The search for new COX-2 inhibitors: a review of 2002 – 2008 patents

Background: Two COX isoenzymes are known, COX-1 and COX-2, for which the main inhibitors are the NSAIDs. The common anti-inflammatory drugs (such as aspirin, ibuprofen and naproxen) all act by blocking the action of both the COX-1 and COX-2 enzymes. The COX-2 inhibitors represent a new class of drugs that do not affect COX-1 but selectively block COX-2. This selective action provides the benefits of reducing inflammation without irritating the stomach and cardiovascular effects. Objective: This review focuses on patents published in the field during 2002 – 2008, paying particular attention to promising COX-2 inhibitors. Conclusion: Structural analogues of the COX-2 inhibitors celecoxib and valdecoxib, and novel potential pyridazine, triazole, indole and thione derivatives emerge as promising leads for the treatment of inflammation, pain and other diseases.