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    • 170. 发明授权
    • SUBSTITUTED (E)-STYRYL BENZYLSULFONES FOR TREATING PROLIFERATIVE DISORDERS
    • SUBSTITUIERTE(E)-STYRYLBENZYLSULFONE ZUR BEHANDLUNG PROLIFERATIVER ERKRANKUNGEN
    • EP1328511B1
    • 2010-03-24
    • EP01977567.5
    • 2001-10-05
    • Temple University - Of The Commonwealth System of Higher Education
    • REDDY, E., PremkumarREDDY, M., V., Ramana
    • C07C317/00C07C317/02A61K31/10
    • C07C317/18A61K31/10C07C317/10C07C317/28
    • (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1-C6 alkoxy, nitro, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R2 and R3 are independently selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, and dimethylamino (C2-C6 alkoxy); provided: R1 may not be halogen when R2 and R3 are both halogen; R2 may not be 2-halogen when R3 is 4-halogen; or a pharmaceutically acceptable salt thereof; or formula II: whrein: R4 is selected from the group consisting of C1-C6 alkoxy, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); R6 is selected from the group consisting of nitro, hydrogen, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R7 is selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, dimethylamino (C2-C6 alkoxy) and trifluoromethyl; provided R5 and R6 may not be hydrogen in the same compound; or a pharmaceutically acceptable salt thereof.
    • (E)可用作抗增殖剂的酪氨酸苄基砜,包括例如抗癌剂,根据式I提供:其中:R 1选自卤素,C 1 -C 6烷氧基 ,硝基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); R 2和R 3独立地选自卤素,C 1 -C 6烷氧基,C 1 -C 6烷基,硝基,氰基,羟基,膦酸根,氨基, 氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); 条件是:当R 2和R 3都是卤素时,R 1可以不是卤素; 当R 3为4-卤素时,R 2可以不为2-卤素; 或其药学上可接受的盐; 或式II化合物:其中:R 4选自C 1 -C 6烷氧基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); R 6选自硝基,氢,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基和二甲基氨基(C 2 -C 6烷氧基); 和R 7选自卤素,C 1 -C 6烷氧基,C 1 -C 6烷基,硝基,氰基,羟基,膦酰基,氨基,氨基磺酰基,羧基,乙酰氧基,二甲基氨基(C 2 -C 6 烷氧基)和三氟甲基; 提供的R 5和R 6可以不是同一化合物中的氢; 或其药学上可接受的盐。