公开(公告)号：US20180042955A1

公开(公告)日：2018-02-15

申请号：US15725703

申请日：2017-10-05

申请人： THE UNIVERSITY OF TOKYO ,  NanoCarrier Co., Ltd.

发明人： Kazunori KATAOKA ,  Kanjiro MIYATA ,  Nobuhiro NISHIYAMA ,  Kensuke OSADA ,  Sumiyo WATANABE ,  Shigeto FUKUSHIMA ,  Hiroyuki CHAYA ,  Hiroyasu TAKEMOTO ,  Yasuki KATO

IPC分类号： A61K31/713 ,  A61K47/60 ,  A61K47/64 ,  A61K9/00

CPC分类号： A61K31/713 ,  A61K9/0019 ,  A61K47/60 ,  A61K47/64 ,  A61K47/645 ,  A61K47/6455 ,  A61K48/00

摘要： A unit structure-type pharmaceutical composition includes a single nucleic acid, such as an antisense nucleic acid, electrostatically bound to a single block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. The negative charges of the nucleic acid are counterbalanced, at least substantially, by the positive charges of the cationic polyamino acid segment such that the pharmaceutical composition is electrically neutral or nearly electrically neutral. Further, the nucleic acid is covered with the hydrophilic polymer chain segment. The block copolymer thereby improves the blood retention capability of the nucleic acids.

公开(公告)号：US20180153920A1

公开(公告)日：2018-06-07

申请号：US15879821

申请日：2018-01-25

申请人： NanoCarrier Co., Ltd. ,  THE UNIVERSITY OF TOKYO

发明人： Kazunori KATAOKA ,  Kanjiro MIYATA ,  Nobuhiro NISHIYAMA ,  Kensuke OSADA ,  Sumiyo WATANABE ,  Shigeto FUKUSHIMA ,  Hiroyuki CHAYA ,  Hiroyasu TAKEMOTO ,  Yasuki KATO

IPC分类号： A61K31/713 ,  A61K47/64 ,  A61K47/60 ,  A61K9/00

CPC分类号： A61K31/713 ,  A61K9/0019 ,  A61K47/60 ,  A61K47/645 ,  A61K47/6455 ,  C08G69/10

摘要： A unit structure consists of a single nucleic acid having a length of 10 to 30 bases, and a single block copolymer having a cationic polyamino acid segment and a hydrophilic polymer chain segment. In this unit structure: (i) a difference between a total of positive charges derived from cationic groups of the cationic polyamino acid segment and a total of negative charges derived from the nucleic acid in the unit structure falls within a range of ±10% of the total of the negative charges derived from the nucleic acid, (ii) the hydrophilic polymer chain segment comprises polyethylene glycol, (iii) the polyethylene glycol has a radius of inertia (Rg) equal to or longer than the length of the nucleic acid, and (iv) the cationic polyamino acid segment is bound to the nucleic acid via electrostatic bonds.