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    NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY
    5.
    发明申请
    NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY 有权
    用于寡核苷酸交付的新型低分子量阳离子脂肪

    公开(公告)号：US20170022146A1

    公开(公告)日：2017-01-26

    申请号：US15282294

    申请日：2016-09-30

    申请人： SIRNA THERAPEUTICS, INC.

    发明人： Steven L. COLLETTI ,  Matthew G. STANTON

    IPC分类号： C07C229/12 ,  A61K31/221 ,  A61K9/51

    CPC分类号： C07C229/12 ,  A61K9/5123 ,  A61K31/221 ,  A61K48/00 ,  C12N15/88

    摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids comprising at least one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

    摘要翻译： 本发明提供了可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与寡核苷酸形成脂质纳米颗粒的新型阳离子脂质。 本发明的目的是提供一种阳离子脂质支架，由于肝中脂质水平降低，其表现出增强的功效以及较低的肝毒性。 本发明使用包含至少一个短脂链的低分子量阳离子脂质，以提高siRNA的体内递送的效率和耐受性。

    NOVEL SINGLE CHEMICAL ENTITIES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES
    8.
    发明申请
    NOVEL SINGLE CHEMICAL ENTITIES AND METHODS FOR DELIVERY OF OLIGONUCLEOTIDES 审中-公开
    新型单一化学实验和交付寡糖的方法

    公开(公告)号：US20160074525A1

    公开(公告)日：2016-03-17

    申请号：US14848118

    申请日：2015-09-08

    申请人： SIRNA THERAPEUTICS, INC.

    发明人： Steven L. COLLETTI ,  Francis GOSSELIN ,  Vasant R. JADHAV ,  Anthony W. SHAW ,  David M. TELLERS ,  Thomas J. TUCKER ,  Yu YUAN ,  Daniel ZEWGE

    IPC分类号： A61K47/48 ,  C12N15/113

    CPC分类号： C12N15/113 ,  A61K47/64 ,  C12N15/111 ,  C12N15/87 ,  C12N2310/14 ,  C12N2310/3513 ,  C12N2310/3515 ,  C12N2320/32

    摘要： In an embodiment the instant invention discloses a modular composition comprising 1) an oligonucleotide; 2) one or more linkers, which may be the same or different, selected from Table 1, wherein the linkers are attached to the oligonucleotide at the 2′-position of the ribose rings and/or the terminal 3′- and/or 5′-positions of the oligonucleotide; 3) optionally, one or more peptides, which may be the same or different, selected from SEQ ID NOs: 1-59, wherein the peptides are attached to the linkers; and optionally one or more lipids, solubilizing groups and/or targeting ligands attached to the oligonucleotide.

    摘要翻译： 在一个实施方案中，本发明公开了一种模块化组合物，其包含：1）寡核苷酸; 2）一个或多个可以相同或不同的接头，其选自表1，其中连接体在核糖环和/或末端3'-和/或5的2'-位上连接于寡核苷酸 寡核苷酸的位置; 3）任选的一个或多个可以相同或不同的选自SEQ ID NO：1-59的肽，其中肽连接到接头上; 和任选的一种或多种脂质，增溶基团和/或靶向与寡核苷酸连接的配体。