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    • 7. 发明申请
    • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    • 化合物及其调节方法及其适应症
    • WO2011063159A1
    • 2011-05-26
    • PCT/US2010/057293
    • 2010-11-18
    • PLEXXIKON, INC.IBRAHIM, Prabha, N.SPEVAK, WayneCHO, HannaSHI, SongyuanZHANG, ChaoZHANG, Ying
    • IBRAHIM, Prabha, N.SPEVAK, WayneCHO, HannaSHI, SongyuanZHANG, ChaoZHANG, Ying
    • A01N43/90A61K31/519
    • C07D487/04A61K31/437A61K31/519A61K31/5377C07D401/04C07D403/04C07D471/04
    • 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 at least one Raf 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 diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.
    • 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,其形式在至少一种Raf蛋白激酶上具有活性。 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,包括与B-Raf V600E突变蛋白激酶(包括黑素瘤,神经胶质瘤,多形性成胶质细胞瘤,纤维细胞性星形细胞瘤,结肠直肠癌,甲状腺癌,肺癌,卵巢)的活动相关的疾病和病症 癌症,前列腺癌,肝癌,胆囊癌,胃肠道间质瘤,胆道癌和胆管癌。 还描述了其用于治疗疾病和病症的方法,包括与c-Raf-1蛋白激酶的活性相关的疾病和病症,包括急性疼痛,慢性疼痛或多囊肾病。