗体,其中轻链和重链的CDR分别重组连接到人轻链和重链可变区的框架序列上,并分别与人类κ和IgG1恒定区结构域连接, 其保留亲本鼠和嵌合LL2单克隆抗体的免疫特异性和B淋巴瘤和白血病细胞内化能力,并且其具有降低的人抗小鼠抗体产生活性的潜力。 提供了用于产生重组嵌合和人源化嵌合单克隆抗体的载体。 描述了编码LL2可变轻链和重链和CDR构架区的氨基酸序列的分离的DNA。 具有细胞毒性剂或标签的嵌合和人源化嵌合LL2抗体的缀合物可用于B细胞淋巴瘤和白血病的治疗和诊断。