IP Library Granted Patent US 12,465,646
Granted Patent B2
US 12,465,646 · App. 17/311,062 · Granted Nov 11, 2025

Linkers

Inventors: Richard Raz (London, GB); Matthew Wood (Oxford, GB); Caroline Godfrey (Wolvercote, GB); Graham McClorey (Oxford, GB); Subhashis Banerjee (Kolkata, IN); Michael Gait (Cambridge, GB); Miguel Varela (Oxford, GB); Ashling Holland (Oxford, GB)
Assignees: Oxford University Innovation Limited; United Kingdom Research and Innovation
A61K47/542A61K47/64A61K47/645
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Quick Facts
Patent No.
US 12,465,646
App. No.
17/311,062
Granted
Nov 11, 2025
Kind
B2
Abstract

The present invention relates to linkers for connecting a carrier molecule to a therapeutic molecule to form a conjugate, in particular linkers formed of amino acids such as glutamic acid, succinic acid, and gamma-aminobutyric acid. The present invention further relates to a conjugate comprising a linker of the invention, and the use of the conjugate in the treatment of various diseases.

Claims (32)

1 . A conjugate or a pharmaceutically acceptable salt or solvate thereof of the structure

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO.

2 . A conjugate or a pharmaceutically acceptable salt thereof, of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO.

3 . A conjugate of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO.

4 . A pharmaceutically acceptable salt of a conjugate of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO.

5 . A pharmaceutical composition comprising:

a conjugate or a pharmaceutically acceptable salt or solvate thereof, of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO; and

a pharmaceutically acceptable carrier.

6 . A pharmaceutical composition comprising:

a conjugate or a pharmaceutically acceptable salt thereof, of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO; and

a pharmaceutically acceptable carrier.

7 . A pharmaceutical composition comprising:

a conjugate of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO; and

a pharmaceutically acceptable carrier.

8 . A pharmaceutical composition comprising:

a pharmaceutically acceptable salt of a conjugate of the structure:

wherein the carrier is a peptide consisting of the sequence RBRRBRFQILYBRBR (SEQ ID NO: 70), wherein the peptide is N-acetylated, and

wherein the therapeutic molecule is an antisense oligonucleotide consisting of the sequence 5′-CAGCAGCAGCAGCAGCAGCAG-3′ (SEQ ID NO: 81), wherein the antisense oligonucleotide is a PMO; and

a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 1, 2024
From: RAZ, RICHARD; WOOD, MATTHEW; GODFREY, CAROLINE; MCCLOREY, GRAHAM; BANERJEE, SUBHASHIS; VARELA, MIGUEL; HOLLAND, ASHLING
To: OXFORD UNIVERSITY INNOVATION LIMITED
Reel/Frame 066965/0902 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 1, 2024
From: GAIT, MICHAEL
To: UNITED KINGDOM RESEARCH AND INNOVATION
Reel/Frame 066965/0910 →
Priority Claims (2)
GB 1820020 · Dec 7, 2018 · national
GB 1911405 · Aug 9, 2019 · national
Continuity (1)
Related Publication 20220125934A1 · Apr 28, 2022
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