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    • 9. 发明授权
    • Diaryl sulphide derivatives
    • 二芳基硫化物衍生物
    • US4771062A
    • 1988-09-13
    • US18091
    • 1987-02-20
    • Siegfried RaddatzHans PlumpeRomanis FruchtmannChristian KohlsdorferBernhard Pelster
    • Siegfried RaddatzHans PlumpeRomanis FruchtmannChristian KohlsdorferBernhard Pelster
    • C07D277/18C07D277/38C07D277/42C07D279/06A61K31/425
    • C07D279/06C07D277/18C07D277/42
    • A diaryl sulphide derivative of the formula ##STR1## in which R.sup.1 represents a thiazolamino radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, alkyl, aralkyl or acyl,R.sup.6 and R.sup.6 ' are identical or different and represent hydrogen, alkyl, aralkyl or aryl,R.sup.7 represents alkyl, cycloalkyl, aralkyl, acyl or aryl andn represents the number 1 or 2,R.sup.2 and R.sup.3 are identical or different and represent hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represent a group of the formula ##STR3## wherein R.sup.8 and R.sup.9 are identical or different and represent hydrogen, alkyl, aryl, aralkyl, acyl, trifluoroacetyl, alkylsulphonyl, arylsulphonyl, trifluoromethylphenylsulphonyl or tolylsulphonyl andR.sup.4 has one of the abovementioned meanings or R.sup.1, or represents hydrogen, alkyl, alkenyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, aryl, aralkyl, aryloxy, aralkoxy, aralkylthio, acyl, carboxyl, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, nitro, cyano or halogen, or represents a group of the formula ##STR4## wherein R.sup.8 and R.sup.9 have the abovementioned meanings, and salts thereof. Such diaryl sulphide derivatives being useful as active compounds in the treatment and prevention of diseases of the respiratory tract and cardiovascular diseases.
    • 式(I)的二芳基硫化物衍生物,其中R 1表示下式的噻唑烷基:其中R 5表示氢,烷基,芳烷基或酰基,R 6和R 6'相同或不同 代表氢,烷基,芳烷基或芳基,R7代表烷基,环烷基,芳烷基,酰基或芳基,n代表数字1或2,R2和R3相同或不同,代表氢,烷基,烯基,环烷基,烷氧基,烷硫基 ,卤代烷基,卤代烷氧基,卤代烷硫基,芳基,芳烷基,芳氧基,芳烷氧基,芳烷硫基,酰基,羧基,烷氧基羰基,羧基烷基,烷氧基羰基烷基,硝基,氰基或卤素,或表示下式的基团:其中R8和R9相同或 代表氢,烷基,芳基,芳烷基,酰基,三氟乙酰基,烷基磺酰基,芳基磺酰基,三氟甲基苯磺酰基或甲苯磺酰基,R4具有上述含义之一或R 1,或表示氢,烷基,烯基,C 烷氧基,烷硫基,卤代烷基,卤代烷氧基,卤代烷硫基,芳基,芳烷基,芳氧基,芳烷氧基,芳烷硫基,酰基,羧基,烷氧基羰基,羧基烷基,烷氧基羰基烷基,硝基,氰基或卤素,或表示下式的基团其中R8 和R9具有上述含义及其盐。 这种二芳基硫化物衍生物可用作活性化合物,用于治疗和预防呼吸道疾病和心血管疾病。