Cycloalkylhydroxyureas and their use as lipoxygenase inhibitors

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 275/64 (2006.01) A61K 31/17 (2006.01) A61K 31/21 (2006.01) C07C 323/47 (2006.01)

Patent

CA 2160140

The present invention provides a novel N-hydroxyurea compound of chemical formula (I) wherein R1 and R2 are each independently hydrogen or C1-C4 alkyl; Ar is phenyl or mono-, di- or trisubstituted phenyl; A is a valence bond or a C1-C6 alkylene chain, optionally having one double bond or one triple bond in the chain, and optionally having one or more C1-C4 alkyl groups attached to the chain; X is oxygen or sulfur; n is an integer of 3 to 6; M is hydrogen, pharmaceutically acceptable cation or a metabolically cleavable group; and X and A may be attached at any available position on the ring. These compounds are useful for treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

La présente invention décrit un nouveau composé N-hydroxyurée de la formule chimique (I) dans laquelle R1 et R2 sont chacun indépendamment hydrogène ou alkyle C1-C4; Ar est phényle ou phényle mono, di ou trisubstitué; A est une liaison de valence ou une chaîne alkylène C1-C6, possédant éventuellement une double liaison ou une triple liaison dans la chaîne, et présentant éventuellement un ou plusieurs groupes alkyle C1-C4 fixés à la chaîne; X est oxygène ou soufre; n est un entier compris entre 3 et 6; M est hydrogène, un cation pharmaceutiquement acceptable ou bien un groupe métaboliquement clivable; et X et A peuvent être accolés à n'importe quelle position disponible sur le noyau. Ces composés sont utiles pour traiter ou atténuer les affections inflammatoires, les allergies et les maladies cardio-vasculaires chez les mammifères, et comme principe actif dans des compositions pharmaceutiques permettant de traiter de telles affections.

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