利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

9 条记录 (耗时 0.061 秒)

    Dihydroquinone and dihydronaphthridine inhibitors of JNK
    3.
    发明授权
    Dihydroquinone and dihydronaphthridine inhibitors of JNK 有权
    二氢醌和二氢萘并吡嗪类抑制剂

    公开(公告)号：US08163906B2

    公开(公告)日：2012-04-24

    申请号：US12152432

    申请日：2008-05-14

    申请人： Sarah C. Abbot ,  Geneviève N. Boice ,  Bernd Buettelmann ,  David Michael Goldstein ,  Leyi Gong ,  Joan Heather Hogg ,  Pravin Iyer ,  Kristen Lynn McCaleb ,  Yun-chou Tan

    发明人： Sarah C. Abbot ,  Geneviève N. Boice ,  Bernd Buettelmann ,  David Michael Goldstein ,  Leyi Gong ,  Joan Heather Hogg ,  Pravin Iyer ,  Kristen Lynn McCaleb ,  Yun-chou Tan

    IPC分类号： C07D471/04

    CPC分类号： C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04

    摘要： 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.

    摘要翻译： 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。

    Pyrimidinyl pyridone inhibitors of JNK
    7.
    发明授权
    Pyrimidinyl pyridone inhibitors of JNK 失效
    JNK的嘧啶基吡啶酮抑制剂

    公开(公告)号：US08404695B2

    公开(公告)日：2013-03-26

    申请号：US12603726

    申请日：2009-10-22

    申请人： Genevieve N. Boice ,  Leyi Gong ,  Kristen Lynn McCaleb ,  Wylie Solang Palmer

    发明人： Genevieve N. Boice ,  Leyi Gong ,  Kristen Lynn McCaleb ,  Wylie Solang Palmer

    IPC分类号： C07D471/04 ,  A61K31/519 ,  A61P35/00 ,  A61P19/00 ,  A61P29/00 ,  A61P37/08 ,  A61P3/10 ,  A61P25/28 ,  A61P25/16 ,  A61P35/02

    CPC分类号： C07D471/04

    摘要： This application discloses novel pyrimidinyl pyridone derivatives according to Formula I, wherein R1, R2, and R3 are defined as described herein, which inhibit JNK. The compounds disclosed herein are useful to modulate the activity of JNK and treat diseases associated with excessive JNK activity. The compounds are useful to treat autoimmune, inflammatory, metabolic, and neurological diseases as well as cancer. Also disclosed are compositions comprising the compound of Formula I and methods of treatment comprising administering a therapeutically effective amount of the compound of Formula I to a subject in need thereof.

    摘要翻译： 本申请公开了根据式I的新型嘧啶基吡啶酮衍生物，其中R1，R2和R3如本文所述限定，其抑制JNK。 本文公开的化合物可用于调节JNK的活性并治疗与过量JNK活性相关的疾病。 这些化合物可用于治疗自身免疫性，炎性，代谢和神经疾病以及癌症。 还公开了包含式I化合物和治疗方法的组合物，其包括向有需要的受试者施用治疗有效量的式I化合物。