Pharmaceutical Composition Comprising Anti-Mirna Antisense Oligonucleotides
    1.
    发明申请
    Pharmaceutical Composition Comprising Anti-Mirna Antisense Oligonucleotides 有权
    包含抗Mirna反义寡核苷酸的药物组合物

    公开(公告)号:US20100286234A1

    公开(公告)日:2010-11-11

    申请号:US12295960

    申请日:2007-03-30

    摘要: The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 26 nucleobases which are complementary to human microRNAs selected from the group consisting of miR19b, miR21, miR122a, miR155 and miR375. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.

    摘要翻译: 本发明提供包含长度为8至26个核碱基的短单链寡核苷酸的药物组合物,其与选自miR19b,miR21,miR122a,miR155和miR375的人微小RNA互补。 短的寡核苷酸在减轻体内抑制miRNA方面特别有效。 发现将高亲和力核苷酸类似物并入寡核苷酸导致高度有效的抗微小RNA分子,其似乎通过与miRNA靶标形成几乎不可逆的双链体起作用,而不是基于RNA切割的机制,例如与 RNaseH或RISC。

    Pharmaceutical Composition
    3.
    发明申请
    Pharmaceutical Composition 审中-公开
    药物组成

    公开(公告)号:US20100004320A1

    公开(公告)日:2010-01-07

    申请号:US12296084

    申请日:2007-03-30

    IPC分类号: A61K31/7052 A61P43/00

    摘要: The invention provides pharmaceutical compositions comprising short single stranded oligonucleotides, of length of between 8 and 17 nucleobases which are complementary to human microRNAs. The short oligonucleotides are particularly effective at alleviating miRNA repression in vivo. It is found that the incorporation of high affinity nucleotide analogues into the oligonucleotides results in highly effective anti-microRNA molecules which appear to function via the formation of almost irreversible duplexes with the miRNA target, rather than RNA cleavage based mechanisms, such as mechanisms associated with RNaseH or RISC.

    摘要翻译: 本发明提供药物组合物,其包含与人微小RNA互补的长度为8至17个核碱基的短单链寡核苷酸。 短的寡核苷酸在减轻体内抑制miRNA方面特别有效。 发现将高亲和力核苷酸类似物并入寡核苷酸导致高度有效的抗微小RNA分子,其似乎通过与miRNA靶标形成几乎不可逆的双链体起作用,而不是基于RNA切割的机制,例如与 RNaseH或RISC。

    LNA MODIFIED PHOSPHOROTHIOLATED OLIGONUCLEOTIDES
    4.
    发明申请
    LNA MODIFIED PHOSPHOROTHIOLATED OLIGONUCLEOTIDES 审中-公开
    LNA改性磷酸酯化寡核苷酸

    公开(公告)号:US20090176977A1

    公开(公告)日:2009-07-09

    申请号:US12162142

    申请日:2007-01-29

    IPC分类号: C07H21/02

    CPC分类号: C07H19/16 C07H19/06

    摘要: The current invention provides oligonucleotides which comprise a dinucleotide consisting of a 5′ locked nucleic acid (LNA), a phosphorothioate internucleoside linkage bond to a 3′ RNA or RNA analogue. The dinucleotide reduces the strength of hybridization of the oligonucleotide to a complementary nucleic acid target. The modification can be used to modulate hybridisation properties in both single stranded oligonucleotides and in double stranded siRNA complexes, particularly in oligonucleotides where the use of LNA results in excessively strong hybridisation properties.

    摘要翻译: 本发明提供了包含由5'锁定核酸(LNA),与3'RNA或RNA类似物的硫代磷酸核苷间键合键的二核苷酸的寡核苷酸。 二核苷酸降低寡核苷酸与互补核酸靶的杂交强度。 该修饰可用于调节单链寡核苷酸和双链siRNA复合物中的杂交性质,特别是在使用LNA导致过强的杂交性质的寡核苷酸中。