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Title:
CATIONIC LIPID
Document Type and Number:
WIPO Patent Application WO/2016/121942
Kind Code:
A1
Abstract:
The purpose of the present invention is to provide a cationic lipid that can be used as a nucleic acid delivery carrier, a lipid membrane structure in which the cationic lipid is used, a nucleic-acid-introducing agent in which the cationic lipid is used, and a method for achieving nucleic acid introduction using the nucleic-acid-introducing agent containing the cationic lipid. The lipid membrane structure containing the cationic lipid represented by formula (1) (in the formula, each of the symbols is as defined in the specification) has exceptional stability in the blood and tumor accumulation properties. The nucleic-acid-introducing agent in which this cationic lipid is used makes it possible to achieve high nucleic acid delivery efficiency of a nucleic acid to be delivered into the cytoplasm.

Inventors:
NAKAI YUTA (JP)
TANGE KOTA (JP)
AKITA HIDETAKA (JP)
HARASHIMA HIDEYOSHI (JP)
TOGASHI RYOHEI (JP)
MIURA NAOYA (JP)
MAETA MIO (JP)
Application Number:
PCT/JP2016/052690
Publication Date:
August 04, 2016
Filing Date:
January 29, 2016
Export Citation:
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Assignee:
NOF CORP (JP)
UNIV HOKKAIDO NAT UNIV CORP (JP)
International Classes:
C07D295/088; A61K9/127; A61K31/7088; A61K45/00; A61K47/22; A61K48/00; A61P43/00; C07D311/00
Domestic Patent References:
WO2013073480A12013-05-23
Foreign References:
US20140335157A12014-11-13
JP2011121966A2011-06-23
JP2011509074A2011-03-24
US6153434A2000-11-28
JP2012509272A2012-04-19
JP2012526134A2012-10-25
JP2005508394A2005-03-31
Other References:
KEDIKA,B. ET AL.: "Synthesis and Gene Transfer Activities of Novel Serum Compatible Reducible Tocopherol-Based Cationic Lipids", MOLECULAR PHARMACEUTICS, vol. 9, no. 5, 2012, pages 1146 - 1162, XP055470382, ISSN: 1543-8384
MARKOV,O.O. ET AL.: "Novel cationic liposomes provide highly efficient delivery of DNA and RNA into dendritic cell progenitors and their immature offsets", JOURNAL OF CONTROLLED RELEASE, vol. 160, no. 2, 2012, pages 200 - 210, XP028926641, ISSN: 0168-3659
TANG,F. ET AL.: "Use of Dithiodiglycolic Acid as a Tether for Cationic Lipids Decreases the Cytotoxicity and Increases Transgene Expression of Plasmid DNA in Vitro", BIOCONJUGATE CHEMISTRY, vol. 10, no. 5, 1999, pages 791 - 796, XP009084473, ISSN: 1043-1802
ZHANG,Y. ET AL.: "Cationic gemini lipids with cyclen headgroups: interaction with DNA and gene delivery abilities", RSC ADVANCES, vol. 4, no. 83, 2014, pages 44261 - 44268, XP055470447, ISSN: 2046-2069
See also references of EP 3252043A4
Attorney, Agent or Firm:
TAKASHIMA, HAJIME (JP)
Takashima 1 (JP)
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