5’-c alkyl substituted rna caps and methods of use
AssigneeNutcracker Therapeutics, Inc.
InventorsColin James McKinlay, Maryam Habibian
Life of this patent
Estimating the term…
Abstract
Provided herein are compounds according to formula (I), wherein each of R7 and R8 is H or C1-C6-alkyl and at least one of R7 and R8 is C1-C6-alkyl, that are cap analogs for polynucleotides, e.g., RNA molecules, such as mRNA molecules. Also provided are capped polynucleotides, e.g., capped RNA molecules, such as capped mRNA molecules, wherein the 5′ end of the RNA molecule comprises a cap analog disclosed herein, drug products comprising the capped RNA molecules, methods for making capped polynucleotides disclosed herein, and kits for making the capped polynucleotides.
Claims75
A compound of Formula (I), or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof:
- wherein
- ring G is guanine or a modified guanine;
- each of R1, R2, R4, and R6 is independently H, C1-6alkyl, halo, OH, CN, or ORx, where Rx is C1-6alkyl, C2-6alkenyl, or C2-6alkynyl, and Rx is optionally substituted with one or more substituents independently selected from halo, OH, C1-6alkoxy, and OC(O)—C1-6alkyl;
- R1A is H, or R1A and R1 together form —O—C1-6alkylene-;
- R4A is H, or R4A and R4 together form —O—C1-6alkylene-;
- X is O, S, SO, SO2, or Se;
- L is a linker;
- R3 is H, C1-6alkyl, C1-6alkoxy, OH, halo, or a polynucleotide;
- R5 is OH, SH, C1-6alkyl, C1-6alkoxy, or N(RN5)2 and each RN5 is independently H or C1-6alkyl;
- each of R7 and R8 is H or C1-6alkyl, and at least one of R7 and R8 is C1-6alkyl;
- W is O, S, or NS(O)2C1-6alkyl;
- and
- each of ring A and ring B is independently a nucleobase.
A compound having a structure as shown in Table 1, or a stereoisomer, tautomer, or salt thereof.
Dependencies are inferred from the claim text.