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    • 3. 发明申请
    • Novel orally active iron (III) chelators
    • 新型口服活性铁(III)螯合剂
    • US20020068758A1
    • 2002-06-06
    • US09944113
    • 2001-09-04
    • BTG International Limited.
    • Robert Charles HiderGary Stuart TilbrookZudong Liu
    • A61K031/357C07D319/04
    • C07D213/69C07D213/81C07D309/40C07D417/06C07D493/04
    • A novel 3-hydroxypyridinone compound of formula I is provided 1 wherein R is hydrogen or a group that is removed by metabolism in vivo to provide the free hydroxy compound, R1 is an aliphatic hydrocarbon group or an aliphatic hydrocarbon group substituted by a hydroxy group or a carboxylic acid ester, sulpho acid ester or a C1-6 alkoxy, C6 -aryloxy or C7-10 aralkoxy ether thereof, R3 is selected from hydrogen and C1-6 alkyl; and R4 is selected from hydrogen, C1-6 alkyl and a group as described for R2 ; characterized in that R2 is selected from groups (i) nullCONHnullR5 (ii) nullCH2NHCOnullR5 (iii) nullSO2NHnullR5 (iv) nullCH2NHSO2nullR5 (v) nullCR6R6OR7 (viii) nullCONHCOR5 wherein R5 is selected from hydrogen and optionally hydroxy, alkoxy, or aralkoxy substituted C1-13 alkyl, aryl and C7-13 aralkyl, R6 is independently selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl, and R7 is selected from hydrogen, C1-13 alkyl, aryl and C7-13 aralkyl or a pharmaceutically acceptable salt of any such compound with the proviso that when R7 is hydrogen, R6 is not selected from aryl and with the proviso that the compound is not 1-ethyl-2-(1null-hydroxyethyl)-3-hydroxypyridin-4-one.
    • 提供式I的新颖的3-羟基吡啶酮化合物,其中R是氢或通过体内代谢除去以提供游离羟基化合物的基团,R 1是脂族烃基或被羟基取代的脂族烃基或 羧酸酯,磺酸酯或C 1-6烷氧基,C 6芳氧基或C 7-10芳烷氧基醚,R 3选自氢和C 1-6烷基; 并且R 4选自氢,C 1-6烷基和如对于R 2所述的基团; 其特征在于R2选自基团(ⅰ)-CONH-R5(ⅱ)-CH2NHCO-R5(ⅲ)-SO2NH-R5(ⅳ)-CH2NHSO2-R5(ⅴ)-CR6R6OR7(ii)-CONHCOR5,其中选择R5 由氢和任选的羟基,烷氧基或芳烷氧基取代的C 1-13烷基,芳基和C 7-13芳烷基,R 6独立地选自氢,C 1-13烷基,芳基和C 7-13芳烷基,并且R 7选自氢,C 1 -13烷基,芳基和C7-13芳烷基或任何此类化合物的药学上可接受的盐,条件是当R7为氢时,R6不选自芳基,条件是该化合物不是1-乙基-2-( 1'-羟乙基)-3-羟基吡啶-4-酮