
Different classes of anti-inflammatory drugs are known to inhibit cycloxygenase enzymes (COXs). However inhibition of the COX by common non-steroidal anti-inflammatory drugs is also known to cause side effects such as gastric ulceration due to lack of selectivity between COX-1 and COX-2. Moreover, some of these drugs, containing a nitrophenyl nucleus, present a high risk of toxicity.
The laboratory has discovered new pyridinic sulfonamide derivatives developed for the treatment of inflammation (arthrosis, rheumatoid arthritis) and pain.
· Advantages
This invention is based on the isosteric replacement of the nitrobenzenic nucleus of N-(nitrophenyl)alkanesulfonamide NSAIDs by a pyridine nucleus. It results in:
- a strong anti-inflammatory activity in vivo in animal models ;
- a beneficial profile as COX-2 preferential or COX-2 selective inhibitors;
- expected poor side effects and toxicity.
· Potential Applications
The pyridinic sulfonamide derivatives can enter in pharmaceutical
composition as active therapeutic substances in the treatment of
diseases in which they can play a role as COX-2
preferential/selective inhibitors (arthrosis, cancer, pain…).
Granted : US 7226936, RU 2309148, AU 202337116, EP 1432684
Pending : WO 03/029217 – US 2007-0173534A1, CA 2460144, JP 2005-504125
The laboratory is looking for out-licensing opportunity for the compounds and their method of synthesis.
· Development stage
Different news compounds have been identified and their synthesis is set up. In vivo studies in animals show promising results.
Mr Julian Vultaggio
Transfer technology Advisor
The Interface Entreprises-Université is a multidisciplinary team committed to industry, which is responsible of the Liège University technology transfer (IP protection, licences, spinoff
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