# US 2010/0166805 A1 · Modulation of immunostimulatory properties by small oligonucleotide-based compounds

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- Number: US 2010/0166805 A1
- Document ID: US20100166805A1
- Status: Published application
- Kind: A1
- Application number: 12/592,850
- Filed: 2009-12-03
- Published: 2010-07-01
- Earliest claimed: 2003-12-08
- Assignees: Idera Pharmaceuticals, Inc.
- Inventors: Sudhir Agrawal; Fu-Gang Zhu; Ekambar Kandimalla
- Web page: https://patentgrep.com/patent/US20100166805A1

## CPC

- C12N 15/117: Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/04: Antipruritics
- A61P 31/00: Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P 31/10: Antimycotics
- A61P 31/12: Antivirals
- A61P 33/00: Antiparasitic agents
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/04: Immunostimulants
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 2039/55561: {CpG containing adjuvants; Oligonucleotide containing adjuvants}
- C12N 2310/17: Immunomodulatory nucleic acids
- C12N 2310/315: Phosphorothioates
- C12N 2310/318: where the PO2 is completely replaced, e.g. MMI or formacetal
- C12N 2310/3183: Diol linkers, e.g. glycols or propanediols
- C12N 2310/32: of the sugar
- C12N 2310/33: of the base
- C12N 2310/336: Modified G
- C12N 2310/52: branched
- 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

## Abstract

The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3′ ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5′ end.

## Claims

### Claim 1

A method for therapeutically treating a patient having airway inflammation, inflammatory disorders, allergy, or asthma, such method comprising administering to the patient an immunomer, wherein the immunomer has the sequence of 5′-TCRTCRTTG-X-GTTRCTRCT-5′, wherein R is arabinoguanosine and X is glycerol linker.

### Claim 2 (depends on 1)

The method according to claim 1, further comprising administering an antigen associated with said disease or disorder.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the immunomer or the antigen, or both, are linked to an immunogenic protein or non-immunogenic protein.

### Claim 4 (depends on 1)

The method according to claim 1, further comprising administering an adjuvant.

### Claim 5 (depends on 1)

The method according to claim 1, further comprising administering a co-stimulatory molecule selected from the group consisting of cytokines, chemokines, protein ligands, a trans-activating factors, peptides, and peptides comprising a modified amino acid.

### Claim 6

A method for preventing airway inflammation, inflammatory disorders, allergy, or asthma in a patient, such method comprising administering to the patient an immunomer, wherein the immunomer has the sequence of 5′-TCRTCRTTG-X-GTTRCTRCT-5′, wherein R is arabinoguanosine and X is glycerol linker.

### Claim 7 (depends on 6)

The method according to claim 6, further comprising administering an antigen associated with said disease or disorder.

### Claim 8 (depends on 6)

The method according to claim 6, wherein the immunomer or the antigen, or both, are linked to an immunogenic protein or non-immunogenic protein.

### Claim 9 (depends on 6)

The method according to claim 6, further comprising administering an adjuvant.

### Claim 10 (depends on 6)

The method according to claim 6, further comprising administering a co-stimulatory molecule selected from the group consisting of cytokines, chemokines, protein ligands, a trans-activating factors, peptides, and peptides comprising a modified amino acid.