Phenylpyridone derivatives,processes for their preparation and pharmaceutical compositions containing them.
申请人:SMITH KLINE & FRENCH LABORATORIES
LIMITED
公开号:EP0347027A2
公开(公告)日:1989-12-20
Compounds of the formula (1):
and pharmaceutically acceptable salts are described, wherein X is O or S; R¹ is C₁₋₆alkyl, C₂₋₆alkenyl, C₃₋₅cycloalkylC₁₋₄alkyl, or C₁₋₄alkyl substituted by 1 to 6 fluoro groups; R² is hydrogen, -CN, -CONR⁵R⁶, -CO₂R⁷, 5-tetrazolyl, -NO₂, -NH₂ or -NHCOR⁸ wherein R⁵, R⁶, R⁷ and R⁸ are independently hydrogen or C₁₋₄alkyl; R³ is hydrogen or C₁₋₄alkyl; and R⁴ is hydrogen or C₁₋₄alkyl; with the proviso that R¹ is not methyl when R² is -CO₂H, -CO₂CH₂CH₃ or -CN, X is 0, R³ is hydrogen and R⁴ is hydrogen or methyl.
These compounds have bronchodilator, anti-allergic, vasodilator and anti-inflammatory activities. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of the compounds of the formula (1) are described.
描述了式(1)化合物
和药学上可接受的盐,其中 X 是 O 或 S;R¹ 是 C₁₋₆烷基、C₂₋₆烯基、C₃₋₅环烷基或被 1 至 6 个氟基团取代的 C₁₋₄ 烷基;R² 是氢、-CN、-CONR⁵R⁶、-CO₂R⁷、5-四唑基、-NO₂、-NH₂ 或 -NHCOR⁸,其中 R⁵、R⁶、R⁷ 和 R⁸ 独立地是氢或 C₁₋₄;R³是氢或C₁₋₄alkyl;R⁴是氢或C₁₋₄alkyl;但R¹不是甲基,当R²是-CO₂H、-CO₂CH₂CH₃或-CN时,X是0,R³是氢,R⁴是氢或甲基。
这些化合物具有支气管扩张、抗过敏、血管扩张和抗炎活性。本文介绍了药物组合物以及使用方法。描述了式 (1) 化合物的制备工艺。