# US 12,600,973 B2 · CpG ODN having immunoregulatory function and use thereof

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- Number: US 12,600,973 B2
- Document ID: US12600973B2
- Status: Granted
- Kind: B2
- Application number: 17/915,805
- Filed: 2021-03-31
- Published: 2023-05-25
- Granted: 2026-04-14
- Earliest claimed: 2020-04-01
- Assignees: Parr Biotechnology (Hebei) Co., Ltd.
- Applicants: Parr Biotechnology (Hebei) Co., Ltd.
- Inventors: Ligong Wang; Yan Shao
- Web page: https://patentgrep.com/patent/US12600973B2

## CPC

- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- C12N 15/117: Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs
- A61K 39/001156: {Tyrosinase and tyrosinase related proteinases [TRP-1 or TRP-2]}
- A61K 39/001192: {Glycoprotein 100 [Gp100]}
- A61K 39/205: Rhabdoviridae, e.g. rabies virus
- A61K 39/215: Coronaviridae, e.g. avian infectious bronchitis virus
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61P 31/14: for RNA viruses
- A61P 35/00: Antineoplastic agents
- A61P 37/04: Immunostimulants
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- A61K 2039/55505: {Inorganic adjuvants}
- A61K 2039/55561: {CpG containing adjuvants; Oligonucleotide containing adjuvants}
- C12N 2310/17: Immunomodulatory nucleic acids
- C12N 2310/315: Phosphorothioates
- C12N 2310/321: 2'-O-R Modification
- C12N 2310/322: 2'-R Modification
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- 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)
- 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)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

Provided are an immunomodulatory CpG ODN chemically modified by means of a structure as shown by general formula I and the use thereof. The CpG ODN has an immunostimulatory activity, can stimulate the proliferation of B cells, and produce specific cytokines. The above-mentioned CpG ODN can be used as a vaccine adjuvant alone or in combination with other adjuvants to exert a synergistic effect, and can also be used in the preparation of drugs for preventing or treating tumors, infections, and allergies.

## Claims

### Claim 1

An immunoregulatory CpG ODN with a maximum length of 26 bp comprising a nucleotide sequence selected from SEQ ID NOs: 1-4 and 6, wherein at least one nucleotide in the nucleotide sequence is a phosphorothioated nucleotide.

### Claim 2 (depends on 1)

The immunoregulatory CpG ODN of claim 1, wherein the immunoregulatory CpG ODN consists of a nucleotide sequence selected from the group consisting of SEQ ID NOs: 1-4 and 6, and wherein the nucleotide sequence is a completely-phosphorothioated nucleotide sequence.

### Claim 3 (depends on 1)

A method of preventing or treating tumors, microbial infections or allergies in a subject, wherein the method comprises administering an effective amount of the immunoregulatory CpG ODN of claim 1 to the subject.

### Claim 4 (depends on 3)

The method of claim 3, wherein the subject is a human or an animal, wherein the animal is a mouse, a rat, a domestic animal, or a domestic bird.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising the immunoregulatory CpG ODN of claim 1 and a pharmaceutically acceptable carrier.

### Claim 6 (depends on 5)

A method of preventing or treating tumors, microbial infections or allergies in a subject, wherein the method comprises administering an effective amount of the pharmaceutical composition of claim 5 to the subject.

### Claim 7 (depends on 1)

A vaccine adjuvant comprising the immunoregulatory CpG ODN of claim 1.

### Claim 8 (depends on 7)

The vaccine adjuvant of claim 7, further comprising one or more other adjuvants selected from the group consisting of insoluble aluminum salt colloids, oil-water emulsions, microorganisms and their metabolites, nucleic acids and the analogs thereof, cytokines, immunostimulatory complexes, propolis, or liposomes.

### Claim 9 (depends on 1)

A vaccine comprising the immunoregulatory CpG ODN of claim 1 and an antigen, wherein the antigen is a rabies antigen or a SARS-COV-2 antigen.

### Claim 10 (depends on 9)

The vaccine of claim 9, wherein the vaccine is a rabies vaccine for a human or an animal, and the immunoregulatory CpG ODN consists of a nucleotide sequence as set forth in SEQ ID NO: 3, wherein the nucleotide sequence is a completely-phosphorothioated nucleotide sequence, and the concentration of the CpG ODN is 0.01 μg/ml-1000 μg/ml.

### Claim 11 (depends on 9)

The vaccine of claim 9, wherein the vaccine is a SARS-COV-2 vaccine, and wherein the vaccine further comprises an aluminum adjuvant.

### Claim 12 (depends on 11)

The vaccine of claim 11, wherein the immunoregulatory CpG ODN consists of a nucleotide sequence as set forth in SEQ ID NO: 6, and wherein the nucleotide sequence is a completely-phosphorothioated nucleotide sequence.

### Claim 13 (depends on 10)

The vaccine of claim 10, wherein the concentration of the CpG ODN is 1 μg/ml-10 μg/ml.

### Claim 14 (depends on 11)

The vaccine of claim 11, wherein the aluminum adjuvant is aluminum hydroxide adjuvant.

### Claim 15 (depends on 11)

The vaccine of claim 11, wherein the vaccine is an inactivated SARS-COV-2 vaccine.

### Claim 16 (depends on 14)

The vaccine of claim 14, wherein the concentration of the antigen is 1 μg/mL-10 g/mL; the concentration of the aluminum hydroxide adjuvant is 1 μg/mL-1000 μg/mL; and the concentration of the immunoregulatory CpG ODN is 1 μg/mL-1000 μg/mL.

### Claim 17 (depends on 7)

A rabies vaccine comprising the vaccine adjuvant of claim 7.

### Claim 18 (depends on 17)

The rabies vaccine of claim 17, wherein the concentration of CpG ODN in the rabies vaccine is 0.01 μg/ml-1000 μg/ml.

### Claim 19 (depends on 17)

The rabies vaccine of claim 17, wherein the concentration of CpG ODN in the rabies vaccine is 1 μg/ml-10 μg/ml.

### Claim 20 (depends on 7)

A SARS-COV-2 vaccine comprising the vaccine adjuvant of claim 7.

### Claim 21 (depends on 20)

The SARS-COV-2 vaccine of claim 20, wherein the SARS-COV-2 vaccine is an inactivated SARS-COV-2 vaccine, and the concentration of CpG ODN in the SARS-COV-2 vaccine is 0.01 μg/ml-1000 μg/ml.

### Claim 22 (depends on 20)

The SARS-COV-2 vaccine of claim 20, wherein the SARS-COV-2 vaccine is an inactivated SARS-COV-2 vaccine, and the concentration of CpG ODN in the SARS-COV-2 vaccine is 1 μg/ml-10 μg/ml.