申请人:Glaxo Group Limited
公开号:US05023255A1
公开(公告)日:1991-06-11
Triazine derivatives of formula (I) ##STR1## or salts thereof, wherein R.sup.1 represents a halogen atom or a group selected from hydroxy; C.sub.1-8 alkyl C.sub.1-6 alkoxy; C.sub.1-3 alkoxy C.sub.1-3 alkoxy; phenoxy or phenyl C.sub.1-3 alkoxy, wherein the phenyl group is optionally substituted by a halogen atom or a group selected from C.sub.1-3 alkyl, C.sub.1-3 alkoxy, or hydroxy; fluoro C.sub.1-3 alkyl; cyano; --CO.sub.2 R.sup.3, wherein R.sup.3 represents a hydrogen atom or a C.sub.1-4 alkyl group; --CONR.sup.4 R.sup.5, wherein R.sup.4 and R.sup.5 each independently represents a hydrogen atom or a C.sub.1-4 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 selected from --NH-- or --N(CH.sub.3)--; and R.sup.2 represents a hydrogen or halogen atom, or a group selected from hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkoxy; are inhibitors of the enzyme 5-lipoxygenase. Processes for preparing the triazine derivatives of formula (I) and compositions containing them are also described.
式(I)的三嗪衍生物或其盐,其中R.sup.1代表卤原子或从羟基中选择的基团; C.sub.1-8烷基C.sub.1-6烷氧基; C.sub.1-3烷氧基C.sub.1-3烷氧基; 苯氧基或苯基C.sub.1-3烷氧基,其中苯基可选择地被卤原子或从C.sub.1-3烷基,C.sub.1-3烷氧基或羟基中选择的基团取代; 氟代C.sub.1-3烷基; 氰基; --CO.sub.2R.sup.3,其中R.sup.3代表氢原子或C.sub.1-4烷基; --CONR.sup.4R.sup.5,其中R.sup.4和R.sup.5各自独立地代表氢原子或C.sub.1-4烷基,或者与它们连接的氮原子一起形成饱和的5-至7-成员环,该环可选择地含有一个或多个从氧原子或硫原子中选择的原子,或从--NH--或--N(CH.sub.3)--中选择的基团; 和R.sup.2代表氢或卤原子,或从羟基,C.sub.1-6烷基或C.sub.1-6烷氧基中选择的基团; 是5-脂氧合酶的抑制剂。还描述了制备式(I)的三嗪衍生物的方法和含有它们的组合物。