IP Library › Granted Patent US 12,251,446
Granted Patent B2
US 12,251,446 · App. 16/314,015 · Granted Mar 18, 2025

Nucleic acid conjugate

Inventors: Keiji Uehara (Tokyo, JP); Yasuhiro Suzuki (Tokyo, JP); Toshimasa Harumoto (Tokyo, JP); Hiroto Iwai (Tokyo, JP); Asana Makino (Tokyo, JP)
Assignee: KYOWA KIRIN CO., LTD.
A61K47/60A61K9/0019A61K31/7088A61K47/54A61K48/00C07H21/02C12N15/09C12N15/113
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Quick Facts
Patent No.
US 12,251,446
App. No.
16/314,015
Granted
Mar 18, 2025
Kind
B2
Abstract

The present invention provides a nucleic acid conjugate in which a sugar chain ligand is bonded to an oligonucleotide via a linker, the sugar chain ligand having O-bonded mannose at its non-reducing end.

Claims (27)

1. A nucleic acid conjugate in which a sugar chain ligand is bonded to an siRNA or an antisense oligonucleotide (ASO) via a linker, wherein the sugar chain ligand has the following structure:

wherein

R 1 and R 2 are 4-hydroxybenzyl,

Y 1 and Y 2 are each NR 3 , and

R 3 is a hydrogen atom.

2. The nucleic acid conjugate according to claim 1 , wherein the sugar chain ligand has the following structure:

wherein

R 1 ′ and R 2 ′ are 4-hydroxybenzyl,

Y 1 ′ and Y 2 ′ are each NR3, and

R 3 ′ is a hydrogen atom.

3. The nucleic acid conjugate according to claim 1 , wherein the linker has any of the following structures:

wherein

X 1 is CH or a nitrogen atom, and

X 2 to X 4 are each independently CH or a nitrogen atom.

4. The nucleic acid conjugate according to claim 1 , wherein the linker has the following structure:

5. The nucleic acid conjugate according to claim 1 , wherein the linker has the following structure:

wherein

n1 is an integer of 1 to 100.

6. The nucleic acid conjugate according to claim 1 , wherein the linker has any of the following structures:

wherein

n2 and n3 are each independently an integer of 1 to 100.

7. The nucleic acid conjugate according to claim 1 , wherein the siRNA or the antisense oligonucleotide comprises a modified nucleotide.

8. A pharmaceutical composition comprising the nucleic acid conjugate according to claim 1 .

9. The pharmaceutical composition according to claim 8 , wherein the pharmaceutical composition is for transfer into a cell.

10. The pharmaceutical composition according to claim 9 , wherein the cell is a dendritic cell or a macrophage.

11. A method for treating or preventing a disease, comprising administering the nucleic acid conjugate according to claim 1 to a patient in need thereof.

12. The method of claim 11 , wherein the nucleic acid conjugate is intravenously administered or subcutaneously administered.

Assignments (2)
CHANGE OF NAME Recorded Nov 21, 2019
From: KYOWA HAKKO KIRIN CO., LTD.
To: KYOWA KIRIN CO., LTD.
Reel/Frame 051076/0509 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 28, 2018
From: UEHARA, KEIJI; SUZUKI, YASUHIRO; HARUMOTO, TOSHIMASA; IWAI, HIROTO; MAKINO, ASANA
To: KYOWA HAKKO KIRIN CO., LTD.
Reel/Frame 047868/0515 →
Priority Claims (1)
JP 2016-131054 · Jun 30, 2016 · national
Continuity (1)
Related Publication 20190192674A1 · Jun 27, 2019
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Cited By (1)
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