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    • 2. 发明申请
    • 5-LIPOXYGENASE INHIBITORS
    • 5-LIPOXYGENASE抑制剂
    • WO2009146871A1
    • 2009-12-10
    • PCT/EP2009/003906
    • 2009-06-01
    • JACKSON, William Paul
    • JACKSON, William Paul
    • A61K31/18C07C311/21A61P35/00
    • A61K31/18C07C311/21C07C311/46
    • The use of compounds of the formula (I) Ar 1 -L 1 -Ar 2 -L 2 -C(R 3 )(R 4 )N(OR 1 )C(=Y)-R 2 (I) where Y is selected from O or S; R 1 is H, a salt or readily hydrolysable substituent; R 2 is selected from H or CH 3 , CH 2 F, CF 2 H or CF 3 ; R 3 and R 4 are selected independently from H, C 1-4 alkyl or alkenyl, CF 3 , CH 2 F, CF 2 H and F, with the proviso that if either R 3 or R 4 is H, then the other is not H; L 1 is a linker group; L 2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar 1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar 2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of 5-lipoxygenase mediated cancer provide improved therapies due to the effective inhibition of 5- lipoxygenase and long duration of activity in vivo after oral administration.
    • 使用式(I)Ar1-L1-Ar2-L2-C(R3)(R4)N(OR1)C(= Y)-R2(I)的化合物,其中Y选自O或S; R1是H,一种盐或易水解的取代基; R2选自H或CH3,CH2F,CF2H或CF3; R 3和R 4独立地选自H,C 1-4烷基或烯基,CF 3,CH 2 F,CF 2 H和F,条件是如果R 3或R 4是H,则另一个不是H; L1是连接基团; L2是包含任选取代或未取代的不饱和支链或直链烷基的连接基团; Ar 1是任选取代或未取代的芳基或杂环基; 并且Ar2是任选取代或未取代的芳基或杂环基,在5-脂氧合酶介导的癌症的治疗中,由于在口服给药后有效抑制5-脂氧合酶和长时间的活性,提供了改善的疗法。