# US 7,038,029 B2 · Immunostimulatory oligonucleotides and uses thereof

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- Number: US 7,038,029 B2
- Document ID: US7038029B2
- Status: Granted
- Kind: B2
- Application number: 10/309,775
- Filed: 2002-12-04
- Published: 2004-01-08
- Granted: 2006-05-02
- Earliest claimed: 2002-05-30
- Assignees: Immunotech
- Inventors: Ricardo Agustin Lopez
- Web page: https://patentgrep.com/patent/US7038029B2

## CPC

- C12N 15/117: Nucleic acids having immunomodulatory properties, e.g. containing CpG-motifs
- A61K 31/7088: Compounds having three or more nucleosides or nucleotides
- A61K 39/00: Medicinal preparations containing antigens or antibodies (materials for immunoassay G01N33/53)
- A61K 39/39: characterised by the immunostimulating additives, e.g. chemical adjuvants
- A61P 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 13/10: of the bladder
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/04: Antipruritics
- A61P 31/18: for HIV
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- 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
- C07H 21/00: Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- 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

Oligonucleotides containing the non-palindromic sequence motif: X1X2X3X4X5X6X7X8, wherein X1 is C,T,G or A (preferably T or C); wherein X2 is C,T,G or A; wherein X7 is C,T,G or A (preferably G); at least three, and preferably all, of X3, X4, X5, X6 and X8 are T; and with the proviso that, in the motif, a C does not precede a G (in other terms, the nucleic acid motif does not consist of a CpG oligonucleotide), that modulate the immune response of animals of the order Primate, including humans, are disclosed. This immune modulation is characterized by stimulation of proliferation, differentiation, cytokine production and antibody production on B-cells and cell differentiation on plasmacytoid dendritic cells.

## Claims

### Claim 1

An immunostimulatory oligonucleotide having 24 to 100 nucleotides, comprising the nucleotide sequence
TCATCATTTTGTCATTTTGTCATT (SEQ ID No 2).

### Claim 2 (depends on 1)

The immunostimulatory oligonucleotide of claim 1, wherein the immunostimulatory oligonucleotide is encapsulated in a slow release delivery vehicle.

### Claim 3 (depends on 1)

The immunostimulatory oligonucleotide of claim 1, wherein the immunostimulatory oligonucleotide is included in a pharmaceutically acceptable carrier.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising an immunostimulatory oligonucleotide according to claim 1 and a pharmaceutically acceptable carrier.

### Claim 5 (depends on 4)

A composition according to claim 4, wherein said immunostimulatory oligonucleotide is included in a plasmid.

### Claim 6 (depends on 4)

A composition according to claim 4, further comprising an antigen.

### Claim 7 (depends on 6)

A composition according to claim 6, wherein the antigen is selected from the group consisting of viruses, bacteria, fungi, parasites, tumor cells, toxins, allergens, proteins, glycolipids, and polysaccharides.

### Claim 8 (depends on 6)

A composition according to claim 6, wherein the antigen is a viral antigen, a bacterial antigen, a human or animal tumor cell antigen, or a fungal antigen.

### Claim 9 (depends on 4)

A composition according to claim 4, further comprising a plasmid encoding an antigen.

### Claim 10 (depends on 9)

A composition according to claim 9, wherein the encoded antigen is a viral antigen, a bacterial antigen, a human or animal tumor cell antigen, or a fungal antigen.

### Claim 11

An immunostimulatory oligonucleotide consisting of the nucleotide sequence
TCATCATTTTGTCATTTTGTCATT (SEQ ID No 2).