申请人:Bayer Aktiengesellschaft
公开号:US05093340A1
公开(公告)日:1992-03-03
New phenylsulphonamides 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 substitutents 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## B denotes --O--; ##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.
新的苯磺酰胺化合物的化学式为:##STR1## 其中,R.sup.1表示未取代或取代的吡啶基、喹啉基或异喹啉基,取代基包括卤素、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表示氢、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表示未取代或取代的芳基,取代基包括卤素、卤代烷基、卤代烷氧基、烷基、烷氧基、烷基硫醇、烷基磺酰基、氰基、硝基或烷氧羰基,取代基可以相同或不同,或表示五氟苯基或未取代或取代的直链、支链或环状烷基,取代基包括卤素、芳基、芳氧基、氰基、烷氧羰基、烷氧基、烷基硫醚或三氟甲基;X表示--O--、--A--B--或--B--A--基团,其中A表示--O--或##STR2## B表示--O--;##STR3## 当X表示--O--基团时,R.sup.1不表示吡啶基。这些化合物的盐是通过将适当的胺与磺酰卤反应制备的。取代的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。