# US 11,298,371 B2 · Regulation of nucleic acid molecule expression

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- Number: US 11,298,371 B2
- Document ID: US11298371B2
- Status: Granted
- Kind: B2
- Application number: 16/754,595
- Filed: 2018-10-11
- Published: 2020-08-20
- Granted: 2022-04-12
- Earliest claimed: 2017-10-11
- Assignees: Nitto Denko Corporation
- Applicants: Nitto Denko Corporation
- Inventors: Kenjiro Minomi; Naoko Urushihara; Yusuke Nakashima; Hiroyuki Tanaka; Erika Terada
- Web page: https://patentgrep.com/patent/US11298371B2

## CPC

- A61K 31/713: Double-stranded nucleic acids or oligonucleotides
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- 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)}
- C12N 2310/14: interfering nucleic acids [NA]
- C12N 2310/141: MicroRNAs, miRNAs
- C12N 2310/3231: having an additional ring, e.g. LNA, ENA
- C12N 2310/532: Closed or circular
- C12N 2320/53: reducing unwanted side-effects
- 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
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention provides a nucleic acid molecule dimer that includes a first nucleic acid molecule having complementarity with at least part of a target nucleic acid molecule, and a second nucleic acid molecule having complementarity with the first nucleic acid molecule, wherein the first nucleic acid molecule has a linear form, the second nucleic acid molecule has a cyclic form, and the first and second nucleic acid molecules at least partially form a double strand.

## Claims

### Claim 1

A nucleic acid molecule dimer comprising:
a first nucleic acid molecule of 15 to 30 mer having at least 80% complementarity to at least a portion of a target nucleic acid molecule; and
a second nucleic acid molecule of 12 to 30 mer having at least 76% complementarity to the first nucleic acid molecule,
wherein the first nucleic acid molecule is linear, the second nucleic acid molecule is circular, and the first nucleic acid molecule and the second nucleic acid molecule at least partially form a duplex.

### Claim 2 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule is longer than the second nucleic acid molecule.

### Claim 3 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the 3′ end or the 5′ end of the first nucleic acid molecule forms a overhang.

### Claim 4 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule forms a nick.

### Claim 5 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the length of the first nucleic acid molecule is 19 to 21 mer.

### Claim 6 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the length of the second nucleic acid molecule is 16 to 25 mer.

### Claim 7 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule and/or the second nucleic acid molecule is modified.

### Claim 8 (depends on 1)

A composition comprising the nucleic acid molecule dimer according to claim 1.

### Claim 9 (depends on 1)

A pharmaceutical composition comprising the nucleic acid molecule dimer according to claim 1 and one or more pharmaceutically acceptable additives.

### Claim 10 (depends on 1)

A method for modulating the expression of a target nucleic acid molecule, comprising administering an effective amount of the nucleic acid molecule dimer according to claim 1 to a cell containing the target nucleic acid molecule.

### Claim 11 (depends on 10)

The method according to claim 10, wherein the method is performed in vitro, ex vivo or in vivo.

### Claim 12 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule has at least 85% complementarity to at least a portion of a target nucleic acid molecule.

### Claim 13 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule has at least 90% complementarity to at least a portion of a target nucleic acid molecule.

### Claim 14 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the second nucleic acid molecule has at least 80% complementarity to the first nucleic acid molecule.

### Claim 15 (depends on 1)

The nucleic acid molecule dimer according to claim 1, wherein the first nucleic acid molecule has at least 90% complementarity to the first nucleic acid molecule.

### Claim 16 (depends on 10)

The method according to claim 10, wherein the method is performed in vitro or ex vivo.