申请人:Knoll Aktiengesellschaft
公开号:US05780482A1
公开(公告)日:1998-07-14
Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which one of A or B represents N and the other represents N or C--R.sub.3 ; R.sub.1 represents hydrogen, halo, alkyl, hydroxy, carboxyalkenyl, alkoxycarbonylalkenyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxy, halogenated alkyl, carboxy, alkoxycarbonyl, alkanoylamino or carbamoylalkenyl; R.sub.2 represents hydrogen, alkyl, halo, alkoxy, hydroxy, alkanoyloxy, or phenoxy; R.sub.3 represents hydrogen or alkyl; R.sub.4 represents hydrogen, halo, alkoxycarbonyl, cyano, benzyloxycarbonyl, alkanoyl, benzoyl, alkyl, carboxy, alkylthio or carbamoyl; R.sub.5 represents hydrogen or alkyl; R.sub.9 represents hydrogen or alkyl; R.sub.10 represents phenyl, pyridyl or pyrimidinyl substituted by OR.sub.6 and optionally further substituted wherein R.sub.6 represents hydrogen, alkyl, alkoxycarbonyl or carbamoyl, alicyclic hydrocarbon, phenyl, cycloalkylalkyl, arylalkyl or pyridyl; or when R.sub.10 represents phenyl, OR.sub.6 represents a monosaccharide group or a disaccharide group; which are antirheumatic agents. Compositions containing these compounds and processes to prepare them are also disclosed.
公式I的化合物及其药学上可接受的盐,其中A或B中的一个代表N,另一个代表N或C-R.sub.3; R.sub.1代表氢,卤素,烷基,羟基,羧基烯基,烷氧羰基烯基,羟基烷基,羧基烷基,烷氧羰基烷基,烷氧基,卤代烷基,羧基,烷氧羰基,烷酰胺基或
氨基烯基; R.sub.2代表氢,烷基,卤素,烷氧基,羟基,烷酰氧基或苯氧基; R.sub.3代表氢或烷基; R.sub.4代表氢,卤素,烷氧羰基,
氰基,苄氧羰基,烷酰基,苯甲酰基,烷基,羧基,烷
硫基或
氨基
甲烷基; R.sub.5代表氢或烷基; R.sub.9代表氢或烷基; R.sub.10代表取代为OR.sub.6的苯基,
吡啶基或
嘧啶基,可选择进一步取代,其中R.sub.6代表氢,烷基,烷氧羰基或
氨基
甲烷基,脂
环烃,苯基烷基,芳基烷基或
吡啶基; 或者当R.sub.10代表苯基时,OR.sub.6代表
单糖基或
双糖基; 这些化合物是抗风湿药物。还公开了含有这些化合物的组合物和制备它们的方法。