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    CATIONIC OLIGONUCLEOTIDES, AUTOMATED METHODS FOR PREPARING SAME AND THEIR USES
    1.
    发明申请
    CATIONIC OLIGONUCLEOTIDES, AUTOMATED METHODS FOR PREPARING SAME AND THEIR USES 有权
    阳离子低聚物，用于制备它们的自动化方法及其用途

    公开(公告)号：US20160280728A1

    公开(公告)日：2016-09-29

    申请号：US14745871

    申请日：2015-06-22

    申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITE DE STRASBOURG ,  POLYPLUS TRANSFECTION

    发明人： Jean-Paul BEHR ,  Mitsuharu KOTERA ,  Benedicte PONS ,  Emilie VOIRIN ,  Jean-Serge REMY

    IPC分类号： C07F9/22

    CPC分类号： C07F9/22 ,  A61K47/59 ,  A61K48/0041 ,  C07H21/00 ,  C12N15/88

    摘要： The invention relates to oligonucleotide-oligocation molecules AiBjH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein .Ai is an i-mer oligonucleotide residue, with i=5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical modifications or substitutions such as phosphorothioate, 2′-fluoro, 2′-O-alkyl, or a marker group such as a fluorescent agent, .Bj is a j-mer organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising .—HPO3—R1—(X—R2n)n1—X—R3—O—, where R1, R2n and R3, identical or different, are lower alkylene, X is NH or NC(NH2)2, n varies from 1 to 5 and n1=2 to 20, .—HPO3—R4—CH(R5X1)—R6—O—, where R4 is lower alkylene, R5 and R6, identical or different, are lower alkylene and X1 is putrescine, spermidine or spermine residue, .—HPO3—R7-(aa)n2-R8—O—, where R7 is lower alkylene and R8 is lower alkylene, serine, a natural aminoalcohol, (aa)n2 is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, -Histidine, Diaminopropionic acid and n2=2 to 20.

    摘要翻译： 本发明涉及可以通过自动亚磷酰胺化学合成寡核苷酸寡聚分子AiBjH，其具有寡核苷酸部分A 1和寡聚核苷酸部分B j，其中A i是i = 5至50的i-mer寡核苷酸残基，其中核苷酸A为低聚物 与天然或非天然存在的核碱基和/或五五烷酰基基团和/或天然磷酸二酯键，例如选自脱氧核糖核酸，核糖体，锁定（LNA）核苷酸以及它们的化学修饰或取代，例如硫代磷酸酯， 氟，2'-O-烷基或标记基团，例如荧光剂.Bj是j-mer有机寡核苷酸部分，其中j = 1-50，其中B选自包含-HPO 3 -R 1 - （X-R2n）n1-X-R3-O-，其中R1，R2n和R3相同或不同，为低级亚烷基，X为NH或NC（NH2）2，n为1至5，n1 = 2 至20，-HPO 3 -R 4 -CH（R 5 X 1）-R 6 -O-，其中R 4是低级亚烷基 e，R5和R6相同或不同，是低级亚烷基，X 1是腐胺，亚精胺或精胺残基。-HPO 3-R7-（aa）n 2 -R 8 -O-，其中R 7是低级亚烷基，R 8是低级亚烷基， 丝氨酸，天然氨基醇，（aa）n2是含有阳离子侧链的天然氨基酸的肽，例如精氨酸，赖氨酸，鸟氨酸，组氨酸，二氨基丙酸，n2 = 2〜20。

    CYCLOHEXENYL NUCLEIC ACIDS ANALOGS
    7.
    发明申请
    CYCLOHEXENYL NUCLEIC ACIDS ANALOGS 有权
    环己酮类核酸类似物

    公开(公告)号：US20110172294A1

    公开(公告)日：2011-07-14

    申请号：US13063917

    申请日：2009-09-23

    申请人： Punit P. Seth ,  Eric E. Swayze

    发明人： Punit P. Seth ,  Eric E. Swayze

    IPC分类号： A61K31/712 ,  C12N5/00 ,  C07F9/24 ,  C07H21/04 ,  C12Q1/68 ,  A61P35/00

    CPC分类号： C07F9/24 ,  C07D239/47 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07F9/22 ,  C07F9/6512 ,  C07F9/65616 ,  C07H19/04 ,  C07H21/00

    摘要： The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

    摘要翻译： 本公开描述了环己烯基核酸类似物，由其制备的低聚化合物和使用低聚化合物的方法。 更具体地，提供具有一个或多个手性取代基的环己烯基核酸类似物，其预期可用于增强低聚化合物的性质，包括核酸酶抗性和结合亲和力。 在一些实施方案中，本文提供的寡聚化合物与靶RNA的一部分杂交，导致靶RNA的正常功能丧失。