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    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    8.
    发明申请
    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
    化合物及其调节方法及其适应症

    公开(公告)号：US20110183988A1

    公开(公告)日：2011-07-28

    申请号：US12975239

    申请日：2010-12-21

    申请人： Prabha N. Ibrahim ,  Guoxian Wu ,  Jack Lin ,  Wayne Spevak ,  Hanna Cho ,  Todd Ewing ,  Chao Zhang

    发明人： Prabha N. Ibrahim ,  Guoxian Wu ,  Jack Lin ,  Wayne Spevak ,  Hanna Cho ,  Todd Ewing ,  Chao Zhang

    IPC分类号： A61K31/498 ,  C07D471/04 ,  A61K31/437 ,  A61K31/506 ,  A61K31/513 ,  A61K31/497 ,  A61P35/00

    CPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/497 ,  A61K31/498 ,  A61K31/506 ,  A61K31/519 ,  C07D519/00

    摘要： Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma.

    摘要翻译： 其化合物及其盐，其制剂，其缀合物，其衍生物，其形式及用途。 在某些方面和实施方案中，所述的化合物或其盐，其制剂，其缀合物，其衍生物，其形式在B-Raf，B-Raf V600E和c-Raf-1蛋白激酶中的每一个上都是活性的。 在某些方面和实施方案中，所述化合物在抑制Ras突变细胞系的增殖中是有活性的。 还描述了其用于治疗疾病和病症的方法，包括黑素瘤，神经胶质瘤，成胶质细胞瘤，纤维细胞性星形细胞瘤，肝癌，胆道癌，胆管癌，结肠直肠癌，肺癌，膀胱癌，胆囊癌，乳腺癌，胰腺癌， 甲状腺癌，肾癌，卵巢癌，肾上腺皮质癌，前列腺癌，胃肠道间质瘤，甲状腺髓样癌，肿瘤血管生成，急性骨髓性白血病，慢性骨髓单核细胞白血病，儿童急性淋巴细胞性白血病，浆细胞白血病和多发性骨髓瘤。