SUBSTITUTED PHENYL DERIVATIVES, THEIR PREPARATION AND USE
    12.
    发明申请
    SUBSTITUTED PHENYL DERIVATIVES, THEIR PREPARATION AND USE 审中-公开
    取代苯基衍生物,其制备和使用

    公开(公告)号:WO98047879A1

    公开(公告)日:1998-10-29

    申请号:PCT/DK1998/000162

    申请日:1998-04-21

    Abstract: A compound having formula (I) or a pharmaceutically acceptable salt thereof wherein one of R , R and R is a cyclic or heterocyclic acidic functional group having a pKa value below 8 or a group which is convertible in vivo to such a group; R , R and the two other substitutents R , R and R are each independently selected from hydrogen; alkyl; alkoxy; hydroxy; halogen; trifluoromethyl; cyano; nitro; amino; alkylamino; -COOR ; -NHSO2-alkyl; -SO2N(R )2; -SO2OR ; -CO-R ; aryl, biphenyl, phenylamino, phenoxy or heteroaryl, wherein the aryl, biphenyl, phenylamino, phenoxy or heteroaryl group may be substituted one or more times with substituents selected from alkyl, hydroxy, alkoxy, halogen, trifluoromethyl, cyano, nitro, amino and alkylamino; aryl and heteroaryl, or R and R or R and R together form a cyclic structure and the other substituents R , R , R , R and R is as defined above; and R is hydrogen, alkyl, amino or phenyl; Y is -CO-, -CS-, -SO2-, or -C(=N-R )-, wherein R is hydrogen, alkyl, or cyano; X is -NH-, -CH2-NH-, or -SO2-NH-; Z is NR , O, -CH=CH-, -N=CH-, or -CH=N-; R is hydrogen, or alkyl; R , R , R , R and R are each independently selected from hydrogen; alkyl; alkoxy; hydroxy; halogen; trifluoromethyl; cyano; nitro; amino; alkylamino; -COOR ; -NHSO2-alkyl; -SO2N(R )2; -SO2OR ; -CO-R ; aryl, biphenyl, phenylamino, phenoxy or heteroaryl, wherein the aryl, biphenyl, phenylamino, phenoxy or heteroaryl group may be substituted one or more times with substituents selected from alkyl, hydroxy, alkoxy, halogen, trifluoromethyl, cyano, nitro, amino and alkylamino; aryl and heteroaryl, or one of R and R , R and R , R and R and R and R together form a cyclic structure and the other substituents R , R , R , R and R is as defined above and R is as defined above; these compounds are particularly useful in the treatment of sickle-cell anaemia.

    Abstract translation: 具有式(I)的化合物或其药学上可接受的盐,其中R 1,R 2和R 3之一是pKa值低于8的环状或杂环酸性官能团或可转化的基团 在这样一个群体中; R 4,R 5和另外两个取代基R 1,R 2和R 3各自独立地选自氢; 烷基; 烷氧基; 羟基; 卤素; 三氟甲基; 氰基; 硝基; 氨基; 烷基; -COOR <7>; -NHSO 2 - 烷基; -SO 2 N(R <7>)2; -SO 2 OR <7>; -CO-R <7>; 芳基,联苯基,苯基氨基,苯氧基或杂芳基,其中芳基,联苯基,苯基氨基,苯氧基或杂芳基可以被选自烷基,羟基,烷氧基,卤素,三氟甲基,氰基,硝基,氨基和烷基氨基的取代基取代一次或多次 ; 芳基和杂芳基,或R 3和R 4或R 4和R 5一起形成环状结构,而其它取代基R 1,R 2,R 3, 4>和R 5如上所定义; 和R 7是氢,烷​​基,氨基或苯基; Y是-CO - , - CS-,-SO 2 - 或-C(= N-R 8) - ,其中R 8是氢,烷基或氰基; X是-NH-,-CH 2 -NH-或-SO 2 -NH-; Z是NR 6,O,-CH = CH-,-N = CH-或-CH = N-; R 6是氢或烷基; R 11,R 12,R 13,R 14和R 15各自独立地选自氢; 烷基; 烷氧基; 羟基; 卤素; 三氟甲基; 氰基; 硝基; 氨基; 烷基; -COOR <7>; -NHSO 2 - 烷基; -SO 2 N(R <7>)2; -SO 2 OR <7>; -CO-R <7>; 芳基,联苯基,苯基氨基,苯氧基或杂芳基,其中芳基,联苯基,苯基氨基,苯氧基或杂芳基可以被选自烷基,羟基,烷氧基,卤素,三氟甲基,氰基,硝基,氨基和烷基氨基的取代基取代一次或多次 ; 芳基和杂芳基,或R 11和R 12之一,R 12和R 13,R 13和R 14和R 14和R 15一起形成环状 结构和其它取代基R 11,R 12,R 13,R 14和R 15如上所定义,R 7如上所定义; 这些化合物特别可用于治疗镰状细胞性贫血。

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