首页> 外国专利> 1- (5-tert-Butyl-2-aryl-pyrazol-3-yl) -3- 2-fluoro-4- 3-oxo-4H-pyrido 2 as a RAF inhibitor for the treatment of cancer , 3-b pyrazin-8-yl) oxy phenyl urea derivatives

1- (5-tert-Butyl-2-aryl-pyrazol-3-yl) -3- 2-fluoro-4- 3-oxo-4H-pyrido 2 as a RAF inhibitor for the treatment of cancer , 3-b pyrazin-8-yl) oxy phenyl urea derivatives

机译:1-(5-叔丁基-2-芳基-吡唑-3-基)-3- [2-氟-4- [3-氧代-4H-吡啶基] [2]作为RAF抑制剂用于治疗癌症, 3-b]吡嗪-8-基)氧基]苯基]脲衍生物

摘要

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)- 3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as "TBAP compounds") that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of mutant BRAF; disorders ameliorated by the inhibition of BRAF and CRAF; disorders associated with RAS mutations and/or MAPK pathway activation; disorders ameliorated by the inhibition of SRC, p38, FGFRA, VEGFR-2 (KDR), and/or LCK; etc.
机译:本发明总体上涉及治疗化合物领域。更具体地,本发明涉及某些1-(5-叔丁基-2-芳基-吡唑-3-基)-3- [2-氟-4-[(3-氧代-4H-吡啶基[2,3] -b]吡嗪-8-基)氧基]苯基]脲化合物(本文称为“ TBAP化合物”),其尤其抑制RAF(例如BRAF,CRAF等)。本发明还涉及包含此类化合物的药物组合物,以及此类化​​合物和组合物在体外和体内在抑制RAF(例如BRAF,CRAF等)中的用途;并治疗疾病包括:增生性疾病;癌症(包括恶性黑色素瘤,大肠癌,胰腺腺癌);炎;免疫性疾病;病毒感染;纤维化疾病;与RAF突变形式相关的疾病(例如BRAF,CRAF等);通过抑制RAF改善的疾病(例如BRAF,CRAF等);通过抑制BRAF突变而改善的疾病;通过抑制BRAF和CRAF而改善的疾病;与RAS突变和/或MAPK途径激活有关的疾病;通过抑制SRC,p38,FGFRA,VEGFR-2(KDR)和/或LCK改善的疾病;等等

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