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US 10,092,655 B2Granted
Cationic lipid for nucleic acid delivery
AssigneesNof Corporation, National University Corporation Hokkaido University
InventorsShota Sasaki, Masaki Ota, Kazuhiro Kubo, Hideyoshi Harashima, Hidetaka Akita, Hiroto Hatakeyama, Yuki Noguchi, Kota Tange, Yuta Nakai, Nayuta Shimizu
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Abstract
The invention provides a cationic lipid capable of achieving higher intracellular delivery efficiency than conventional cationic lipids, when used as a lipid membrane structure which is a carrier for delivering functional nucleic acid. The cationic lipid is represented by the formula (1): wherein each symbol is as defined herein.
Claims9
A cationic lipid represented by the formula (1):
- wherein any 4 of X1-X6 are each independently a group represented by the formula (Xa), a group represented by the formula (Xb) or a hydroxyl group (provided that said 4 are not hydroxyl groups at the same time), and the remaining 2 are each independently a group represented by the formula (Xc) or a hydroxyl group (provided that said 2 are not hydroxyl groups at the same time))
- —Y1—R1 (Xa)
- wherein R1 is an aliphatic hydrocarbon group having 8-22 carbon atoms or an acyl group having 8-22 carbon atoms;
- Y1 is —O— or —NH—)
- wherein R2 is a sterol residue or a liposoluble vitamin residue;
- Z1 is an alkylene group having 2 or 3 carbon atoms;
- Y2 is —O—CO— or —NH—CO—)
- wherein R3 and R4 are each independently an alkyl group having 1-6 carbon atoms, R3 and R4 are optionally bonded to form a ring;
- Z2 is an alkylene group having 1-6 carbon atoms;
- Y3 is —O—, —O—CO— or —NH—CO—;
- n is 0 or 1.
8 more elements
Dependencies are inferred from the claim text.