申请人:BOBEL246 S.L.
公开号:EP0707849A1
公开(公告)日:1996-04-24
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 bisubstituted by (C₁-C₃)-alkyl; R⁴ is (C₁-C₄)-alkyl, (C₁-C₄)-acyl, CF₃, F, Cl, Br, I, carboxilo, (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-lipoxigenase inhibiting activity much higher than that of benaprofene or ketoconazol. These characteristics make the disclosed derivates extremely useful for the preparation of drugs against leukotrien-mediated diseases, such as rheumatoid arthritis, ulcerative colitis, asthma, psoriasis and herpes.
具有式 (I) 的产品 其中 R² 是 (C₁-C₄)-烷基、(C₁-C₄)-酰基、CF₃、Cl、Br 或 I;R³ 是 H、(C₁-C₄)-烷基、(C₁-C₄)-酰基、(C₁-C₄)-烷氧基、CF₃、F、Cl、Br、苯基、OH、SH、NH₂ 或由(C₁-C₃)-烷基单取代或双取代的氨基;R⁴ 是 (C₁-C₄)- 烷基、(C₁-C₄)-酰基、CF₃、F、Cl、Br、I、羧基、(C₁-C₄)-丙氧羰基、氰基、硝基或苯基;R⁶为 H、(C₁-C₄)-烷基、(C₁-C₄)酰基、CF₃、Cl、Br 或 I,上述产物具有低毒性,其 5-脂氧原酶抑制活性远高于苯并吡芬或酮康唑。这些特性使得所公开的衍生物在制备治疗白三烯介导的疾病(如类风湿性关节炎、溃疡性结肠炎、哮喘、牛皮癣和疱疹)的药物时极为有用。