Preparation of a polymer/interleukin-2 conjugate
    15.
    发明授权
    Preparation of a polymer/interleukin-2 conjugate 失效
    聚合物/白介素-2缀合物的制备

    公开(公告)号:US4902502A

    公开(公告)日:1990-02-20

    申请号:US299235

    申请日:1989-01-23

    IPC分类号: A61K47/48

    CPC分类号: A61K47/48215

    摘要: The present invention is a process for preparing a pharmaceutical composition comprising a biologically active conjugated protein. It comprises a polyethylene glycol or a polyoxyethylated polyol conjugated to IL-2. This protein is conjugated to reduce its immunogenicity, and increase it solubility, and increase its circulating in vivo half-life.

    摘要翻译: 本发明是一种制备包含生物活性共轭蛋白质的药物组合物的方法。 它包含与IL-2缀合的聚乙二醇或聚氧乙烯化多元醇。 这种蛋白质被缀合以降低其免疫原性,并增加其溶解度,并增加其体内循环体内的半衰期。

    Method of conjugating an activated ester to an amine-containing
biological material
    18.
    发明授权
    Method of conjugating an activated ester to an amine-containing biological material 失效
    将活化的酯与含胺生物材料共轭的方法

    公开(公告)号:US5663306A

    公开(公告)日:1997-09-02

    申请号:US95396

    申请日:1987-09-10

    摘要: A coupling agent which is an activated ester such as N-maleimido-6-aminocaproyl-HNSA (mal-sac-HNSA) is formed by reacting 4-hydroxyl-3-nitrobenzene sulfonic acid sodium salt (HNSA) with a carboxylic acid moiety of a compound such as N-maleimido-6-aminocaproic acid. The coupling agent is reacted with an amino group of an amine-containing biological material such as a protein at a pH of about 5.5 to 10.0 and HNSA is released. The released HNSA is spectroscopically measured at a wavelength of from about 350 nm to about 500 nm to precisely monitor and control conjugating of the coupling agent to the biological material. The resulting product is coupled to a sulfhydryl group or other group of another material to provide cross-linking between the two. This enables joining the biological material to one another, to a support matrix, to a label, to a hapten, and to other materials. An immunotoxin for therapeutic use can be prepared by conjugating the coupling agent to an antibody such as a monoclonal antibody with tumor cell specificity and then joining the resultant conjugate to a cytotoxic molecule.

    摘要翻译: 通过使4-羟基-3-硝基苯磺酸钠盐(HNSA)与羧酸部分的反应形成N-二异氰酸基-6-氨基己酰基-HNSA(mal-sac-HNSA)等活性酯的偶联剂 化合物如N-马来酰亚胺基-6-氨基己酸。 偶联剂与pH为5.5〜10.0左右的含胺生物材料如蛋白质的氨基反应,释放HNSA。 释放的HNSA在约350nm至约500nm的波长处进行光谱测量,以精确监测和控制偶联剂与生物材料的缀合。 将所得产物偶联至巯基或其它另一组材料以提供两者之间的交联。 这使得能够将生物材料彼此连接,支撑基质,标签,半抗原和其他材料。 用于治疗用途的免疫毒素可以通过将偶联剂与具有肿瘤细胞特异性的抗体(例如单克隆抗体)缀合,然后将所得缀合物连接到细胞毒性分子来制备。