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    SUBSTITUTED AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES (IRAK-4)
    8.
    发明公开
    SUBSTITUTED AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES (IRAK-4) 审中-公开
    替代亚胺基二苯并噻唑酮（IRAK-4）

    公开(公告)号：EP3019171A4

    公开(公告)日：2017-01-25

    申请号：EP14823386

    申请日：2014-07-07

    申请人： MERCK SHARP & DOHME

    发明人： LIM JONGWON ,  ALTMAN MICHAEL D

    IPC分类号： A61K31/519 ,  A61K31/497 ,  A61K45/06 ,  A61P29/00 ,  C07D487/04

    CPC分类号： A61K31/519 ,  A61K45/06 ,  C07D487/04 ,  A61K2300/00

    摘要： This invention relates to amidopyrazole compounds that are inhibitors of Interieukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases. Speifically (5-methylpyridin-2-yl)-1 H-pyrazol-5-yl]pyrazolo[1,5-a]pyrimidine-3-carboxamide derivatives are disclosed for use in the method of treating inflammatory disorders such as rheumatoid arthritis, inflammatory bowel disease and cancer.

    摘要翻译： 本发明涉及作为白介素受体相关激酶抑制剂，特别是IRAK-4的氨基吡唑化合物，可用于治疗细胞增殖性疾病。 公开了用于治疗炎症性疾病如类风湿性关节炎的方法中使用的（5-甲基吡啶-2-基）-1H-吡唑-5-基]吡唑并[1,5-a]嘧啶-3-甲酰胺衍生物， 炎性肠病和癌症。

    NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    9.
    发明公开
    NOVEL COMPOUNDS THAT ARE ERK INHIBITORS 审中-公开
    新的连接作为ERK HEMMER

    公开(公告)号：EP2991654A4

    公开(公告)日：2016-12-14

    申请号：EP14791539

    申请日：2014-04-25

    申请人： MERCK SHARP & DOHME

    发明人： LIM JONGWON ,  HUANG XIANHAI ,  FERGUSON RONALD D ,  ZHOU WEI ,  BOYCE CHRISTOPHER W ,  SILIPHAIVANH PHIENG ,  WITTER DAVID J ,  MALETIC MILANA M ,  KOZLOWSKI JOSEPH A ,  WILSON KEVIN J

    IPC分类号： A61K31/655 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D519/00

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D471/14 ,  C07D519/00

    摘要： Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I).

    摘要翻译： 公开了式（I）的ERK抑制剂及其药学上可接受的盐。 还公开了使用式（I）化合物治疗癌症的方法。 本发明还提供了包含有效量的至少一种式（I）化合物和药学上可接受的载体的药物组合物。 本发明还提供一种药物组合物，其包含有效量的至少一种式（I）化合物和有效量的至少一种其它药物活性成分（例如化学治疗剂）和药学上可接受的载体 。 本发明还提供了在需要这种治疗的患者中抑制ERK的方法（即，抑制ERK2的活性），包括向所述患者施用有效量的至少一种式（I）的化合物。