Cox-2 selective carprofen for treating pain and inflammation...

A - Human Necessities – 61 – K

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A61K 31/40 (2006.01)

Patent

CA 2288759

Treating or preventing inflammatory processes and diseases in dogs associated with the activity of inducible cyclo-oxygenase-2 (COX-2), while at the same time reducing or eliminating undesirable side effects associated with simultaneous inhibition of the activity of constitutive cyclo-oxygenase-1 (COX- 1) by selectively inhibiting COX-2 activity with reference to COX-1 activity, wherein the selectivity ratio or COX-2 : COX-1 activity inhibition is at least 3 : 1 based on ex vivo inhibition levels measured in whole blood; the inhibitor is a member selected from the group of anti-inflammatory compounds consisting essentially of salicylic acid derivatives, p-aminophenol derivatives, indole and indene acetic acids, heteroaryl acetic acids, arylpropionic acids, anthranilic acids, enolic acids, and alkanones; the inhibitor in particular is comprised of (+)(S)-enantiomer of 6-chloro-.alpha.- methyl-9H-carbazole-2-acetic acid.

L'invention porte sur des procédés de traitement ou de prévention des inflammations chez les chiens ou des maladies associées à l'activité de cyclo-oxygénase-2 (COX-2) inductive, et simultanément sur la réduction ou l'élimination d'effets secondaires indésirables associés à l'inhibition simultanée de l'activité de cyclo-oxygénase-1 (COX-1) constitutive en sélectionnant sélectivement l'activité de COX-2 en tenant compte de l'activité de COX-1, le rapport de sélectivité ou d'inhibition de l'activité de COX-2 : COX-1 étant au moins de 3 : 1 sur la base des taux d'inhibition ex vivo relevés dans le sang entier; l'inhibiteur est un élément sélectionné dans le groupe des composés anti-inflammatoires constitués principalement des dérives d'acide salicylique, des dérivés de p-aminophénol, d'indole et des acides acétiques d'indène, des acides acétiques d'hétéroaryle, des acides arylproprioniques, des acides anthraniliques, des acides énoliques et des alcanones; l'inhibiteur comprend notamment (+)(S)-énantiomère de l'acide 6-chloro-.alpha.-méthyl-9H-carbazole-2-acétique.

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