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1.发明申请公开(公告)号：US20100298411A1
公开(公告)日：2010-11-25
申请号：US12738797
申请日：2008-10-24
IPC分类号： A61K31/713 , C07H21/02 , C12N15/113 , A61P5/00
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。
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2.发明授权公开(公告)号：US09040492B2
公开(公告)日：2015-05-26
申请号：US12935546
申请日：2009-03-31
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 an antisense strand having a nucleotide sequence complementary to a target sequence in a target gene, and a sense strand having a nucleotide sequence complementary to the antisense 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反义链和具有与反义链互补的核苷酸序列的有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，并且将具有直链或经由连接基结合的双链脂质的有义链与5'末端的至少一个第一至第六个核苷酸结合。
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3.发明授权公开(公告)号：US08981074B2
公开(公告)日：2015-03-17
申请号：US12738797
申请日：2008-10-24
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。
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4.发明申请公开(公告)号：US20110034545A1
公开(公告)日：2011-02-10
申请号：US12935546
申请日：2009-03-31
IPC分类号： A61K31/713 , C07H21/02 , C12N5/071 , A61P35/00 , A61P31/18
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，并且将具有直链或经由连接基结合的双链脂质的有义链与5'末端的至少一个第一至第六个核苷酸结合。
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公开(公告)号：US20100112043A1
公开(公告)日：2010-05-06
申请号：US12593827
申请日：2008-03-28
CPC分类号： A61K9/1277 , A61K9/007 , A61K9/0078 , A61K9/1271 , A61K45/06 , A61K47/32 , A61K47/36 , A61K48/00 , A61K48/0075 , C12N15/88 , C12N2810/10
摘要： An object of the present invention is to provide a liposome which is excellent in intrapulmonary delivery controllability of drugs or genes and is suited for pulmonary administration.By modifying the surface of a liposome using a terminal hydrophobized polyvinyl alcohol and/or chitosan, retention of drugs or genes encapsulated in the liposome on the surface of lung tissue and transfer of drugs or genes into lung tissue can be properly modulated, and thus in vivo behavior can be controlled.
摘要翻译： 本发明的目的是提供一种在药物或基因的肺内递送可控性优异且适于肺部给药的脂质体。 通过使用末端疏水化聚乙烯醇和/或壳聚糖改性脂质体的表面，可以适当地调节将包封在脂质体中的药物或基因保留在肺组织表面上并将药物或基因转移到肺组织中， 可以控制体内行为。
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6.发明申请Agent improving proton-driven transporter-mediated absorption in digestive tract and process for producing the same 审中-公开改善质子驱动的转运蛋白介导的消化道吸收及其制备方法公开(公告)号：US20060121107A1
公开(公告)日：2006-06-08
申请号：US10541019
申请日：2004-01-08
申请人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K31/401 , A61K31/198 , A61K9/20 , A61K31/716
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译： 本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法 。 本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收 复合成细胞。
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公开(公告)号：US20100063131A1
公开(公告)日：2010-03-11
申请号：US12532949
申请日：2008-03-26
IPC分类号： A61K31/7105 , A61K31/7088 , C12N5/07 , A61P35/00
CPC分类号： C12N15/87 , A61K9/127 , A61K31/7088 , A61K31/713 , A61K48/00 , C12N15/111 , C12N2310/14 , C12N2320/32
摘要： An object of the present invention is to provide a carrier composition for nucleic acid delivery, which can efficiently deliver a nucleic acid into cells when a nucleic acid such as siRNA is administered to animal-derived cells or animals, and also has low toxicity and high safety, and a composition for nucleic acid delivery containing the carrier composition and nucleic acid.A carrier for nucleic acid delivery is prepared by using (A) a diacylphosphatidylcholine, (B) at least one member selected from the group consisting of cholesterol and derivatives thereof, and (C) an aliphatic primary amine. Also, a composition for nucleic acid delivery is prepared by mixing the carrier for nucleic acid delivery with a nucleic acid.
摘要翻译： 本发明的目的是提供一种用于核酸递送的载体组合物，当向动物来源的细胞或动物施用siRNA等核酸时，可以将核酸有效地递送到细胞中，并且还具有低毒性和高 安全性和用于含有载体组合物和核酸的核酸递送的组合物。 通过使用（A）二酰基磷脂酰胆碱，（B）至少一种选自胆固醇及其衍生物的组分和（C）脂族伯胺制备核酸递送载体。 而且，通过将用于核酸递送的载体与核酸混合来制备用于核酸递送的组合物。
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公开(公告)号：US20090258923A1
公开(公告)日：2009-10-15
申请号：US12083727
申请日：2006-10-17
申请人： Hidekazu Toyobuku , Hideo Miyao , Masako Sato , Kazuo Sekiguchi
发明人： Hidekazu Toyobuku , Hideo Miyao , Masako Sato , Kazuo Sekiguchi
IPC分类号： A61K31/713 , A61K47/28
CPC分类号： A61K9/1272 , A61K47/543 , C12N15/88
摘要： An object of the present invention is to provide a nucleic acid delivery carrier composition of low toxicity and high safety, the carrier composition, when used to administer a nucleic acid such as an siRNA into an animal-derived cell or organism, being capable of delivering efficiently the nucleic acids into the cells while protecting it from being degraded; and a nucleic acid deliver composition containing the carrier and a nucleic acid.The carrier composition for delivery of a nucleic acid is prepared by mixing (A) a cationic lipid having a steroid skeleton with (B) a tertiary ammonium salt-type cationic lipid. The nucleic acid delivery composition is prepared by mixing the nucleic acid delivery carrier with a nucleic acid.
摘要翻译： 本发明的目的是提供一种低毒性和高安全性的核酸递送载体组合物，该载体组合物当用于将诸如siRNA的核酸施用于动物来源的细胞或生物体时，能够递送 将核酸有效地进入细胞同时保护其免于降解; 以及含有载体和核酸的核酸递送组合物。 用于递送核酸的载体组合物通过将（A）具有类固醇骨架的阳离子脂质与（B）叔铵盐型阳离子脂质混合来制备。 通过将核酸递送载体与核酸混合来制备核酸递送组合物。
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公开(公告)号：US20130217754A1
公开(公告)日：2013-08-22
申请号：US13824080
申请日：2011-10-14
IPC分类号： C07H21/02
CPC分类号： C12N15/1136 , A61K31/713 , C07H21/02 , C12N15/113 , C12N2310/14 , C12N2310/315 , C12N2320/30
摘要： Provided is siRNA effective for the treatment of fibrosis and a pharmaceutical containing the siRNA. An siRNA having a full length of 30 or fewer nucleotides and targeting a sequence consisting of 17 to 23 consecutive bases selected from the group consisting of bases at positions 1285 to 1318, bases at positions 1398 to 1418, bases at positions 1434 to 1463, bases at positions 1548 to 1579, bases at positions 1608 to 1628, bases at positions 1700 to 1726, bases at positions 1778 to 1798, bases at positions 1806 to 1826, and bases at positions 1887 to 1907 of SEQ ID NO: 1.
摘要翻译： 提供了对于治疗纤维化有效的siRNA和含有siRNA的药物。 具有30个或更少核苷酸的全长的siRNA，靶向由17至23个连续碱基组成的序列，所述序列选自1285至1318位的碱基，1398至1418位的碱基，1434至1463位的碱基， 位于第1608至1628位的碱基，位置1700至1726的碱基，1778至1798位的碱基，位置1806至1826的碱基和SEQ ID NO：1的1887至1907的碱基。
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10.发明申请Gastrointestinal Absorption Enhancer Mediated By Proton-Coupled Transporter and Its Preparing Method 审中-公开通过质子耦合转运体介导的胃肠吸收增强剂及其制备方法公开(公告)号：US20080119568A1
公开(公告)日：2008-05-22
申请号：US11971243
申请日：2008-01-09
申请人： Akira TSUJI , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira TSUJI , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K47/30
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译： 本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法 。 本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收 复合成细胞。
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