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Title:
CATIONIC LIPID HAVING IMPROVED INTRACELLULAR KINETICS
Document Type and Number:
WIPO Patent Application WO/2013/073480
Kind Code:
A1
Abstract:
Provided is a cationic lipid with which it is possible to achieve high intracellular expression efficiency when used as a nucleic acid delivery carrier. The lipid is a compound represented by formula (1) (where Xa and Xb are, independently, X1 or X2; s is 1 or 2; R4 is a C1-6 alkyl group, na and nb are, independently, 0 or 1; R1a and R1b are, independently, a C1-6 alkylene group; R2a and R2b are, independently, a C1-6 alkylene group; Ya and Yb are, independently, an ester bond, an amide bond, a carbamate bond, an ether bond, or a urea bond; and R3a and R3b are, independently, a sterol residue, a fat-soluble vitamin residue, or a C12-22 aliphatic hydrocarbon group).

Inventors:
TANGE KOTA (JP)
ARAI MASAYA (JP)
KUBO KAZUHIRO (JP)
AKITA HIDETAKA (JP)
HARASHIMA HIDEYOSHI (JP)
HATAKEYAMA HIROTO (JP)
ISHIBA RYOHEI (JP)
UKAWA MASAMI (JP)
TANAKA HIROKI (JP)
Application Number:
PCT/JP2012/079160
Publication Date:
May 23, 2013
Filing Date:
November 09, 2012
Export Citation:
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Assignee:
NOF CORP (JP)
UNIV HOKKAIDO NAT UNIV CORP (JP)
International Classes:
C07C323/25; A61K47/20; A61K47/44; A61K48/00
Domestic Patent References:
WO1999058152A11999-11-18
WO2008045486A22008-04-17
WO1999058152A11999-11-18
WO2010054405A12010-05-14
WO2005032593A12005-04-14
WO2008105178A12008-09-04
WO2011132713A12011-10-27
Foreign References:
DE2521898A11975-12-04
JP2011121966A2011-06-23
Other References:
See also references of EP 2781507A4
BIOMATERIALS, vol. 29, no. 24-25, 2008, pages 3477 - 96
GENE THERAPY, vol. 6, 1999, pages 271 - 281
MOLECULAR THERAPY, vol. 13, no. 4, 2006, pages 786 - 794
UKAWA ET AL., BIOMATERIALS, vol. 31, no. 24, 2010, pages 6355 - 6362
KHALIL ET AL., J CONTROL RELEASE., vol. 156, no. 3, 2011, pages 374 - 80
KHALIL ET AL., J CONTROL RELEASE., vol. 156, no. 3, pages 374 - 80
SHIMIZU K ET AL., J BIOSCI BIOENG, vol. 112, no. 5, pages 508 - 10
AKINC ET AL., MOLECULAR THERAPY, vol. 17, no. 5, 2009, pages 872 - 879
Attorney, Agent or Firm:
TAKASHIMA, HAJIME (JP)
Takashima 1 (JP)
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Claims: