Antisense oligonucleotides (ODN) against SMAD7 and uses thereof in medical field

Patent metadata

Field	Value
Publication number	US-9382541-B2
Application number	US-201514815339-A
Country	US
Kind code	B2
Filing date	Jul 31, 2015
Priority date	Apr 2, 2003
Publication date	Jul 5, 2016
Grant date	Jul 5, 2016

Abstract

The invention relates to antisense oligonucleotidic sequences (ODN) against Smad7 suitably modified, and their uses in medical field as therapeutic biological agents, in particular in the treatment of chronic inflammatory bowel disease, such as Crohn's disease and ulcerative colitis.

First claim

The invention claimed is:

1. An oligonucleotide comprising SEQ ID NO:2 (5′-GTXYCCCCTTCTCCCXYCAG-3′) wherein X is C and Y is G, and wherein at least one CG grouping is modified.

2. The oligonucleotide of claim 1 , wherein at least one of the nucleotides X comprises a methylated nitrogenous base.

3. The oligonucleotide of claim 2 , wherein the nitrogenous base is 5-methyl-cytosine.

4. The oligonucleotide of claim 1 , wherein at least one internucleoside linkage is a phosphorothioate linkage or a methylphosphonate linkage.

5. The oligonucleotide of claim 1 , wherein all internucleoside linkages are phosphorothioate linkages.

6. A pharmaceutical composition comprising the oligonucleotide of claim 1 , and a pharmaceutically acceptable adjuvant and/or excipient.

7. The pharmaceutical composition of claim 6 , wherein the pharmaceutical composition is an oral pharmaceutical composition.

8. A method of treating inflammatory bowel disease, comprising administering to a patient in need thereof an effective amount of the oligonucleotide of claim 1 , wherein the oligonucleotide is effective to treat inflammatory bowel disease.

9. The method of claim 8 , wherein the inflammatory bowel disease is Crohn's disease.

10. The method of claim 8 , wherein the inflammatory bowel disease is ulcerative colitis.

Assignees

• Nogra Pharma Ltd

Inventors

• Monteleone Giovanni

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61P1/00

  Drugs for disorders of the alimentary tract or the digestive system · CPC title

• A61P1/04

  for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants · CPC title

• C12N2310/3125

  Methylphosphonates · CPC title