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US 6,583,301 B1Granted
Lipids
AssigneeCelltech R&D Limited
InventorsMichael Anthony William Eaton, Timothy John Norman, David Parker, Terence Seward Baker, Andrew Neil Charles Weir, Catherine Fiona Catterall
Life of this patent
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Abstract
Bipolar lipids are described which are able to form complexes with polyanions. The lipids comprise a cationic head linked to a hydrophobic backbone and a hydrophilic tail and are capable of self assembly to form stable complexes in aqueous solutions. The lipids are of particular use for the delivery of bioactive substances such as nucleic acids to cells in vitro and especially in vivo.
Claims43
A bipolar lipid comprising a cationic head (1), a hydrophobic backbone (2) and a hydrophilic tail (3) wherein:
- (A) the cationic head comprises two or more cationic centers, wherein each center is covalently linked to one or more other centers by one or more carbon-containing spacer groups;
- (B) the hydrophobic backbone comprises at least one hydrocarbon chain;
- and
- (C) the hydrophilic tail comprises at least one tail unit selected from the group consisting of a synthetic polyol, naturally occurring polyol, poly(alkylene oxide) and derivative of poly(alkylene oxide);
- wherein each of said components (1) to (3) is covalently linked head (1) to backbone (2) to tail (3) and arranged such that said at least one hydrocarbon chain of the hydrophobic backbone (2) is covalently attached to a carbon atom of a spacer group in the cationic head (1) and to said at least one tail unit in the hydrophilic tail (3) such that the chain contains at least ten chain-linked atoms between its points of attachments to said spacer group and said at least one tail unit.
2 more elements
Dependencies are inferred from the claim text.