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.
化学式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、烷硫基或氨基甲酰;R.sub.5代表氢或烷基;R.sub.9代表氢或烷基;R.sub.10代表苯基、吡啶基或嘧啶基,被OR.sub.6取代,并且可选择进一步取代,其中R.sub.6代表氢、烷基、烷氧羰基或氨基,脂环烃、苯基、环烷基烷基、芳基烷基或吡啶基;或当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。揭示了含有这些化合物的组合物和制备它们的方法。