Use of derivatives of 2,4-bisubstituted phenols as...

Details Use of derivatives of 2,4-bisubstituted phenols as... Use of derivatives of 2,4-bisubstituted phenols as...

C - Chemistry, Metallurgy

07

C

C07C 39/26 (2006.01) A61K 31/055 (2006.01) A61P 29/00 (2006.01) C07C 39/27 (2006.01)

Patent

CA 2160161

Products having formula (I) wherein R2 is (C1-C4)-alkyl, (C1-C4)-acyl, CF3, Cl, Br or I; R3 is H, (C1-C4)-alkyl, (C1- C4)-acyl, (C1-C4)-alcoxyl, CF3, F, Cl, Br, phenyl, OH, SH, NH2 or amino mono- or disubstituted by (C1-C4)-alkyl; R4 is (C1-C4)-alkyl, (C1-C4)-acyl, CF3, F, Cl, I, carboxyl, (C1- C4)-alcoxycarbonyl, cyano, nitro or phenyl; and R6 is H, (C1-C4)-alkyl, (C1-C4)-acyl, CF3, Cl, Br or I, said products presenting, together with a low toxicity, a 5-lipoxygenase inhibiting activity much higher than that of benoxaprofen or ketoconazole. These characteristics make the disclosed derivatives extremely useful for the preparation of medicaments against leukotriene-mediated diseases are involved, such as rheumatoid arthritis, ulcerative colitis, asthma, psoriasis and herpes.

Les produits ayant la formule (I) dans laquelle R<2> représente (C1-C4)-alkyle, (C1-C4)-acyle, CF3, Cl, Br ou I; R<3> représente H, (C1-C4)-alkyle, (C1-C4)-acyle, (C1-C4)-alcoxyle, CF3, F, Cl, Br, phényle, OH, SH, NH2 ou amino mono- ou bisubstitué par (C1-C3)-alkyle; R<4> représente (C1-C4)-alkyle, (C1-C4)-acyle, CF3, F, Cl, Br, I, carboxyle, (C1-C4)-alcoxycarbonyle, cyano, nitro ou phényle; et R<6> représente H, (C1-C4)-alkyle, (C1-C4)-acyle, CF3, Cl, Br ou I, présentent, conjointement à une faible toxicité, une activité inhibitrice de la 5-lipoxygénase bien supérieure à celle du benaprofène ou du ketoconazol. Ceci rend les dérivés de l'invention extrêmement utiles pour la préparation de médicaments contre des maladies induites par leucotriènes, telles que l'arthrite rumathoïde, la collite ulcéreuse, l'asthme, le psoriasis et l'herpès.

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