公开(公告)号：EP3252043B1

公开(公告)日：2020-09-30

申请号：EP16743545.2

申请日：2016-01-29

申请人： NOF Corporation ,  National University Corporation Hokkaido University

发明人： NAKAI, Yuta ,  TANGE, Kota ,  AKITA, Hidetaka ,  HARASHIMA, Hideyoshi ,  TOGASHI, Ryohei ,  MIURA, Naoya ,  MAETA, Mio

IPC分类号： C07D295/088 ,  A61K9/127 ,  A61K31/7088 ,  A61K45/00 ,  A61K47/22 ,  A61K48/00 ,  A61P43/00 ,  C07D311/00

公开(公告)号：EP3360576A1

公开(公告)日：2018-08-15

申请号：EP16853305.7

申请日：2016-06-29

申请人： NOF Corporation ,  National University Corporation Hokkaido University

发明人： TANGE, Kota ,  NAKAI, Yuta ,  AKITA, Hidetaka ,  TANAKA, Hiroki ,  WATANABE, Ayaka ,  MIURA, Naoya ,  HARASHIMA, Hideyoshi

IPC分类号： A61K47/20 ,  A61K9/107 ,  A61K31/37 ,  A61K31/573 ,  A61K45/00 ,  A61K47/22 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34 ,  A61P3/06 ,  A61P29/00 ,  A61P31/00 ,  A61P31/04 ,  A61P31/10 ,  A61P35/00 ,  A61P37/06

CPC分类号： A61K9/107 ,  A61K31/37 ,  A61K31/573 ,  A61K45/00 ,  A61K47/20 ,  A61K47/22 ,  A61K47/24 ,  A61K47/28 ,  A61K47/34

摘要： The present invention provides an O/W type emulsion having a volume median diameter of not more than 100 nm and containing a compound represented by the formula (1)

wherein X a and X b are each independently X 1 , X 2 or a 1,4-piperazinediyl group;

s is 1 or 2,
R 4 is an alkyl group having 1 - 6 carbon atoms,
n a and n b are each independently 0 or 1,
R 1a , R 1b , R 2a and R 2b are each independently an alkylene group having 1 - 6 carbon atoms,
Y a and Y b are each independently an ester bond, or the like, and
R 3a and R 3b are each independently a liposoluble vitamin residue or the like.

公开(公告)号：EP3252043A1

公开(公告)日：2017-12-06

申请号：EP16743545.2

申请日：2016-01-29

申请人： NOF Corporation ,  National University Corporation Hokkaido University

发明人： NAKAI, Yuta ,  TANGE, Kota ,  AKITA, Hidetaka ,  HARASHIMA, Hideyoshi ,  TOGASHI, Ryohei ,  MIURA, Naoya ,  MAETA, Mio

IPC分类号： C07D295/088 ,  A61K9/127 ,  A61K31/7088 ,  A61K45/00 ,  A61K47/22 ,  A61K48/00 ,  A61P43/00 ,  C07D311/00

摘要： The present invention aims to provide a cationic lipid that can be used as a nucleic acid delivery carrier, a lipid membrane structure using a cationic lipid, a nucleic acid-introducing agent using a cationic lipid, and a method of achieving nucleic acid introduction by using a nucleic acid-introducing agent containing a cationic lipid. A lipid membrane structure containing a cationic lipid represented by the formula (1)

wherein each symbol is as defined in the DESCRIPTION, is superior in the stability in blood and tumor accumulation property. A nucleic acid-introducing agent using the cationic lipid can achieve high nucleic acid delivery efficiency of nucleic acid to be delivered into the cytoplasm.

摘要翻译： 本发明的目的在于提供可用作核酸递送载体的阳离子性脂质，使用阳离子脂质的脂质膜结构体，使用阳离子性脂质的核酸导入剂，以及使用阳离子脂质的核酸导入剂的使用方法 含有阳离子脂质的核酸引入剂。 包含由式（1）表示的阳离子脂质的脂质膜结构体，其中每个符号如说明书中所定义，在血液稳定性和肿瘤积聚性方面优异。 使用阳离子脂质的核酸引入剂可以实现待递送到细胞质中的核酸的高核酸递送效率。