Pyridazinones as prostaglandin endoperoxide h synthase...

C - Chemistry – Metallurgy – 07 – D

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C07D 237/14 (2006.01) A61K 31/50 (2006.01)

Patent

CA 2294548

The present invention describes pyridazinone compounds which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).

La présente invention concerne des composés de pyridazinone inhibiteurs des cyclooxygénases (COX) et notamment des inhibiteurs sélectifs de la cyclooxygénase-2 (COX-2). COX-2 est l'isoforme inductible associée à l'inflammation, par opposition à l'isoforme constitutive, la cyclooxygénase-1 (COX-1), qui est une enzyme "domestique" importante dans beaucoup de tissus, notamment le tractus gastro-intestinal (GI) et les reins. La sélectivité de ces composés vis-à-vis de COX-2 réduit les effets secondaires rénaux ou gastro-intestinaux des anti-inflammatoires non stéroïdiens (AINS) actuellement sur le marché.

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