# US 11,028,395 B2 · TNF-alpha-binding aptamer, and therapeutic use for same

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- Number: US 11,028,395 B2
- Document ID: US11028395B2
- Status: Granted
- Kind: B2
- Application number: 16/344,107
- Filed: 2016-10-24
- Published: 2019-10-24
- Granted: 2021-06-08
- Earliest claimed: 2016-10-24
- Assignees: Biois Co., Ltd
- Applicants: Biois Co., Ltd.
- Inventors: Sung-Chun Kim
- Web page: https://patentgrep.com/patent/US11028395B2

## CPC

- C12N 15/115: Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith {; Nucleic acids binding to non-nucleic acids, e.g. aptamers}
- A61K 31/7105: Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
- C12N 15/1048: {SELEX}
- C12N 2310/16: Aptamers
- C12N 2310/31: of the backbone
- C12N 2310/32: of the sugar
- C12N 2310/321: 2'-O-R Modification
- C12N 2310/334: Modified C
- C12N 2310/335: Modified T or U
- C12N 2310/344: Position-specific modifications, e.g. on every purine, at the 3'-end
- C12N 2310/351: Conjugate
- 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)

## Abstract

The present invention relates to a TNF-α-binding RNA aptamer disclosed in SEQ ID NO: 1 or SEQ ID NO: 2, and to the therapeutic use thereof.

## Claims

### Claim 1

An RNA aptamer or a variant thereof, comprising SEQ ID NO: 1 or SEQ ID NO: 2 and binding to TNF-α.

### Claim 2 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is a modified aptamer, and the modified aptamer is an aptamer which is chemically modified in at least one position of a sugar position, a phosphate position, a base position, a 5′ end position and a 3′ end position of a ribonucleotide.

### Claim 3 (depends on 2)

The aptamer of claim 2, wherein the modified aptamer is an aptamer modified at the sugar position, and the aptamer is configured such that at least one hydroxyl group of the sugar is modified with any one of a halogen group, an aliphatic group, an ether group, and an amine group.

### Claim 4 (depends on 2)

The aptamer of claim 2, wherein the modified aptamer is an aptamer modified at the sugar position, and the aptamer is configured such that a 2′-OH group of the sugar is modified with any one of OMe, O-alkyl, O-allyl, S-alkyl, S-allyl and halogen.

### Claim 5 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is a modified aptamer, and the modified aptamer is configured such that all C and U of SEQ ID NO: 1 or SEQ ID NO: 2 are 2′-F-modified C and 2′-F-modified U, respectively.

### Claim 6 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is an aptamer modified at a phosphate position, and the modified aptamer is configured such that a phosphate is modified with P(O)S (“thioate”), P(S)S (“dithioate”), P(O)NR2 (“amidate”), P(O)R, P(O)OR′, CO or CH2 (“formacetal”).

### Claim 7 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is an aptamer modified at a base position, and the modified aptamer is configured such that a 5-position of pyrimidine, an 8-position of purine, a 4-position of uracil, a 5-position of uracil, or an exocyclic amine position of cytosine is modified.

### Claim 8 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is an aptamer modified at a 5′ end position, and the modified aptamer is configured such that —NH2 is bound to the 5′ end.

### Claim 9 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is an aptamer modified at a 3′ end position, and the modified aptamer is configured such that an inverted thymidine is bound to form a 3′-3′linkage.

### Claim 10 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is modified by connecting polyalkylene glycol via a linker or without a linker.

### Claim 11 (depends on 1)

The aptamer of claim 1, wherein the RNA aptamer is modified by connecting polyethylene glycol via a linker or without a linker.

### Claim 12 (depends on 11)

The aptamer of claim 11, wherein the RNA aptamer is modified through introduction of polyethylene glycol at a 5′ end position using amine (R—NH2) as a linker.

### Claim 13 (depends on 1)

A pharmaceutical composition, comprising the aptamer of claim 1.