Compounds and methods for kinase modulation, and indications therefor
    1.
    发明授权
    Compounds and methods for kinase modulation, and indications therefor 有权
    用于激酶调节的化合物和方法及其适应症

    公开(公告)号:US08673928B2

    公开(公告)日:2014-03-18

    申请号:US12949741

    申请日:2010-11-18

    摘要: and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds of Formula (I) 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.

    摘要翻译: 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,所述式(I)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。

    Compounds and methods for kinase modulation, and indications therefor
    4.
    发明授权
    Compounds and methods for kinase modulation, and indications therefor 有权
    用于激酶调节的化合物和方法及其适应症

    公开(公告)号:US08198273B2

    公开(公告)日:2012-06-12

    申请号:US12773798

    申请日:2010-05-04

    CPC分类号: C07D471/04

    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, and forms thereof are active on each of BRaf and c-Raf-1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.

    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,所描述的化合物或其盐,其制剂,其缀合物,其衍生物及其形式在BRaf和c-Raf-1蛋白激酶中的每一个上都是有活性的,并且还可以在 A-Raf和B-Raf V600E蛋白激酶。 还描述了其用于治疗疾病和病症的方法,包括黑素瘤,结肠直肠癌,甲状腺癌,卵巢癌和胆道癌。

    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    5.
    发明申请
    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
    化合物及其调节方法及其适应症

    公开(公告)号:US20090286783A1

    公开(公告)日:2009-11-19

    申请号:US12467208

    申请日:2009-05-15

    CPC分类号: C07D487/04

    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 at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, pain or polycystic kidney disease.

    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,其衍生物,其衍生物,其形式在至少一种Raf蛋白激酶上具有活性。 还描述了其用于治疗疾病和病症的方法,包括与Raf蛋白激酶(包括黑素瘤,结肠直肠癌,甲状腺癌,卵巢癌,胆管癌,疼痛或多囊肾病)的活动相关的疾病和病症。