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    CATIONIC LIPID
    6.
    发明公开
    CATIONIC LIPID 审中-公开
    阳离子脂质

    公开(公告)号：EP3252043A1

    公开(公告)日：2017-12-06

    申请号：EP16743545.2

    申请日：2016-01-29

    申请人： NOF Corporation ,  National University Corporation Hokkaido University

    发明人： NAKAI, Yuta ,  TANGE, Kota ,  AKITA, Hidetaka ,  HARASHIMA, Hideyoshi ,  TOGASHI, Ryohei ,  MIURA, Naoya ,  MAETA, Mio

    IPC分类号： C07D295/088 ,  A61K9/127 ,  A61K31/7088 ,  A61K45/00 ,  A61K47/22 ,  A61K48/00 ,  A61P43/00 ,  C07D311/00

    摘要： The present invention aims to provide a cationic lipid that can be used as a nucleic acid delivery carrier, a lipid membrane structure using a cationic lipid, a nucleic acid-introducing agent using a cationic lipid, and a method of achieving nucleic acid introduction by using a nucleic acid-introducing agent containing a cationic lipid. A lipid membrane structure containing a cationic lipid represented by the formula (1)

    wherein each symbol is as defined in the DESCRIPTION, is superior in the stability in blood and tumor accumulation property. A nucleic acid-introducing agent using the cationic lipid can achieve high nucleic acid delivery efficiency of nucleic acid to be delivered into the cytoplasm.

    摘要翻译： 本发明的目的在于提供可用作核酸递送载体的阳离子性脂质，使用阳离子脂质的脂质膜结构体，使用阳离子性脂质的核酸导入剂，以及使用阳离子脂质的核酸导入剂的使用方法 含有阳离子脂质的核酸引入剂。 包含由式（1）表示的阳离子脂质的脂质膜结构体，其中每个符号如说明书中所定义，在血液稳定性和肿瘤积聚性方面优异。 使用阳离子脂质的核酸引入剂可以实现待递送到细胞质中的核酸的高核酸递送效率。

    NOVEL CATIONIC LIPID EXHIBITING IMPROVED INTRACELLULAR DYNAMICS
    8.
    发明公开
    NOVEL CATIONIC LIPID EXHIBITING IMPROVED INTRACELLULAR DYNAMICS 审中-公开

    公开(公告)号：EP3778572A1

    公开(公告)日：2021-02-17

    申请号：EP19778026.5

    申请日：2019-03-25

    申请人： NOF Corporation ,  National University Corporation Chiba University

    发明人： NAKAI, Yuta ,  TANGE, Kota ,  YOSHIOKA, Hiroki ,  TAMAGAWA, Shinya ,  AKITA, Hidetaka ,  TANAKA, Hiroki ,  TAKATA, Nae ,  KONISHI, Manami ,  TAKAHASHI, Tatsunari

    IPC分类号： C07D211/22 ,  A61K47/22 ,  A61K48/00 ,  C07D405/14

    摘要： Provided are a cationic lipid having improved intracellular kinetics, a lipid membrane structure containing same, and use thereof.
    A cationic lipid represented by the formula (1)

    (in the formula (1),
    R 1a and R 1b are each independently an alkylene group having 1 - 6 carbon atoms,
    X a and X b are each independently a non-cyclic alkyl tertiary amino group having 1 - 6 carbon atoms and one tertiary amino group, or a cyclic alkylene tertiary amino group having 2 - 5 carbon atoms and 1 - 2 tertiary amino groups,
    R 2a and R 2b are each independently an alkylene group or an oxydialkylene group each having not more than 8 carbon atoms,
    Y a and Y b are each independently an ester bond, an amide bond, a carbamate bond, an ether bond or a urea bond,
    Z a and Z b are each independently a divalent group derived from an aromatic compound having 3 - 16 carbon atoms and at least one aromatic ring, and optionally having a hetero atom, and
    R 3a and R 3b are each independently a residue derived from a reaction product of a liposoluble vitamin having a hydroxyl group, and succinic anhydride or glutaric anhydride, or a residue derived from a reaction product of a sterol derivative having a hydroxyl group, and succinic anhydride or glutaric anhydride, or an aliphatic hydrocarbon group having 12 - 22 carbon atoms).