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US 9,220,683 B2Granted
Lipids and compositions for the delivery of therapeutics
AssigneeTekmira Pharmaceuticals Corporation
InventorsMuthiah Manoharan, Kallanthottathil G. Rajeev, David Butler, Jayaprakash K. Narayanannair, Muthusamy Jayaraman, Laxmab Eltepu
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Abstract
The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).
Claims17
A lipid of formula I
- or a salt or isomer thereof, wherein
- R1 and R2 are each independently for each occurrence optionally substituted C10-C20 alkyl, optionally substituted C10-C20 alkenyl, or optionally substituted C10-C20 alkynyl;
- R3 is independently for each occurrence H, optionally substituted C1-C10 alkyl, optionally substituted alkylheterocycle, optionally substituted heterocyclealkyl, optionally substituted amino, optionally substituted alkylamino, optionally substituted di(alkyl)amino, optionally substituted aminoalkyl, optionally substituted alkylaminoalkyl, or optionally substituted di(alkyl)aminoalkyl;
- X and Y are each independently —O— or alkylene;
- A1 and A2 are each independently —O— or —CH2—;
- Z is N, or C(R3);
- and
- m and n are each independently 0 to 5, where m and n taken together result in a 5, 6, or 7 member ring.
5 more elements
A lipid selected from
- and salts thereof.
Dependencies are inferred from the claim text.