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US 2021/0196831 A1Published application
Oligonucleotide constructs and uses thereof
AssigneeJanssen BioPharma, Inc.
InventorsSergei GRYAZNOV, Leonid BEIGELMAN, Theodore YUN
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Abstract
Oligodeoxynucleotide-based immunostimulatory Toll-Like Receptor 9 (TLR9) agonists are described. Also described are compositions comprising the TLR9 agonists, methods of making the TLR9 agonists, and methods of using the TLR9 agonists to treat immune diseases, disorders or conditions, such as viral infections or cancer.
Claims21
A CpG ODN construct having a formula of:
- 5′M-L-[CpG ODN]3′, or Formula (IIa):
- 5′[CpG ODN]-L-M3′ Formula (IIb):
- wherein:
- M represents a lipid moiety, preferably the lipid moiety comprises at least one lipid moiety selected from the group consisting of cholesterol, tocopherol, a palmitoyl group, and a stearyl group;
- L represents a linker comprising 10-100 atoms selected from the group consisting of carbon, nitrogen, oxygen, hydrogen, sulfur and phosphorus, wherein L is covalently linked to the CpG ODN via a cleavable linkage, preferably via an ester or an amide bond;
- and
- CpG ODN comprises at least one CpG motif having a po internucleotide linkage;
- optionally, the CpG ODN construct of Formula (IIa) or (IIb) is further covalently conjugated to a targeting moiety, which is preferably selected from the group consisting of galactose, N-acetylgalactosamine (GalNAc), fucose, mannose, sialic acid, N-acetyl neuraminic acid.
5 more elements
A CpG ODN construct having a structure of:
- 5′M1-Y1—(((CH2)2O)m—X)n—Y2-[CpG ODN]-Y3-M23′, or Formula (IIIa):
- 5′M2-Y3-[CpG ODN]-Y2—(((CH2)2O)m—X)n—Y1-M13′ Formula (IIIb):
- wherein:
- M1 represents a lipid moiety, preferably the lipid moiety comprises at least one selected from the group consisting of cholesterol, tocopherol, a palmitoyl group, and a stearyl group,
- M2 represents a lipid moiety, a targeting moiety, or is absent,
- Y1 is a bond or a linker, preferably ethylene glycol having the formula ((CH2)2O)o, wherein o is 1-15, covalently linked to (((CH2)2O)m—X)n via a phosphodiester (po) linkage, a phosphorothioate (ps) linkage or a bond,
- X is independently a bond, a po linkage or a ps linkage,
- each of Y2 and Y3 is independently a cleavable linkage, preferably comprises an ester or an amide bond, more preferably comprises a po linkage or a phosphoramidate linkage, most preferably a po linkage, provided that when M2 is absent, Y3 is absent,
- CpG ODN comprises at least one CpG motif having a po internucleotide linkage, preferably comprises at least two, three or four CpG motifs each having the po internucleotide linkage;
- m is an integer from 1 to 15, and
- n is an integer from 1 to 5.
8 more elements
(canceled)
An ODN construct having a structure of:
- or a pharmaceutically acceptable salt thereof, wherein the Oligonucleotides represents a CpG ODN comprising at least one CpG motif having a po internucleotide liknage.
An ODN construct having a structure of:
Dependencies are inferred from the claim text.