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US 11,013,696 B2Granted
Lipids and lipid compositions for the delivery of active agents
AssigneeNovartis AG
InventorsLuis Brito, Delai Chen, Gabriel Grant Gamber, Andrew Geall, Kevin Love, Thomas Zabawa, Frederic Zecri
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Abstract
This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
Claims20
A compound, or salt thereof, of formula (Ia):
- n is 0, 1, 2, 3 or 4;
- p is 0, 1, 2, 3, 4, 5, 6, 7 or 8;
- L1 is —O— or a bond;
- L2a is —O— or a bond;
- L3 is —O— or a bond;
- R1a is selected from:
- v is 0, 1, 2, 3 or 4;
- w is 0, 1, 2, or 3;
- Cyl is a 5-7 membered nitrogen containing heterocycle containing 1 or 2 heteroatoms selected from N and O, and optionally substituted with one or two C1-5 alkyl groups;
- Ar is a 5-7 membered monocyclic aryl group, optionally substituted with 1-2 N, optionally substituted with C1-5 alkyl amino group;
- R and R′ are each, independently, hydrogen or C1-8 alkyl;
- and
- R2a is selected from C6-20 alkyl optionally substituted with a hydroxyl, C15-19 alkenyl, C1-12alkyl-OC(O)—C5-20alkyl, C1-12alkyl-C(O)O—C5-20alkyl and
- R3 is selected from:
- C4-22 alkyl, C12-22 alkenyl,
12 more elements
Dependencies are inferred from the claim text.