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    PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
    2.
    发明申请
    PYRAZOLOPYRIMIDINE DERIVATIVES AS TYROSINE KINASE INHIBITORS 有权
    作为酪氨酸激酶抑制剂的吡唑并嘧啶衍生物

    公开(公告)号：US20140221398A1

    公开(公告)日：2014-08-07

    申请号：US14117927

    申请日：2012-05-16

    Applicant: David Michael Goldstein ,  Kenneth Albert Brameld

    Inventor： David Michael Goldstein ,  Kenneth Albert Brameld

    IPC: C07D487/04

    CPC classification number: C07D487/04

    Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, Jak3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.

    Abstract translation: 本公开提供了酪氨酸激酶抑制剂，特别是BLK，BMX，EGFR，HER2，HER4，ITK，Jak3，TEC，Btk和TXK的化合物和药学上可接受的盐，因此可用于治疗可通过抑制 酪氨酸激酶如癌症和炎性疾病如关节炎等。 还提供了含有这些化合物的药物组合物和药学上可接受的盐以及制备这些化合物和药学上可接受的盐的方法。

    Dihydroquinone and dihydronaphthridine inhibitors of JNK
    9.
    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

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

    Inventor： 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: C07D471/04

    CPC classification number: C07D215/48 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/04 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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。

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