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    CHEMICAL COMPOUNDS
    1.
    发明申请
    CHEMICAL COMPOUNDS 审中-公开
    化学化合物

    公开(公告)号：US20120077828A1

    公开(公告)日：2012-03-29

    申请号：US13069569

    申请日：2011-03-23

    申请人： Jeffrey Michael Axten ,  Seth Wilson Grant ,  Dirk A. Heerding ,  Jesus Raul Medina ,  Stuart Paul Romeril ,  Jun Tang

    发明人： Jeffrey Michael Axten ,  Seth Wilson Grant ,  Dirk A. Heerding ,  Jesus Raul Medina ,  Stuart Paul Romeril ,  Jun Tang

    IPC分类号： A61K31/519 ,  A61P35/00 ,  A61P25/28 ,  A61P25/00 ,  A61P3/10 ,  A61P25/16 ,  A61P25/14 ,  A61P9/10 ,  A61P9/00 ,  A61P9/06 ,  A61P27/02 ,  A61P35/04 ,  A61P35/02 ,  A61P27/10 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/405 ,  A61K45/06 ,  C07D403/04 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

    摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein.The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    摘要翻译： 本发明涉及取代的二氢吲哚衍生物。 具体地，本发明涉及式I化合物：其中R1，R2和R3如本文所定义。 本发明的化合物是PERK的抑制剂，可用于治疗癌症，眼部疾病和与活化的未折叠蛋白反应途径相关的疾病，例如阿尔茨海默氏病，中风，1型糖尿病帕金森病，亨廷顿舞蹈病，肌萎缩性侧索 硬化症，心肌梗死，心血管疾病，动脉粥样硬化和心律失常，更具体地说是乳腺癌，结肠癌，胰腺癌和肺癌。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。

    Chemical compounds
    2.
    发明授权
    Chemical compounds 有权
    化合物

    公开(公告)号：US08598156B2

    公开(公告)日：2013-12-03

    申请号：US13637127

    申请日：2011-03-23

    申请人： Jeffrey Michael Axten ,  Seth Wilson Grant ,  Dirk A. Heerding ,  Jesus Rual Medina ,  Stuart Paul Romeril ,  Jun Tang

    发明人： Jeffrey Michael Axten ,  Seth Wilson Grant ,  Dirk A. Heerding ,  Jesus Rual Medina ,  Stuart Paul Romeril ,  Jun Tang

    IPC分类号： A01N43/62 ,  A61K31/55

    CPC分类号： C07D487/04 ,  A61K31/405 ,  A61K45/06 ,  C07D403/04 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

    摘要： The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

    摘要翻译： 本发明涉及取代的二氢吲哚衍生物。 具体地，本发明涉及式I化合物：其中R1，R2和R3如本文所定义。 本发明的化合物是PERK的抑制剂，可用于治疗癌症，眼部疾病和与活化的未折叠蛋白反应途径相关的疾病，例如阿尔茨海默氏病，中风，1型糖尿病帕金森病，亨廷顿舞蹈病，肌萎缩性侧索 硬化症，心肌梗死，心血管疾病，动脉粥样硬化和心律失常，更具体地说是乳腺癌，结肠癌，胰腺癌和肺癌。 因此，本发明进一步涉及包含本发明化合物的药物组合物。 本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制PERK活性和与之相关疾病的治疗方法。