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US 9,352,042 B2Granted
Trialkyl cationic lipids and methods of use thereof
AssigneeProtiva Biotherapeutics, Inc.
InventorsJames Heyes, Mark Wood, Alan Martin
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Abstract
The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel, trialkyl, cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses.
Claims21
A lipid having a structural Formula (I):
- X-A-Y—Z;
- (I)
- or salts thereof, wherein:
- X is alkylamino;
- A is C1 to C6 optionally substituted alkyl, wherein said C1 to C6 optionally substituted alkyl can be saturated or unsaturated, and wherein A may or may not be present;
- Y is selected from the group consisting of ketal, ester, optionally substituted carbamate, ether, and optionally substituted amide;
- and
- Z has the formula:
- wherein, R1, R2, and R3 are each independently selected from the group consisting of C8 to C11 alkyl, wherein each of R1, R2, and R3 can independently be saturated or unsaturated, and wherein each of R1, R2, and R3 is optionally substituted.
6 more elements
A lipid selected from the group consisting of:
- or a salt thereof.
Dependencies are inferred from the claim text.