申请人:GLAXO GROUP LIMITED
公开号:EP0340030A2
公开(公告)日:1989-11-02
Compounds of formula I
wherein R¹ represents a hydrogen or a halogen atom, or a group selected from hydroxy, C₁₋₆ alkyl, C₁₋₆ alkoxy, phenylC₁₋₃alkoxy (in which the phenyl group is unsubstituted or substituted by a halogen atom or a C₁₋₃ alkyl, C₁₋₃ alkoxy or hydroxy group), nitro, trifluoromethyl, cyano, -CO₂R³ (wherein R³ represents a hydrogen atom or a C₁₋₄ alkyl group) and -CONR⁴R⁵ (wherein R⁴ and R⁵ each independently represents a hydrogen atom or a C₁₋₄ alkyl group, or together with the nitrogen atom to which they are attached form a saturated 5- to 7-membered ring, which ring optionally contains one or more atoms selected from an oxygen or a sulphur atom, or a group -NH- or -N(CH₃)-); and R² represents a hydrogen or halogen atom, or a hydroxy, C₁₋₆ alkyl or C₁₋₆ alkoxy group; and salts thereof are inhibitors of the enzyme 5-lipoxygenase.
Processes for preparing the compounds of formula (I) and compositions containing them are also described.
式 I 的化合物
其中 R¹ 代表氢原子或卤素原子,或选自羟基、C₁₋₆ 烷基、C₁₋₆ 烷氧基的基团、苯基₁₋₃烷氧基(其中苯基未被取代或被卤原子或 C₁₋₃烷基、C₁₋₃烷氧基或羟基取代)、硝基、三氟甲基、氰基、-CO₂R³(其中 R³ 代表氢原子或 C₁₋₄ 烷基)和 -CONR⁴R⁵(其中 R⁴ 和 R⁵ 各自独立地代表氢原子或 C₁₋₄ 烷基、或与所连接的氮原子一起形成饱和的 5 至 7 元环,该环可选择包含一个或多个选自氧原子或硫原子的原子,或一个基团 -NH- 或 -N(CH₃)-);和 R² 代表氢原子或卤素原子,或羟基、C₁₋₆ 烷基或 C₁₋₆ 烷氧基;其盐类是 5-脂氧合酶的抑制剂。
还描述了制备式 (I) 化合物的工艺和含有它们的组合物。