申请人:Bayer Aktiengesellschaft
公开号:US05070096A1
公开(公告)日:1991-12-03
New phenylsulphonamide of the formula in which ##STR1## R.sup.1 represents a pyridyl, quinolyl or isoquinolyl radical which is unsubstituted or substituted by halogen, alkyl, cycloalkyl, alkoxy, cyano, nitro, halogenoalkyl, halogenoalkoxy, alkoxycarbonyl or alkylsulphonyl, R.sup.2 represents hydrogen, cyano, nitro, halogen, alkyl, alkoxy, halogenoalkyl, halogenoalkoxy or alkoxycarbonyl, R.sup.3 represents an aryl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted by halogen, halogenoalkyl, halogenoalkoxy, alkyl, alkoxy, alkylthio, alkylsulphonyl, cyano, nitro or alkoxycarbonyl, the substituents being identical or different, or represents pentafluorophenyl or represents a straight-chain, branched or cyclic alkyl which is unsubstituted or substituted by halogen, aryl, aryloxy, cyano, alkoxycarbonyl, alkoxy, alkylthio or trifluoromethyl, and X represents an --O--, --A--B-- or --B--A-- group where A denotes --O--, ##STR2## and B denotes --CH.sub.2 -- or ##STR3## where R.sup.1 does not represent a pyridyl radical when x represents an --O-- group, and salts thereof are prepared by reacting appropriate amines with sulphonyl halides. The substituted phenylsulphonamides can be employed as active compounds for inhibiting enzymatic reactions and for inhibiting thrombocyte aggregations.
新的苯磺酰胺的化学式如下:
R.sup.1代表未取代或取代的吡啶基、喹啉基或异喹啉基,取代基可以是卤素、烷基、环烷基、烷氧基、氰基、硝基、卤代烷基、卤代烷氧基、烷氧羰基或烷基磺酰基;R.sup.2代表氢、氰基、硝基、卤素、烷基、烷氧基、卤代烷基、卤代烷氧基或烷氧羰基;R.sup.3代表未取代或经卤素、卤代烷基、卤代烷氧基、烷基、烷氧基、烷硫基、烷基磺酰基、氰基、硝基或烷氧羰基单取代、双取代或三取代的芳基;取代基可以相同也可以不同,或者代表五氟苯基,或者代表未取代或经卤素、芳基、芳氧基、氰基、烷氧羰基、烷氧基、烷硫基或三氟甲基取代的直链、支链或环烷基;X代表--O--,--A--B--或--B--A--基团,其中A代表--O--,B代表--CH.sub.2--或--CH.sub.2--,R.sup.1在X代表--O--基团时不代表吡啶基;这些化合物及其盐是通过适当的胺与磺酰卤反应制备而成。这些取代苯磺酰胺可以作为抑制酶反应和抑制血小板聚集的活性化合物使用。