# US 12,600,964 B2 · Compound for treatment of heart failure

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- Number: US 12,600,964 B2
- Document ID: US12600964B2
- Status: Granted
- Kind: B2
- Application number: 17/529,119
- Filed: 2021-11-17
- Published: 2022-05-26
- Granted: 2026-04-14
- Earliest claimed: 2017-12-15
- Assignees: Medizinische Hochschule Hannover
- Applicants: Medizinische Hochschule Hannover
- Inventors: Thomas Thum; Sandor Batkai; Ariana Foinquinos
- Web page: https://patentgrep.com/patent/US12600964B2

## CPC

- C12N 15/11: DNA or RNA fragments; Modified forms thereof (DNA or RNA not used in recombinant technology, C07H21/00); {Non-coding nucleic acids having a biological activity}
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- A61K 31/712: Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A61P 19/04: for non-specific disorders of the connective tissue
- C07H 21/04: with deoxyribosyl as saccharide radical
- C12N 2310/113: targeting other non-coding nucleic acids, e.g. antagomirs
- C12N 2310/315: Phosphorothioates
- C12N 2310/3231: having an additional ring, e.g. LNA, ENA
- C12N 2310/346: having a combination of backbone and sugar modifications
- C12N 2310/351: Conjugate
- C12N 2320/31: Combination therapy
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)

## Abstract

The present invention refers to an oligonucleotide which is an effective inhibitor of microRNA miR-132 and its use in medicine, particularly in the prevention or treatment of cardiac and/or fibrotic disorders.

## Claims

### Claim 1

An oligonucleotide comprising a sequence of formula III:
5′-dA*+T*dG*+G*dC*+T*dG*+T*dA*+G*dA*dC*dT*dG*+T*+T-3′ (SEQ ID NO: 3)
wherein dA is 2′-deoxyadenosine, dG is 2′-deoxyguanosine, dC is 2′-deoxycytidine and T is thymidine, wherein +T is an LNA-T building block and +G is an LNA-G building block, and wherein * is a phosphorothioate linkage,
the oligonucleotide being conjugated to a heterologous moiety, wherein the heterologous moiety is a lipid moiety.

### Claim 2 (depends on 1)

The oligonucleotide of claim 1, wherein the heterologous moiety comprises a N-galactosamine.

### Claim 3 (depends on 1)

The oligonucleotide of claim 1, wherein the heterologous moiety is conjugated at the 5′ or 3′ terminus of the oligonucleotide.