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 relates generally to the field of therapeutic compounds. More specifically, the present invention provides, inter alia, certain 1- (5-tert-butyl-2-aryl-pyrazol-3-yl) -3- [2 which inhibit RAF (eg, BRAF, CRAF, etc.). -Fluoro-4- [3-oxo-4H-pyrido [2,3-b] pyrazin-8-yl) oxy] phenyl] urea compounds (referred to herein as “TBAP compounds”). The invention also inhibits pharmaceutical compositions comprising such compounds, as well as RAF (eg, BRAF, CRAF, etc.); and the following disorders: proliferative disorders; cancer (eg, malignant melanoma, colon cancer, Pancreatic adenocarcinoma, etc.); inflammation; immune disorders; viral infections; fibrotic diseases; disorders associated with mutant forms of RAF (eg, BRAF, CRAF, etc.); Disorders ameliorated by inhibition of mutant BRAF; disorders ameliorated by inhibition of BRAF and CRAF; disorders associated with RAS mutation and / or MAPK pathway activation; SRC, p38, FGFRA, VEGFR- 2 (KDR) and / or in vitro and in vivo for treating disorders ameliorated by inhibition of LCK Also it relates to the use of both these compounds and compositions in. [Chemical 1]
机译:本发明总体上涉及治疗化合物领域。更具体地,本发明尤其提供了某些抑制RAF的1-(5-叔丁基-2-芳基-吡唑-3-基)-3- [2](例如BRAF,CRAF等)。 -氟-4- [3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基)氧基]苯基]脲化合物(在本文中称为“ TBAP化合物”)。本发明还抑制了包含此类化合物以及RAF(例如BRAF,CRAF等)的药物组合物;以及以下疾病:增生性疾病;癌症(例如,恶性黑色素瘤,结肠癌,胰腺腺癌等);炎;免疫疾病;病毒感染;纤维化疾病;与RAF的突变形式有关的疾病(例如BRAF,CRAF等);通过抑制突变型BRAF改善了疾病;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; SRC,p38,FGFRA,VEGFR-2(KDR)和/或在体内和体外用于治疗通过抑制LCK改善的疾病。它还涉及这些化合物和组合物在其中的用途。[化学1]

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