Back to results
US 12,760,307 B2Granted
Morpholino oligonucleotide derivatives
AssigneeNexoligo Co., Ltd.
InventorYeohong Yoon
Life of this patent
Estimating the term…
Abstract
The present invention relates to a novel morpholino oligonucleotide comprising at least one type of morpholino nucleotide monomer having pyrrolocytosine (pC) among unnatural cytosines, and relates to a morpholino oligonucleotide capable of more selectively binding to a target RNA and exhibiting excellent cell penetration compared to an MPO having a natural cytosine, and thus being capable of greatly contributing to the development of a therapeutic agent for incurable diseases in the area of morpholino oligonucleotides.
Claims2
A morpholino nucleotide monomer substituted with pyrrolocytosine of the following Chemical Formula 6:
- wherein:
- PG3 is selected from the group consisting of fluorenylmethoxycarbonyl (Fmoc), 1,1-dioxobenzo[b]thiophen-2-ylmethoxycarbonyl (Bsmoc), 2-(4-nitrophenylsulfonyl)ethoxycarbonyl (Nsc), 2-(4-sulfophenylsulfonyl)ethoxycarbonyl (Sps), ethanesulfonylethoxycarbonyl (Esc), phthaloyl, tetrachlorophthaloyl (TCP), 2-fluoro fluorenylmethoxycarbonyl (Fmoc (2F)) and 2,7-ditert-butyl fluorenylmethoxycarbonyl (DtBFmoc);
- PG4 is selected from the group consisting of tert-butoxycarbonyl (Boc), trityl (Trt), α,α-dimethyl-3,5-dimethylbenzyloxycarbonyl (Ddz), 2-(4-biphenyl) isopropoxycarbonyl (Bpoc) and 2-nitrophenylsulfenyl (Nps);
- x is an integer of 1 to 3;
- and
- y is an integer of 1 to 3.
3 more elements
Dependencies are inferred from the claim text.