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    • 9. 发明授权
    • Substituted pyrazolyl benzenesulfonamides
    • 取代的吡唑基苯磺酰胺
    • US5510496A
    • 1996-04-23
    • US456441
    • 1995-06-01
    • John J. TalleyThomas D. PenningPaul W. CollinsJames W. MalechaStephen R. BertenshawMatthew J. Graneto
    • John J. TalleyThomas D. PenningPaul W. CollinsJames W. MalechaStephen R. BertenshawMatthew J. Graneto
    • A61K31/415A61P11/06A61P17/06C07D231/12C07D231/14C07D231/16C07D231/54C07D401/04C07D403/04C07D405/04C07D409/04C07D495/04
    • C07D405/04C07D231/12C07D231/14C07D231/16C07D231/54C07D401/04C07D403/04C07D409/04C07D495/04
    • A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 is selected from sulfamyl, fluoro, chloro, methyl, hydroxyl, methoxy and trifluoromethyl: wherein R.sup.2 is selected from hydrido, difiuoromethyl, trifluoromethyl, amido, dichloromethyl, trichloromethyl, pentafluoroethyl, cyano, heptatluoropropyl, difluorochloromethyl, methoxycarbonyl, dichlorofluoromethyl, N-phenylamido, N-3-fluorophenyl) amido, 2-pyridylamido, N-(4-methylphenyl)amido, hydroxypropyl, N-(3-chlorophenyl)amido, N-(4-methoxyphenyl)amido, hydroxymethyl, hydroxyethyl, carboxylpropyl, carboxymethyl and carboxyethyl; wherein R.sup.3 is selected from hydrido, methyl, triflouromethyl, fluoro, chloro and bromo; wherein R.sup.4 is selected from phenyl, biphenyl, pyrazinyl, cyclohexyl, cyclohexenyl and thienyl; and wherein R.sup.4 is optionally substituted at a substitutable position with one or more radicals selected from chloro, bromo, fluoro, methylthio, methylsulfonyl, morpholinyl, amino, methyl, ethyl, propyl, isopropyl, butyl, ethoxy, nitro, chloromethyl, trifluoromethoxy, trifluoroenhoxy, fluoromethyl, methoxy, difluoromethyl, trifluoromethyl, dichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, and difluoropropyl; or wherein R.sup.3 and R.sup.4 together form ##STR2## provided R.sup.2 and R.sup.3 are not both hydrido; or a pharmaceutically-acceptable salt thereof.
    • 描述了一类吡唑基苯磺酰胺化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式I定义:其中R 1选自氨磺酰基,氟,氯,甲基,羟基,甲氧基和三氟甲基:其中R 2选自氢,二氟甲基,三氟甲基,酰氨基,二氯甲基, 三氯甲基,五氟乙基,氰基,七氟丙基,二氟氯甲基,甲氧基羰基,二氯氟甲基,N-苯基酰氨基,N-3-氟苯基)酰氨基,2-吡啶基酰氨基,N-(4-甲基苯基)酰氨基,羟丙基,N-(3-氯苯基) N-(4-甲氧基苯基)酰氨基,羟甲基,羟乙基,羧基丙基,羧甲基和羧乙基; 其中R 3选自氢,甲基,三氟甲基,氟,氯和溴; 其中R 4选自苯基,联苯基,吡嗪基,环己基,环己烯基和噻吩基; 并且其中R 4在可取代位置任选被一个或多个选自氯,溴,氟,甲硫基,甲基磺酰基,吗啉基,氨基,甲基,乙基,丙基,异丙基,丁基,乙氧基,硝基,氯甲基,三氟甲氧基,三氟甲氧基 氟甲基,甲氧基,二氟甲基,三氟甲基,二氯甲基,五氟乙基,七氟丙基,二氟氯甲基,二氯氟甲基,二氟乙基和二氟丙基; 或者其中R3和R4一起形成“IMAGE”,其中R2和R3不都是氢的; 或其药学上可接受的盐。