COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    3.
    发明公开
    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
    VERBINDUNGEN UND VERFAHREN ZUR激酶调节剂ANZEIGENDAFÜR

    公开(公告)号:EP2560972A4

    公开(公告)日:2013-11-20

    申请号:EP11772612

    申请日:2011-04-20

    申请人: PLEXXIKON INC

    CPC分类号: C07D487/04 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, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, including rheumatoid arthritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, global ischemia, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, and giant cell tumors.

    摘要翻译: 描述了其化合物和盐,其制剂,其结合物,其衍生物,其形式及其用途。 在某些方面和实施方案中,所述化合物或其盐,其制剂,其缀合物,其衍生物,其形式对Fms,Kit,Flt3,TrkA,TrkB和TrkC激酶蛋白中的一种或多种具有活性。 还描述了其用于治疗疾病和病症的方法,包括与Fms,Kit,Flt3,TrkA,TrkB和TrkC中的一种或多种相关的疾病和病症,包括类风湿性关节炎,骨关节炎,骨质疏松症,假体周围骨质溶解, 全身缺血,溃疡性结肠炎,克罗恩病,免疫性血小板减少性紫癜,动脉粥样硬化,系统性红斑狼疮,用于自体移植的骨髓移植,移植排斥反应,全身性硬化症,脱髓鞘病症,多发性硬化症,Charcot Marie Tooth综合征,肌萎缩性侧索硬化症,阿尔茨海默病 ,肾小球肾炎,间质性肾炎,狼疮肾炎,肾小管坏死,糖尿病性肾病,肾肥大,I型糖尿病,急性疼痛,炎性疼痛,神经性疼痛,急性骨髓性白血病,黑素瘤,多发性骨髓瘤,乳腺癌,前列腺癌,胰腺癌,肺 癌症,卵巢癌,神经胶质瘤,胶质母细胞瘤,神经瘤 溶血性骨转移,脑转移,胃肠道间质瘤和巨细胞肿瘤。

    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    5.
    发明公开
    COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
    VERBINDUNGEN UND VERFAHREN ZUR KINASE-MODULATION UND ANZEIGENDAFÜR

    公开(公告)号:EP2501236A4

    公开(公告)日:2013-05-15

    申请号:EP10832209

    申请日:2010-11-18

    申请人: PLEXXIKON INC

    IPC分类号: A01N43/90 A61K31/519

    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)的活性相关的疾病和病症 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。