公开(公告)号：US20130172402A1

公开(公告)日：2013-07-04

申请号：US13819722

申请日：2011-08-31

申请人： Satoshi Obika ,  Takeshi Imanishi ,  Tsuyoshi Yamamoto ,  Keisuke Narukawa ,  Mariko Shiba ,  Tetsuji Yamaoka ,  Hidetaka Torigoe ,  Atsushi Yamashita ,  Yoichi Tachibana ,  Sachiro Kakinoki ,  Kiyomi Sasaki

发明人： Satoshi Obika ,  Takeshi Imanishi ,  Tsuyoshi Yamamoto ,  Keisuke Narukawa ,  Mariko Shiba ,  Tetsuji Yamaoka ,  Hidetaka Torigoe ,  Atsushi Yamashita ,  Yoichi Tachibana ,  Sachiro Kakinoki ,  Kiyomi Sasaki

IPC分类号： C12N15/113

CPC分类号： C12N15/1137 ,  A61K9/0019 ,  A61K9/0021 ,  A61K9/06 ,  A61K31/712 ,  C12N2310/11 ,  C12N2310/3231 ,  C12N2310/351 ,  C12Y304/21

摘要： An object of the present invention is to provide an oligonucleotide useful as a therapeutic agent for dyslipidemia that has excellent binding affinity to the PCSK9 gene as well as stability and safety. The oligonucleotide of the present invention contains a sugar-modified nucleoside, the sugar-modified nucleoside has a bridging structure between 4′-position and 2′-position, and the oligonucleotide can bind to the human PCSK9 gene. Also, the present invention provides a therapeutic agent for dyslipidemia containing the oligonucleotide as an active ingredient, and the therapeutic agent preferably contains a bioabsorbable material as a carrier. The bioabsorbable material is preferably atelocollagen or peptide gel.

摘要翻译： 本发明的目的是提供一种可用作血脂异常的治疗剂的寡核苷酸，其对PCSK9基因具有优异的结合亲和力以及稳定性和安全性。 本发明的寡核苷酸含有糖修饰的核苷，糖修饰的核苷具有4'-位和2'-位之间的桥连结构，寡核苷酸可以结合人PCSK9基因。 此外，本发明提供了含有寡核苷酸作为活性成分的血脂异常的治疗剂，优选以生物体吸收性材料为载体。 生物可吸收材料优选为胶原蛋白或肽凝胶。

公开(公告)号：US09127280B2

公开(公告)日：2015-09-08

申请号：US13819722

申请日：2011-08-31

申请人： Satoshi Obika ,  Takeshi Imanishi ,  Tsuyoshi Yamamoto ,  Keisuke Narukawa ,  Mariko Shiba ,  Tetsuji Yamaoka ,  Hidetaka Torigoe ,  Atsushi Yamashita ,  Yoichi Tachibana ,  Sachiro Kakinoki ,  Kiyomi Sasaki

发明人： Satoshi Obika ,  Takeshi Imanishi ,  Tsuyoshi Yamamoto ,  Keisuke Narukawa ,  Mariko Shiba ,  Tetsuji Yamaoka ,  Hidetaka Torigoe ,  Atsushi Yamashita ,  Yoichi Tachibana ,  Sachiro Kakinoki ,  Kiyomi Sasaki

IPC分类号： C07H21/04 ,  A61K31/70 ,  C12N15/113 ,  A61K9/00 ,  A61K9/06 ,  A61K31/712 ,  C12Q1/68

CPC分类号： C12N15/1137 ,  A61K9/0019 ,  A61K9/0021 ,  A61K9/06 ,  A61K31/712 ,  C12N2310/11 ,  C12N2310/3231 ,  C12N2310/351 ,  C12Y304/21

摘要： An object of the present invention is to provide an oligonucleotide useful as a therapeutic agent for dyslipidemia that has excellent binding affinity to the PCSK9 gene as well as stability and safety. The oligonucleotide of the present invention contains a sugar-modified nucleoside, the sugar-modified nucleoside has a bridging structure between 4′-position and 2′-position, and the oligonucleotide can bind to the human PCSK9 gene. Also, the present invention provides a therapeutic agent for dyslipidemia containing the oligonucleotide as an active ingredient, and the therapeutic agent preferably contains a bioabsorbable material as a carrier. The bioabsorbable material is preferably atelocollagen or peptide gel.

摘要翻译： 本发明的目的是提供一种可用作血脂异常的治疗剂的寡核苷酸，其对PCSK9基因具有优异的结合亲和力以及稳定性和安全性。 本发明的寡核苷酸含有糖修饰的核苷，糖修饰的核苷具有4'-位和2'-位之间的桥连结构，寡核苷酸可以结合人PCSK9基因。 此外，本发明提供了含有寡核苷酸作为活性成分的血脂异常的治疗剂，优选以生物体吸收性材料为载体。 生物可吸收材料优选为胶原蛋白或肽凝胶。