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    Substituted styryl benzylsulfones for treating proliferative disorders
    24.
    发明公开
    Substituted styryl benzylsulfones for treating proliferative disorders 审中-公开
    取代基苯乙烯基苄基砜zur Behandlung von Proliferationskrankheiten

    公开(公告)号：EP2359819A1

    公开(公告)日：2011-08-24

    申请号：EP10178360.3

    申请日：2001-04-13

    申请人： Temple University - Of The Commonwealth System of Higher Education

    发明人： Reddy, E. Premkumar ,  Reddy, M.V. Ramana

    IPC分类号： A61K31/10 ,  A61K31/19 ,  A61K31/216

    CPC分类号： C07C323/52 ,  C07C317/10 ,  C07C317/18 ,  C07C317/44 ,  C07C323/60 ,  C07F9/12

    摘要： Styryl benzylsulfones of formula I are useful as ant-proliferative agents, including, for example, anticancer agents. In formula I:

    (a) (i) R 1 , R 2 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;
    (ii) R 3 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, provided at least three of R 1 , R 2 , R 3 , R 4 and R 5 are other than hydrogen; and
    (iii) R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl;

    or
    (b) (i) R 6 , R 8 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and R 7 and R 9 are hydrogen; and
    (ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;

    or
    (c) (i) at least four of R 6 , R 7 , R 8 , R 9 and R 10 are halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl, and the remainder of R 6 , R 7 , R 8 , R 9 and R 10 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy) or trifluoromethyl; and
    (ii) R 1 , R 2 , R 3 , R 4 and R 5 are hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, nitro, cyano, carboxyl, hydroxyl, phosphonato, amino, sulfamyl, acetoxy, dimethylamino(C2-C6 alkoxy), or trifluoromethyl;

    or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式I的苯乙烯基苄基砜可用作抗增殖剂，包括例如抗癌剂。 在式I中：（a）（i）R 1，R 2，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酸根，氨基，氨磺酰基， 乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基; （ⅱ）R 3为氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，羧基，羟基，膦酸基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基， 1，R 2，R 3，R 4和R 5不同于氢; 和（iii）R 6，R 7，R 8，R 9和R 10是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基， （C 2 -C 6烷氧基）或三氟甲基; 或（b）（i）R 6，R 8和R 10是卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基 ）或三氟甲基，R 7和R 9为氢; 和（ii）R 1，R 2，R 3，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基， （C 2 -C 6烷氧基）或三氟甲基; 或（c）（i）R 6，R 7，R 8，R 9和R 10中的至少四个为卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酸根，氨基， 亚磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基，R 6，R 7，R 8，R 9和R 10的其余部分为氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基 ，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基，二甲基氨基（C 2 -C 6烷氧基）或三氟甲基; 和（ii）R 1，R 2，R 3，R 4和R 5是氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氰基，羧基，羟基，膦酰基，氨基，氨基磺酰基，乙酰氧基， （C 2 -C 6烷氧基）或三氟甲基; 或其药学上可接受的盐。