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发明授权
CN105793260B 作为用于治疗癌症的RAF抑制剂的1-(5-叔丁基-2-芳基-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4H-吡啶并[2，3-B]吡嗪-8-基)氧基]苯基]脲衍生物 有权

作为用于治疗癌症的RAF抑制剂的1-(5-叔丁基-2-芳基-吡唑-3-基)-3-[2-氟-4-[(3-氧代-4H-吡啶并[2，3-B]吡嗪-8-基)氧基]苯基]脲衍生物
摘要：
本发明总体上涉及治疗化合物的领域。更确切地说，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‑吡啶并[2,3‑B]吡嗪‑8‑基)氧基]苯基]脲化合物(在此称为“TBAP化合物”)，所述化合物尤其抑制RAF(例如BRAF、CRAF等)。本发明还涉及包括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与在体内两者均抑制RAF(例如BRAF、CRAF等)、以及治疗包括以下各项的病症的用途：增殖性病症；癌症(包括例如恶性黑色素瘤、结直肠癌、胰腺癌)；炎症；免疫病症；病毒性感染；纤维化病症；与RAF(例如BRAF、CRAF等)的突变形式相关的病症；通过抑制RAF(例如BRAF、CRAF等)而改善的病症；通过抑制突变体BRAF而改善的病症；通过抑制BRAF和CRAF而改善的病症；与RAS突变和/或MAPK途径活化相关的病症；通过抑制SRC、p38、FGFRA、VEGFR‑2(KDR)、和/或LCK而改善的病症；等等。
摘要（英）：

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.

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