Carbonate containing lipid compounds and compositions for intracellular delivery of therapeutic agents
AssigneeModernaTX, Inc.
InventorsKerry E. Benenato, Souvik Biswas, Mark Cornebise, Edward Hennessy, Ellalahewage S. Kumarasinghe
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Abstract
The disclosure features novel lipids and compositions involving the same. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Lipid nanoparticles (e.g., empty LNPs or loaded LNPs) further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
Claims25
A compound of Formula (A):
- or its N-oxide, or a salt thereof, wherein
- m is selected from 5, 6, 7, 8, and 9;
- R2 and R3 are each independently selected from the group consisting of H, C1-14 alkyl, and C2-14 alkenyl;
- R4 is selected from —(CH2)nOH, wherein n is selected from 1, 2, 3, 4, and 5, and
- wherein n2 is selected from 1, 2, 3, 4, 5, 6, 7, 8, 9, and 10;
- and R10 is —N(R)2, wherein each R is independently selected from the group consisting of C1-6 alkyl, C2-3 alkenyl, and H;
- M and M′ are each independently selected from —OC(O)O— and —C(O)O—;
- wherein at least one of M and M′ is —OC(O)O—;
- R′a is C1-18 alkyl or C2-18 alkenyl;
- and
- R″ is a C3-C13 alkyl, optionally substituted with OH.
A compound selected from:
- and N-oxides and salts thereof.
Dependencies are inferred from the claim text.