Arylpyridazinones as prostaglandin endoperoxide h synthase...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 237/14 (2006.01) A61K 31/50 (2006.01) C07D 237/18 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 405/06 (2006.01) C07D 409/06 (2006.01) C07D 409/12 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07F 11/00 (2006.01)

Patent

CA 2299300

The present invention describes pyridazinone compounds of formula III, which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX/2), COX-2 us 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 marked non-steroidal anti-inflammatory drugs (NSAIDs).

L'invention porte sur des composés de pyridazinone inhibiteurs de la cyclo-oxygénase (COX) et en particulier inhibiteurs sélectifs de la cyclo-oxygénase-2 (COX-2), laquelle représente l'isoforme inductible associée à l'inflammation par opposition à l'isoforme constitutive, la cyclo-oxygénase-1 (COX-1), qui est une importante enzyme "ménagère" présente dans beaucoup de tissus, y compris les voies digestives (GI) et les reins. La sélectivité desdits composés vis-à-vis du COX-2 réduit les effets secondaires indésirables affectant les voies digestives (GI) et les reins observés avec les anti-inflammatoires non stéroïdiens (NSAID) actuellement sur le marché.

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