Chiral design
US-10160969-B2 · Dec 25, 2018 · US
Linkers
US12465646B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12465646-B2 |
| Application number | US-201917311062-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 6, 2019 |
| Priority date | Dec 7, 2018 |
| Publication date | Nov 11, 2025 |
| Grant date | Nov 11, 2025 |
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- Title
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- Abstract
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- Assignees and inventors
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- Key dates
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- First independent claim
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- CPC / IPC classifications
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- Citations and related patents
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Abstract
Official abstract text for this publication.
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.
First claim
Opening claim text (preview).
The invention claimed is: 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.
Assignees
Inventors
Classifications
- A61K47/542Primary
Carboxylic acids, e.g. a fatty acid or an amino acid · CPC title
containing oxygen, {e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides} · CPC title
Carboxylic acids; Salts or anhydrides thereof · CPC title
Amino acids, e.g. glycine, EDTA or aspartame · CPC title
Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US12465646B2 cover?
- 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.
- Who is the assignee on this patent?
- Univ Oxford Innovation Ltd, Res & Innovation Uk
- What technology area does this patent fall under?
- Primary CPC classification A61K47/542. Mapped technology areas include Human Necessities.
- When was this patent published?
- Publication date Tue Nov 11 2025 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 12 related publications on this page (citations in our corpus or others sharing the same primary CPC).