MONOFUNCTIONAL BRANCHED POLYETHYLENEGLYCOL AND BIO-RELATED SUBSTANCE MODIFIED BY SAME
    5.
    发明公开
    MONOFUNCTIONAL BRANCHED POLYETHYLENEGLYCOL AND BIO-RELATED SUBSTANCE MODIFIED BY SAME 有权
    MONOFUNKTIONELLES VERZWEIGTES POLYETHYLENGLYCOL UND DAMIT MODIFIZIERTE BIOBEZOGENE SUBSTANZ

    公开(公告)号:EP2947111A1

    公开(公告)日:2015-11-25

    申请号:EP13871951.3

    申请日:2013-03-29

    摘要: Disclosed are a monofunctional branched polyethyleneglycol and a bio-related substance modified by same. The general formula of the monofunctional branched polyethyleneglycol is shown in Formula (1), and the general formula of the bio-related substance modified by the polyethyleneglycol is shown in Formula (2), wherein X 1 and X 2 are respectively an alkyl group with 1 to 20 carbon atoms; n 1 and n 2 are respectively an integer ranging from 1 to 1000; n 3 is an integer ranging from 11 to 1000; L 1 and L 2 are respectively a linking group stably existing in illumination, enzyme, acidic, or alkaline conditions; p is 0 or 1, and q is 0 or 1; R1 is a hydrogen atom or an alkyl group with 1 to 20 carbon atoms; D is the bio-related substance; and Z is a linking group, through which a functional group capable of reacting with the bio-related substance is linked to a symmetric axis polyethyleneglycol main chain. The bio-related substance modified by the polyethyleneglycol maintains good biological activity, and has good solubility and long metabolic half-life in an organism.

    摘要翻译: 公开了单官能支化聚乙二醇和通过其改性的生物相关物质。 单官能支化聚乙二醇的通式如式(1)所示,由聚乙二醇改性的生物相关物质的通式示于式(2)中,其中X 1和X 2分别为具有 1至20个碳原子; n 1和n 2分别为1〜1000的整数; n 3为11〜1000的整数, L 1和L 2分别是在照明,酶,酸性或碱性条件下稳定存在的连接基团; p为0或1,q为0或1; R1是氢原子或碳原子数为1〜20的烷基; D是生物相关物质; Z是与生物相关物质反应的官能团与对称轴聚乙二醇主链连接的连接基团。 由聚乙二醇修饰的生物相关物质保持良好的生物活性,并且在生物体中具有良好的溶解性和长的代谢半衰期。