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    RNAi PHARMACEUTICAL COMPOSITION FOR SUPPRESSING EXPRESSION OF KRAS GENE
    1.
    发明申请
    RNAi PHARMACEUTICAL COMPOSITION FOR SUPPRESSING EXPRESSION OF KRAS GENE 有权
    用于抑制KRAS基因表达的RNAi药物组合物

    公开(公告)号：US20140044755A1

    公开(公告)日：2014-02-13

    申请号：US13943038

    申请日：2013-07-16

    申请人： Kyowa Hakko Kirin Co., Ltd. ,  DICERNA PHARMACEUTICALS, INC.

    发明人： Tomoyuki NAOI ,  Takeshi KUBOYAMA ,  Junichi ENOKIZONO ,  Toshihiko ISHII ,  Akihiro TOKUNAGA ,  Kentarou HATANAKA

    IPC分类号： A61K47/22 ,  A61K47/48 ,  A61K31/713

    CPC分类号： A61K47/22 ,  A61K9/0019 ,  A61K9/1272 ,  A61K31/713 ,  C12N15/1135 ,  C12N2310/14 ,  C12N2320/32

    摘要： The present invention provides a composition for suppressing the expression of a KRAS gene, comprising a lipid particle containing, as a drug, a double-stranded nucleic acid having an antisense strand having a sequence of bases complementary to the sequence of at least 19 continuous bases of any one KRAS gene's mRNA of sequence Nos. 1 to 3; anda cationic lipid represented by the following formula (I): wherein R1 and R2, which are the same or different, are each linear or branched alkyl, alkenyl or alkynyl having a carbon number of from 12 to 24; L1 and L2, which are the same or different, are each —CO—O— or —O—CO—; a and b, which are the same or different, are each 1 to 3; and R3 is a hydrogen atom, alkyl having a carbon number of from 1 to 6, or alkenyl having a carbon number of from 3 to 6, and the like.

    摘要翻译： 本发明提供了一种用于抑制KRAS基因表达的组合物，其包含含有作为药物的双链核酸的脂质颗粒，所述双链核酸具有具有与至少19个连续碱基的序列互补的碱基序列的反义链 任何一个KRAS基因的序列号1至3的mRNA; 和由下式（I）表示的阳离子脂质：其中相同或不同的R 1和R 2各自为碳数为12至24的直链或支链烷基，烯基或炔基; L1和L2各自相同或不同，分别为-CO-O-或-O-CO-; a和b相同或不同，分别为1〜3; 并且R 3是氢原子，碳数为1至6的烷基或碳数为3至6的烯基等。

    CATIONIC LIPID
    3.
    发明申请
    CATIONIC LIPID 审中-公开
    阳离子脂

    公开(公告)号：US20140294978A1

    公开(公告)日：2014-10-02

    申请号：US14206193

    申请日：2014-03-12

    申请人： Kyowa Hakko Kirin Co., Ltd.

    发明人： Takeshi KUBOYAMA ,  Kaori YAGI ,  Tomoyuki NAOI ,  Tomohiro ERA

    IPC分类号： A61K47/18 ,  A61K47/48

    CPC分类号： A61K47/543 ,  A61K9/127 ,  A61K48/0025 ,  C12N15/111 ,  C12N2310/14 ,  C12N2320/32

    摘要： The present invention provides a cationic lipid and the like. The cationic lipid is for delivering a medicament containing a cationic lipid which facilitates the introduction of a nucleic acid into a cell or the like, and is represented by formula (I). In the formula, R1 is linear or branched alkyl, alkenyl, or alkynyl, each having 8 to 24 carbon atoms, R2 is linear or branched alkyl, alkenyl, or alkynyl, each having 8 to 24 carbon atoms, or alkoxyethylene, alkoxypropylene, alkenyloxyethylene, alkenyloxypropylene, alkynyloxyethylene, or alkynyloxypropylene, R3 and R4 may be the same or different, and are each alkyl having 1 to 3 carbon atoms or are combined together to form alkylene having 2 to 6 carbon atoms, or R3 and R5 are combined together to form alkylene having 2 to 6 carbon atoms, R5 is a hydrogen atom, alkyl having 1 to 6 carbon atoms, alkenyl having 3 to 6 carbon atoms, amino, monoalkylamino, hydroxy, alkoxy, carbamoyl, monoalkylcarbamoyl, dialkylcarbamoyl, or the like, or is combined together with R3 to form alkylene having 2 to 6 carbon atoms, X is alkylene having 1 to 6 carbon atoms, and Y is a single bond, alkylene having 1 to 6 carbon atoms, or the like.

    摘要翻译： 本发明提供阳离子脂质等。 阳离子脂质用于递送含有阳离子脂质的药物，其有利于将核酸引入细胞等，并由式（I）表示。 式中，R 1为碳原子数为8〜24的直链或支链烷基，链烯基或炔基，R2为碳原子数为8〜24的直链或支链烷基，链烯基或炔基，或烷氧基亚乙基，烷氧基亚丙基， ，链烯氧基亚丙基，炔氧基亚乙基或炔氧基丙烯，R 3和R 4可以相同或不同，并且各自是具有1至3个碳原子的烷基，或者组合在一起形成具有2至6个碳原子的亚烷基，或者R 3和R 5结合在一起至 形成具有2至6个碳原子的亚烷基，R5是氢原子，具有1至6个碳原子的烷基，具有3至6个碳原子的烯基，氨基，单烷基氨基，羟基，烷氧基，氨基甲酰基，单烷基氨基甲酰基，二烷基氨基甲酰基等，或 与R3结合形成碳原子数2〜6的亚烷基，X为碳原子数为1〜6的亚烷基，Y为单键，碳原子数1〜6的亚烷基等。

    LIPID NANO PARTICLES COMPRISING COMBINATION OF CATIONIC LIPID
    9.
    发明申请
    LIPID NANO PARTICLES COMPRISING COMBINATION OF CATIONIC LIPID 审中-公开
    包含阳离子脂肪组合的脂质纳米颗粒

    公开(公告)号：US20140045913A1

    公开(公告)日：2014-02-13

    申请号：US13711909

    申请日：2012-12-12

    申请人： KYOWA HAKKO KIRIN CO., LTD.

    发明人： Takeshi KUBOYAMA ,  Tomohiro ERA ,  Tomoyuki NAOI

    IPC分类号： A61K47/22 ,  A61K47/18 ,  A61K31/713

    CPC分类号： A61K47/22 ,  A61K9/5123 ,  A61K31/713 ,  A61K47/18 ,  C07C211/21 ,  C07D207/12 ,  C12N15/88

    摘要： The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X3 is absent or is alkyl, etc, X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y1 is absent or anion, L1 is a single bond, etc, R3 is alkyl, etc), and a cationic lipid represented by formula (II) (wherein: R4 and R5 are, the same or different, alkenyl, etc, and X4 and X5 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X6 is absent or is alkyl, etc, Y2 is absent or anion, a and b are, the same or different, 0 to 3, and L4 is a single bond, etc, R6 is alkyl, etc, L2 and L3 are —O—, —CO—O— or —O—CO—), and the like.

    摘要翻译： 本发明提供一种脂质纳米颗粒，其允许将核酸容易地引入细胞，其包含由式（I）表示的阳离子脂质（其中：R1和R2相同或不同，烯基等，X3 或者是烷基等，X1和X2是氢原子，或者组合在一起形成单键或亚烷基，Y1不存在或阴离子，L1是单键等，R3是烷基等），和 由式（II）表示的阳离子脂质（其中：R4和R5为相同或不同的烯基等，X4和X5为氢原子，或组合在一起形成单键或亚烷基，X 6不存在 或烷基等，Y2不存在或阴离子，a和b相同或不同，0〜3，L4为单键等，R6为烷基等，L2和L3为-O-， - CO-O-或-O-CO-）等。