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21. 发明申请

US20120010271A1 SINGLE-STRANDED NUCLEIC ACID MOLECULE FOR CONTROLLING GENE EXPRESSION 有权
标题翻译：用于控制基因表达的单链核酸分子
公开(公告)号：US20120010271A1
公开(公告)日：2012-01-12
申请号：US13254150
申请日：2011-07-08
申请人： Tadaaki Ohgi , Hirotake Hayashi , Hisao Shirohzu , Tomohiro Hamasaki , Akihiro Itoh , Hiroshi Suzuki
发明人： Tadaaki Ohgi , Hirotake Hayashi , Hisao Shirohzu , Tomohiro Hamasaki , Akihiro Itoh , Hiroshi Suzuki
IPC分类号： A61K31/7088 , C12N5/00 , A61P43/00 , C07H21/04 , A61K31/7105 , A61K31/711 , C07H21/02 , C12N5/071
CPC分类号： C12N15/113 , A61K31/7105 , A61K31/7115 , A61K31/712 , A61K31/7125 , C12N15/111 , C12N2310/14 , C12N2320/30 , C12N2330/51
摘要： Provided is a novel nucleic acid molecule that can inhibit the expression of a gene and can be produces easily and efficiently. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes, in sequence from the 5′ side to the 3′ side: a 5′ side region (Xc); an inner region (Z); and a 3′ side region (Yc). The inner region (Z) is composed of an inner 5′ side region (X) and an inner 3′ side region (Y) that are linked to each other. The 5′ side region (Xc) is complementary to the inner 5′ side region (X). The 3′ side region (Yc) is complementary to the inner 3′ side region (Y). At least one of the inner region (Z), the 5′ side region (Xc), and the 3′ side region (Yc) includes the expression inhibitory sequence. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.
摘要翻译：提供了可以抑制基因表达并且可以容易且有效地产生的新型核酸分子。核酸分子是包含抑制靶基因表达的表达抑制性序列的单链核酸分子。单链核酸分子包括从5'侧到3'侧的顺序：5'侧区（Xc）; 内部区域（Z）; 和3'侧区域（Yc）。内部区域（Z）由彼此连接的内部5'侧区域（X）和内部3'侧区域（Y）构成。 5'侧区域（Xc）与内部5'侧区域（X）互补。 3'侧区域（Yc）与内3'侧区域（Y）互补。内部区域（Z），5'侧区域（Xc）和3'侧区域（Yc）中的至少一个包括表达抑制序列。根据该单链核酸分子，可以抑制靶基因的表达。

22. 发明授权

US07820629B2 Galactose derivative, drug carrier and medicinal composition 有权
标题翻译：半乳糖衍生物，药物载体和药用组合物
公开(公告)号：US07820629B2
公开(公告)日：2010-10-26
申请号：US12280778
申请日：2007-02-28
申请人： Tadaaki Ohgi , Toshihiro Ueda , Satoru Sonoke
发明人： Tadaaki Ohgi , Toshihiro Ueda , Satoru Sonoke
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K47/26 , A61K9/10 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K31/713 , C07H15/04
摘要： The object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine.The present invention relates to a galactose derivative represented by the following general formula (I) a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, an oligo nucleic acid). wherein, R1 represents hydrogen, an alkyl having 1 to 10 carbons which may be substituted or 1-(D)-deoxylactito-1-yl; R2 represents a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms.
摘要翻译：本发明的目的是提供一种新颖有用的半乳糖衍生物，其是药物载体的组分，药物可以通过其有效转移到肝脏中，药物载体包含该衍生物，以及包含该药物的药物组合物载体和药物。本发明涉及由以下通式（I）表示的包含该衍生物和阳离子脂质的药物载体的半乳糖衍生物，以及包含该载体和药物（优选双链RNA，双链 DNA，寡核酸）。其中，R 1表示氢，可以被取代的具有1至10个碳的烷基或1-（D） - 脱氧葡糖基-1-基; R2表示具有10至30个碳原子的饱和或不饱和脂肪酸残基。

23. 发明申请

US20070172925A1 Ribonucleic acid compound and method of liquid-phase synthesis of oligonucleic acid compound 审中-公开
标题翻译：核糖核酸化合物和液相合成低聚核酸化合物的方法
公开(公告)号：US20070172925A1
公开(公告)日：2007-07-26
申请号：US10597445
申请日：2005-01-26
申请人： Tadaaki Ohgi , Toshihiro Ueda , Yasufumi Maruyama , Hirofumi Masuda
发明人： Tadaaki Ohgi , Toshihiro Ueda , Yasufumi Maruyama , Hirofumi Masuda
IPC分类号： C12P19/28 , C07H21/04 , C07H19/04
CPC分类号： C07H19/167 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7088 , C07H19/067 , C07H19/10 , C07H19/20 , C07H21/02 , C07H21/04 , Y02P20/55
摘要： A novel phosphotriesterified ribonucleic acid compound which is important for liquid-phase synthesis of oligo-RNA is provided. Examples of the ribonucleic acid compound of the invention may include ribonucleic acid compounds represented by the following general formula: (wherein B represents adenine, guanine, cytosine or uracil or a modified form thereof; R21 represents aryl which may be substituted or a monocyclic or bicyclic heterocyclic group which may be substituted; R20 represents H or alkyl which may be substituted; and R1 represents a protecting group which can be removed at 90% or more at a temperature in the range from 0° C. to 60° C. under acidic conditions at a pH value from 2 to 4 within 24 hours).
摘要翻译：提供了一种对寡核苷酸的液相合成非常重要的新型磷酸酯化核糖核酸化合物。本发明的核糖核酸化合物的实例可以包括由以下通式表示的核糖核酸化合物：其中B表示腺嘌呤，鸟嘌呤，胞嘧啶或尿嘧啶或其修饰形式; R 21表示可以被取代或可以被取代的单环或双环杂环基; R 20表示H或可被取代的烷基; R 1表示可以被取代的保护基在酸性条件下，在24小时内pH为2〜4的温度下，在0℃〜60℃的温度下，90％以上除去）。

24. 发明授权

US07223857B2 Chain-shortened polynucleotide and method for preparation thereof 失效
标题翻译：链缩短的多核苷酸及其制备方法
公开(公告)号：US07223857B2
公开(公告)日：2007-05-29
申请号：US10873797
申请日：2004-06-22
申请人： Shinji Matsuyama , Kouichi Ishiyama , Junzo Seki , Tadaaki Ohgi
发明人： Shinji Matsuyama , Kouichi Ishiyama , Junzo Seki , Tadaaki Ohgi
IPC分类号： C07H21/00 , C07H21/04 , C12Q1/68
CPC分类号： A61K31/7125 , A61K9/1272 , A61K31/7088 , A61K31/713
摘要： The present invention provides a chain-shortened polynucleotide wherein the proportion of a 2′-5′ phosphodiester bond is up to 3% based on the whole phosphodiester bonds or a salt thereof and a pharmaceutical composition containing the same, and a method for producing the same.
摘要翻译：本发明提供了一种链缩短的多核苷酸，其中基于整个磷酸二酯键的2'-5'磷酸二酯键的比例高达3％或其盐和含有它们的药物组合物，以及制备相同。

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