公开(公告)号：EP2612914B1

公开(公告)日：2017-06-21

申请号：EP11821885.8

申请日：2011-08-31

申请人： Osaka University ,  National Cerebral and Cardiovascular Center ,  Tokyo University Of Science Educational Foundation Administrative Organization

发明人： OBIKA, Satoshi ,  IMANISHI, Takeshi ,  YAMAMOTO, Tsuyoshi ,  NARUKAWA, Keisuke ,  SHIBA, Mariko ,  YAMAOKA, Tetsuji ,  TORIGOE, Hidetaka ,  YAMASHITA, Atsushi ,  TACHIBANA Yoichi ,  KAKINOKI, Sachiro ,  SASAKI, Kiyomi

IPC分类号： C12N15/09 ,  A61K31/712 ,  A61K47/42 ,  A61P3/10 ,  A61P43/00

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

公开(公告)号：EP2612914A1

公开(公告)日：2013-07-10

申请号：EP11821885.8

申请日：2011-08-31

申请人： Osaka University ,  National Cerebral and Cardiovascular Center ,  Tokyo University Of Science Educational Foundation Administrative Organization

发明人： OBIKA, Satoshi ,  IMANISHI, Takeshi ,  YAMAMOTO, Tsuyoshi ,  NARUKAWA, Keisuke ,  SHIBA, Mariko ,  YAMAOKA, Tetsuji ,  TORIGOE, Hidetaka ,  YAMASHITA, Atsushi ,  TACHIBANA Yoichi ,  KAKINOKI, Sachiro ,  SASAKI, Kiyomi

IPC分类号： C12N15/09 ,  A61K31/712 ,  A61K47/42 ,  A61P3/10 ,  A61P43/00

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可用作对于与PCSK9基因具有优异的结合亲和力以及稳定性和安全性的用于血脂异常的治疗剂的寡核苷酸。 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。