LOW-MOLECULAR CONJUGATES FOR INTRACELLULAR DELIVERY OF BIOLOGICALLY ACTIVE COMPOUNDS Russian patent published in 2017 - IPC A61K48/00 C12N15/87 C12N15/11 A61K31/713 A61K47/18 

Abstract RU 2629957 C2

FIELD: biotechnology.

SUBSTANCE: invention relates to application of a formula (III) ligand for preparation of conjugates of oligonucleotides and compositions based thereon, which can be used in medicine

(III).

A new effective ligand of formula (III) is provided for preparation of a conjugate in which the ligand for the asialoglycoprotein receptor is attached to an antisense oligonucleotide or siRNA via an amide bond to deliver the said antisense oligonucleotide or siRNA to the cell, respectively. A method for preparation of such a conjugate comprises conjugating a formula (III) ligand and an oligonucleotide or siRNA with NHC-6 hexylaminolinker at the 5'-end of the sense strand and O-acetate groups removal.

EFFECT: increased compound efficiency.

3 cl, 6 dwg, 18 tbl, 52 ex

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RU 2 629 957 C2

Authors

Khadviger Filipp

Khoffmann Torsten

Yan-Khofmann Kerstin

Kitas Erik A.

Lyuis Devid L.

Mor Peter

Myuller Khans Martin

Ott Gyunter

Rel Ingo

Rozema Devid B.

Dates

2017-09-05Published

2011-12-22Filed