US 12,544,449 B2Granted

Antisense nucleic acid targeting PCSK9

AssigneeNational Cerebral and Cardiovascular Center

InventorsMariko Harada-Shiba, Fumito Wada, Satoshi Obika, Tsuyoshi Yamamoto, Keisuke Tachibana, Tadayuki Kobayashi, Kosuke Ito, Motoki Sawamura

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Abstract

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.

Claims6

Dependent claims

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):

Dependencies are inferred from the claim text.

Facts

Application: 17/649,895Filed 3 Feb 2022 · continuation
Priority: JP 2017-10512126 May 2017
Published: US 2022/0160880 A126 May 2022
Granted: 10 Feb 2026
Term ends: Not estimatedThe source records don’t support an estimate.

Classification17 codes

A61K 47/549
The modifying agent being an organic compound: sugars, nucleosides, nucleotides or nucleic acids
A61K 47/54
The non-active ingredient being a modifying agent: the modifying agent being an organic compound
A61K 48/00
Medicinal preparations containing genetic material which is inserted into cells of the
A61P 3/06
Drugs for disorders of the metabolism: antihyperlipidemics

Family

PCT/JP2018/020081Parent of this continuation · filed 24 May 2018
US 2022/0160880 A1Pre-grant publication · published 26 May 2022
Application16/616,724Parent of this continuation
US 11,273,222 B2Parent of this continuation
US 2021/0170032 A1Published application
US 12,544,449 B2This patent

From the US filing history. Foreign family members aren’t listed.