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    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
    1.
    发明申请
    SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3, 4-B] PYRIDINE AND PYRAZOLO [3, 4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-B]吡啶和吡唑并[3,4-B]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US20160074395A1

    公开(公告)日：2016-03-17

    申请号：US14871285

    申请日：2015-09-30

    申请人： Arrien Pharmaceuticals LLC

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： A61K31/497 ,  A61K31/5377

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3, 4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。

    Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
    3.
    发明授权
    Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3, 4-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors 有权
    取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶和吡唑并[3,4-b]吡啶衍生物作为蛋白激酶抑制剂

    公开(公告)号：US09187473B2

    公开(公告)日：2015-11-17

    申请号：US14290125

    申请日：2014-05-29

    申请人： Arrien Pharmaceuticals LLC

    发明人： Hariprasad Vankayalapati ,  Rajendra P. Appalaneni ,  Y. Venkata Krishna Reddy

    IPC分类号： C07D401/14 ,  A61K31/437 ,  C07D471/04

    CPC分类号： A61K31/497 ,  A61K31/5377 ,  C07C249/00 ,  C07D471/04

    摘要： Substituted 5-(pyrazin-2-yl)-1H-pyrazolo[3,4-b]pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo[3,4-b]pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson's disease, Alzheimer's disease, Down's Syndrome, Huntington's disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated therewith using compounds and pharmaceutical compositions including the compounds.

    摘要翻译： 取代5-（吡嗪-2-基）-1H-吡唑并[3,4-b]吡啶，5-（吡嗪-2-基）-1H-吡咯并[2,3-b]吡啶和吡唑并[3,4 -b]吡啶衍生物及其制备方法，其为组成型激活酪氨酸激酶（TKL），CMGC蛋白激酶家族成员的抑制剂，可用于治疗帕金森病， 阿尔茨海默病，唐氏综合症，亨廷顿病，其他神经变性和中枢神经系统疾病，癌症，代谢紊乱和炎性疾病。 还公开了包括这些化合物的化合物和抑制这些家族的野生型和/或突变的蛋白激酶活性的方法的药物组合物，以及使用包括该化合物的化合物和药物组合物治疗与其相关的病症。

    ITK and JAK Kinase Inhibitors
    7.
    发明申请
    ITK and JAK Kinase Inhibitors 审中-公开
    ITK和JAK激酶抑制剂

    公开(公告)号：US20160046627A1

    公开(公告)日：2016-02-18

    申请号：US14924427

    申请日：2015-10-27

    申请人： Arrien Pharmaceuticals LLC

    发明人： Hariprasad Vankayalapati ,  Venkatakrishnareddy Yerramreddy ,  Paramareddy Gangireddy ,  Rajendra P. Appalaneni

    IPC分类号： C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention relates to compounds described by Formula I: salts thereof, their synthesis, and their use as ITK and JAK3 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and or disorders such disease associated with abnormal cell growth such as autoimmune, inflammation, rheumatoid arthritis, systemic lupus erythematosus, atherosclerosis, ulcerative colitis, psoriatic arthritis, psoriasis, Crohn's, metabolic and cancer diseases. The present invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions and processes for preparing the compounds of the invention.

    摘要翻译： 本发明涉及式I所述的化合物：其盐，它们的合成及其作为包括这些化合物的ITK和JAK3抑制剂的用途以及使用所述化合物治疗各种疾病和/或障碍的方法，所述疾病与异常细胞生长相关 例如自身免疫，炎症，类风湿性关节炎，系统性红斑狼疮，动脉粥样硬化，溃疡性结肠炎，银屑病关节炎，牛皮癣，克罗恩病，代谢和癌症疾病。 本发明还提供包含本发明化合物的药学上可接受的组合物和使用组合物和制备本发明化合物的方法的方法。