Antisense nucleic acid targeting PCSK9
US-11273222-B2 · Mar 15, 2022 · US
Antisense nucleic acid targeting PCSK9
US12544449B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12544449-B2 |
| Application number | US-202217649895-A |
| Country | US |
| Kind code | B2 |
| Filing date | Feb 3, 2022 |
| Priority date | May 26, 2017 |
| Publication date | Feb 10, 2026 |
| Grant date | Feb 10, 2026 |
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Abstract
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Provided is an oligonucleotide conjugate comprising an oligonucleotide and two or more linearly connected asialoglycoprotein receptor-binding molecules attached to the oligonucleotide, wherein the oligonucleotide comprises a locked nucleoside analog having a bridging structure between the 4′ and 2′ positions, is complementary to a human PCSK9 gene, and has inhibitory activity on the expression of the human PCSK9 gene. The oligonucleotide conjugate of the present invention can be used in the field of pharmaceutical products, in particular, the field of the development and production of therapeutic agents for diseases associated with a high LDL cholesterol level.
First claim
Opening claim text (preview).
The invention claimed is: 1 . An oligonucleotide conjugate comprising an oligonucleotide and a functional molecule attached to the oligonucleotide via a linker, wherein the functional molecule is at least one selected from the group consisting of sugars, antibodies, aptamers, intercalators, reporter molecules, polyamines, polyamides, polyethylene glycols, thioethers, polyethers, cholesterols, thiocholesterols, cholic-acid moieties, folic acid, lipids, phospholipids, biotin, phenazine, phenanthridine, anthraquinone, adamantane, acridine, fluorescein, rhodamine, coumarin, and pigments, wherein the linker comprises a main-chain linker that binds to the oligonucleotide and a side-chain linker that is branched from the main-chain and binds to the functional molecule, wherein the linker has the following structure (I): 2 . The oligonucleotide conjugate according to claim 1 , wherein the functional molecule is at least one selected from the group consisting of sugars, antibodies, and aptamers. 3 . The oligonucleotide conjugate according to claim 1 , wherein the functional molecule is at least one selected from the group consisting of cholesterols, thiocholesterols, cholic-acid moieties, folic acid, lipids, phospholipids, biotin, and adamantane. 4 . The oligonucleotide conjugate according to claim 1 , wherein the functional molecule is at least one selected from the group consisting of polyethylene glycols, thioethers, and polyethers. 5 . The oligonucleotide conjugate according to claim 1 , wherein the functional molecule is at least one selected from the group consisting of intercalators, reporter molecules, polyamines, polyamides, anthraquinone, phenanthridine, acridine, and phenazine. 6 . The oligonucleotide conjugate according to claim 1 , wherein the functional molecule is at least one selected from the group consisting of fluorescein, rhodamine, coumarin, and pigments.
Assignees
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Classifications
Conjugate · CPC title
having an additional ring, e.g. LNA, ENA · CPC title
Phosphorothioates · CPC title
Antisense · CPC title
- C12N15/1137Primary
against enzymes (viral enzymes C12N15/1131; receptors C12N15/1138) · CPC title
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- What does patent US12544449B2 cover?
- Provided is an oligonucleotide conjugate comprising an oligonucleotide and two or more linearly connected asialoglycoprotein receptor-binding molecules attached to the oligonucleotide, wherein the oligonucleotide comprises a locked nucleoside analog having a bridging structure between the 4′ and 2′ positions, is complementary to a human PCSK9 gene, and has inhibitory activity on the expression …
- Who is the assignee on this patent?
- Nat Cerebral & Cardiovascular Ct
- What technology area does this patent fall under?
- Primary CPC classification C12N15/1137. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Feb 10 2026 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 6 related publications on this page (citations in our corpus or others sharing the same primary CPC).