Modified nucleoside and synthetic methods thereof
AssigneeStemirna Therapeutics Co., Ltd.
InventorsYunsong Cai, Hangwen Li, Lianxiao Liu, Ning Li
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Abstract
Disclosed are a modified cytidine compound, i.e. a new derivative cytidine generated by adding a guanidyl at position 4 of a cytidine, and a nucleic acid containing the modified compound, for example, RNA. The nucleic acid containing the modified cytidine, especially mRNA, can significantly increase the expression quantity of the mRNA in vivo.
Claims11
A compound of Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 and R2 are both OH;
- R4 and R5 are each independently selected from the group consisting of —H, —OH, —NH2, halo, and substituted or unsubstituted C1-C10 alkyl;
- and R3 is —OH, phosphate, diphosphate, or triphosphate.
A compound, or a pharmaceutically acceptable salt thereof, wherein the compound is
A compound, which is 2-(1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxyl-methyl)tetrahydrofuran-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl)guanidine (4-guanidinocytidine) or 4-guanidinocytidine-5′-triphosphate, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.