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US 10,426,737 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
Life of this patent
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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.
Claims29
A compound of formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- 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
- v is 0, 1, 2, 3 or 4;
- w is 0, 1, 2 or 3;
- R and R′ are each, independently, hydrogen or C1-8 alkyl;
- R2 is selected from:
- (i) C6-20 alkyl optionally substituted with a hydroxyl, and (ii) C15-19 alkenyl;
- R3 is selected from:
- C4-22 alkyl, C12-22 alkenyl,
10 more elements
A compound:
- 2-(10-dodecyl-3-ethyl-8,14-dioxo-7,9,13-trioxa-3-azaoctadecan-18-yl)propane-1,3-diyl dioctanoate or a pharmaceutically acceptable salt thereof.
A compound:
- (13Z,16Z)-4-(((3-(dimethylamino)propoxy)carbonyl)oxy)docosa-13,16-dien-1-yl heptadecan-9-yl succinate or a pharmaceutically acceptable salt thereof.
A compound:
- 3-(((3-(dimethylamino)propoxy)carbonyl)oxy)-5-octyltridecyl decanoate or pharmaceutically acceptable salt thereof.
A compound:
- (9Z,9′Z,12Z,12′Z)-2-((4-(((3-(dimethylamino)propoxy)carbonyl)oxy)hexadecanoyl)oxy)propane-1,3-diyl bis(octadeca-9,12-dienoate) or a pharmaceutically acceptable salt thereof.
A compound:
- (9Z,9′Z,12Z,12′Z)-2-((2-(((3-(dimethylamino)propoxy)carbonyl)oxy)tetradecanoyl)oxy)propane-1,3-diyl bis(octadeca-9,12-dienoate) or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.