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US 2019/0358170 A1Published application
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 (I):
- 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;
- L2 is —OC(O)— or —C(O)O—;
- R1 is selected from:
- v is 0, 1, 2, 3 or 4;
- w is 0, 1, 2, or 3;
- Cyl is 5-7 membered nitrogen containing heterocycle optionally substituted with one or two alkyl groups;
- Ar is an aryl group, optionally substituted with C1-8 alkyl amino group;
- R and R′ are each, independently, hydrogen or C1-8 alkyl;
- and
- R2 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,
11 more elements
Dependencies are inferred from the claim text.