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US 2024/0166593 A1Published application
Lipids suitable for nucleic acid delivery
AssigneeRamot at Tel-Aviv University Ltd.
InventorsSrinivas RAMISHETTI, Dan PEER
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Abstract
The present invention provides lipids and lipid nanoparticle formulations comprising these lipids, alone or in combination with other lipids. These lipid nanoparticles may be formulated with nucleic acids to facilitate their intracellular delivery both in vitro and for therapeutic applications. The present invention also provides methods of chemical synthesis of these lipids, lipid nanoparticle preparation and formulation with nucleic acids.
Claims21
1-54. (canceled)
A lipid represented by the structure of Formula (II):
- wherein
- R1 is selected from the group consisting of:
- OH and C1-3 alkyl-OH
- R13 is selected from the group consisting of:
- OH, C1-3 alkyl-OH, C4-14 alkyl and C4-14 alkenyl;
- R12 is selected from the group consisting of:
- C1-13 alkyl;
- C2-15 alkenyl, C1-6 alkyl-CO2—C0-3 alkylene-N(C1-8 alkyl)2 and C1-6 alkyl-CO2— C0-3 alkylene-NH—C1-8 alkyl;
- R14 is selected from the group consisting of:
- C1-13 alkyl;
- C2-15 alkenyl and
- each L is an alkylene ester linker represented by:
- La-Xa-Lb;
- Xa is selected from the group consisting of:
- —O2C—, —CO2—C2-4 alkylene-O2C—, O2C—C2-4 alkylene-O2C—, —CO2—C2-4 alkylene-CO2—, and O2C—C2-4 alkylene-CO2—;
- La is selected from the group consisting of:
- C1-3 alkylene, C4-12 alkylene, C2-10 alkenylene and absent;
- and
- Lb is selected from the group consisting of:
- C1-3 alkylene, C2-10 alkenylene and C4-12 alkylene.
17 more elements
A lipid selected from the group consisting of:
Dependencies are inferred from the claim text.