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1. 发明申请

WO2009054551A2 LIPID-MODIFIED DOUBLE-STRANDED RNA HAVING POTENT RNA INTERFERENCE EFFECT 审中-公开
标题翻译：脂质修饰双链RNA具有RNA干扰效应
公开(公告)号：WO2009054551A2
公开(公告)日：2009-04-30
申请号：PCT/JP2008/069829
申请日：2008-10-24
申请人： NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE AND TECHNOLOGY , OTSUKA PHARMACEUTICAL CO., LTD. , HAYASHI KASEI CO., LTD. , KUBO, Takanori , OHBA, Hideki , TOYOBUKU, Hidekazu , HAYASHI, Hirotake
发明人： KUBO, Takanori , OHBA, Hideki , TOYOBUKU, Hidekazu , HAYASHI, Hirotake
IPC分类号： A61K47/48
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/543
摘要： An object of the present invention is to provide a novel double-stranded RNA that has high nuclease resistance and high cellular uptake efficiency, and that is capable of producing an excellent RNA interference effect. The present invention provides a lipid-modified double-stranded RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of inhibiting the expression of the target gene, the sense strand having a lipid linked to at least one of the first to sixth nucleotides from the 5' end side directly or via a linker.
摘要翻译：本发明的目的是提供具有高核酸酶抗性和高细胞摄取效率的新型双链RNA，并能够产生优异的RNA干扰效果。本发明提供脂质修饰的双链RNA，其包含具有与靶序列互补的核苷酸序列的有义链和具有与有义链互补的核苷酸序列的反义链，所述双链RNA能够抑制靶基因的表达，有义链具有从5'末端侧的至少一个第一至第六个核苷酸直接或通过连接体连接的脂质。

2. 发明公开

EP2264167A1 DOUBLE-STRANDED LIPID-MODIFIED RNA HAVING HIGH RNA INTERFERENCE EFFECT 有权
标题翻译： DOPPELSTRÄNGIGE脂质变性RNA麻醉HOHEM RNA-INTERFERENZEFFEKT
公开(公告)号：EP2264167A1
公开(公告)日：2010-12-22
申请号：EP09729165.2
申请日：2009-03-31
申请人： National Institute of Advanced Industrial Science and Technology , Otsuka Pharmaceutical Co., Ltd. , Hayashi Kasei Co., Ltd.
发明人： KUBO, Takanori , OHBA, Hideki , TOYOBUKU, Hidekazu , HAYASHI, Hirotake
IPC分类号： C12N15/09 , A61K31/7088 , A61K48/00
CPC分类号： C12N15/111 , C12N2310/3515 , C12N2320/32
摘要： An object of the present invention is to provide a novel double-stranded RNA that has high resistance to nuclease and cellular uptake efficiency and that can produce an excellent RNA interference effect. The present invention provides a double-stranded lipid-modified RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence in a target gene, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of suppressing the expression of the target gene, and the sense strand having a double-stranded lipid bound directly or via a linker to at least one of the first to sixth nucleotides from the 5' end.
摘要翻译：本发明的目的是提供对核酸酶和细胞摄取效率具有高抗性并且可以产生优异的RNA干扰效果的新型双链RNA。本发明提供了包含具有与靶基因中的靶序列互补的核苷酸序列的有义链和具有与有义链互补的核苷酸序列的反义链的双链脂质修饰的RNA，所述双链RNA为能够抑制靶基因的表达，并且具有直链或经由连接体结合至5'末端的至少一个第一至第六个核苷酸的双链脂质的有义链。

3. 发明授权

EP2264167B1 DOUBLE-STRANDED LIPID-MODIFIED RNA HAVING HIGH RNA INTERFERENCE EFFECT 有权
标题翻译：双链脂质修饰RNA高RNA干扰作用
公开(公告)号：EP2264167B1
公开(公告)日：2016-10-12
申请号：EP09729165.2
申请日：2009-03-31
申请人： National Institute of Advanced Industrial Science and Technology , Otsuka Pharmaceutical Co., Ltd.
发明人： KUBO, Takanori , OHBA, Hideki , TOYOBUKU, Hidekazu , HAYASHI, Hirotake
IPC分类号： C12N15/09 , A61K31/7088 , A61K48/00
CPC分类号： C12N15/111 , C12N2310/3515 , C12N2320/32

4. 发明公开

EP2217284A2 LIPID-MODIFIED DOUBLE-STRANDED RNA HAVING POTENT RNA INTERFERENCE EFFECT 审中-公开
标题翻译：与有效RNA干扰效应的脂质修饰的双链RNA
公开(公告)号：EP2217284A2
公开(公告)日：2010-08-18
申请号：EP08841497.4
申请日：2008-10-24
申请人： National Institute of Advanced Industrial Science And Technology , Otsuka Pharmaceutical Co., Ltd.
发明人： KUBO, Takanori , OHBA, Hideki , TOYOBUKU, Hidekazu , HAYASHI, Hirotake
IPC分类号： A61K47/48
CPC分类号： A61K47/48038 , A61K47/542 , A61K47/543
摘要： An object of the present invention is to provide a novel double-stranded RNA that has high nuclease resistance and high cellular uptake efficiency, and that is capable of producing an excellent RNA interference effect. The present invention provides a lipid-modified double-stranded RNA comprising a sense strand having a nucleotide sequence complementary to a target sequence, and an antisense strand having a nucleotide sequence complementary to the sense strand, the double-stranded RNA being capable of inhibiting the expression of the target gene, the sense strand having a lipid linked to at least one of the first to sixth nucleotides from the 5′ end side directly or via a linker.

5. 发明公开

EP2226384A1 COMPLEX OF POLYSACCHARIDE AND DOUBLE-STRANDED RNA 有权转让
标题翻译： KOMPLEX AUS POLYSACCHARID UND DOPPELSTRANG-RNA
公开(公告)号：EP2226384A1
公开(公告)日：2010-09-08
申请号：EP08862702.1
申请日：2008-12-18
申请人： National Institute of Advanced Industrial Science and Technology , Napa Jenomics Co., Ltd.
发明人： KUBO, Takanori , OHBA, Hideki , SAKURAI, Kazuo , MINARI, Jusaku , UNO, Atsushi
IPC分类号： C12N15/09
CPC分类号： C12N15/111 , C12N2310/14 , C12N2310/3519 , C12N2320/32 , C12N2320/51
摘要： An object of the present invention is to provide novel double-stranded RNA having an RNA interference effect, in which the cellular uptake and the resistance to enzymatic degradation are improved, without reducing the RNA interference effect.
The cellular uptake and the resistance to enzymatic degradation of a complex of a polysaccharide having a β-1,3-glucan skeleton and double-stranded RNA can be significantly improved while maintaining the RNA interference effect, by fulfilling the following conditions (i) to (iii): (i) the double-stranded RNA has a sense strand consisting of a base sequence complementary to a target sequence in a target gene and an antisense strand containing a base sequence complementary to the sense strand, and the double-stranded RNA can inhibit expression of the target gene; (ii) the double-stranded RNA has a single-stranded polydeoxyadenine bound directly or via a linker to the end of at least one of the sense strand and the antisense strand; and (iii) the polysaccharide and the single-stranded polydeoxyadenine form a complex.
摘要翻译：本发明的目的是提供具有RNA干扰作用的新型双链RNA，其中细胞摄取和对酶降解的抗性得到改善，而不降低RNA干扰效应。通过满足以下条件，可以显着改善具有2-1,3-葡聚糖骨架和双链RNA的多糖的复合物的细胞摄取和耐酶降解，同时保持RNA干扰效应（i）至（iii）：（i）双链RNA具有由与靶基因中的靶序列互补的碱基序列的有义链和含有与有义链互补的碱基序列的反义链，双链RNA 可抑制靶基因的表达; （ii）双链RNA具有单链多脱氧腺嘌呤，其直接或经由接头连接至至少一个有义链和反义链的末端; 和（iii）多糖和单链多脱氧腺嘌呤形成复合物。

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