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    • 4. 发明授权
    • Dihydroquinone and dihydronaphthridine inhibitors of JNK
    • 二氢醌和二氢萘并吡嗪类抑制剂
    • US08163906B2
    • 2012-04-24
    • US12152432
    • 2008-05-14
    • Sarah C. AbbotGeneviève N. BoiceBernd BuettelmannDavid Michael GoldsteinLeyi GongJoan Heather HoggPravin IyerKristen Lynn McCalebYun-chou Tan
    • Sarah C. AbbotGeneviève N. BoiceBernd BuettelmannDavid Michael GoldsteinLeyi GongJoan Heather HoggPravin IyerKristen Lynn McCalebYun-chou Tan
    • C07D471/04
    • C07D215/48C07D401/06C07D401/12C07D405/06C07D405/12C07D413/04C07D471/04
    • Compounds of formula I are effective modulators of JNK: wherein X is CR11 or N; Y is —C(O)R3, 5-membered heteroaryl, or 5-membered heterocyclyl; Z is phenyl, cycloalkyl, heterocyclyl or heteroaryl, and is substituted with R1 and R2; R1 and R2 are each independently H, halo, CN, lower alkyl, or —Y1—Y2—Y3—R8, or R1 and R2 together form —O(CH2)nO—, where n is 1 or 2; Y1 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —S—, —SO2—, or a bond; Y2 is cycloalkylene, heterocycloalkylene, lower alkylene or a bond; Y3 is —O—, —C(O)—, —C(O)O—, —C(O)NR9—, —NR9C(O)—, —SO2—, or a bond; R8 is H, lower alkyl, lower alkoxy, cycloalkyl, heterocycloalkyl, or —NR9R10, wherein R8 other than H is optionally substituted with lower alkyl, halo, —CF3, or —OH; R9 and R10 are each independently H or lower alkyl; R3 is OH, lower alkyl, lower alkoxy, (lower alkoxy)-lower alkoxy, or —NR9R10; R4 is lower alkyl, phenyl, heterocyclyl, cycloalkyl, heterocycloalkyl, or heteroaryl, and is optionally substituted with lower alkyl, hydroxy, lower alkoxy, halo, nitro, amino, cyano, or halo-lower alkyl; R5 and R6 are each independently H, halo, cyano, lower alkyl, —CF3, lower alkoxy, —OCHF2, —NO2, or —NR9R10; R7 is H, F, Cl, methyl, or OH; R11 is H, lower alkyl, lower cycloalkyl, or phenyl; or a pharmaceutically acceptable salt thereof.
    • 式I化合物是JNK的有效调节剂:其中X是CR11或N; Y是-C(O)R 3,5元杂芳基或5元杂环基; Z是苯基,环烷基,杂环基或杂芳基,并被R1和R2取代; R1和R2各自独立地为H,卤素,CN,低级烷基或-Y1-Y2-Y3-R8,或R1和R2一起形成-O(CH 2)n O-,其中n为1或2; Y1是-O - , - C(O) - , - C(O)O - , - C(O)NR 9 - , - NR 9 C(O) - , - S - , - SO 2 - 或键; Y2是亚环烷基,杂环亚烷基,低级亚烷基或键; Y 3是-O - , - C(O) - , - C(O)O-,-C(O)NR 9 - , - NR 9 C(O) - , - SO 2 - 或键; R8是H,低级烷基,低级烷氧基,环烷基,杂环烷基或-NR9R10,其中R8以外的R8任选被低级烷基,卤素,-CF 3或-OH取代; R9和R10各自独立地为H或低级烷基; R3是OH,低级烷基,低级烷氧基,(低级烷氧基) - 低级烷氧基或-NR9R10; R 4是低级烷基,苯基,杂环基,环烷基,杂环烷基或杂芳基,并且任选被低级烷基,羟基,低级烷氧基,卤素,硝基,氨基,氰基或卤代低级烷基取代。 R 5和R 6各自独立地为H,卤素,氰基,低级烷基,-CF 3,低级烷氧基,-OCHF 2,-NO 2或-NR 9 R 10; R7是H,F,Cl,甲基或OH; R11是H,低级烷基,低级环烷基或苯基; 或其药学上可接受的盐。