6-(2-fluoropyridin-3-yl)-7H-purine | 1093101-56-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 6-(2-fluoropyridin-3-yl)-7H-purine
• CAS: 1093101-56-4
• 化学式: C₁₀H₆FN₅
• 分子量: 215.19
• InChiKey: IJIQMHLSDXEMFA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  67.4
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• NOVEL PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYL SULFONAMIDE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION WITH INHIBITORY ACTIVITY AGAINST RAF KINASE, CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：Youai Co., Ltd.

  公开号：EP2647637A2

  公开（公告）日：2013-10-09

  A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.

  本发明提供了一种新的嘌呤基吡啶基氨基-2,4-二氟苯磺酰胺衍生物、其药学上可接受的盐、其制备方法以及以其为活性成分的对 Raf 激酶具有抑制活性的药物组合物。本发明的嘌呤吡啶基氨基-2,4-二氟苯磺酰胺衍生物可有效调节B-Raf激酶的活性，因此可用于预防或治疗由Raf激酶过度激活诱发的癌症，特别是各种黑色素瘤、结直肠癌、前列腺癌、甲状腺癌、卵巢癌等。
• Pyridine derivative inhibiting RAF kinase and vascular endothelial growth factor receptor, method for preparing same, pharmaceutical composition containing same, and use thereof
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US10844062B2

  公开（公告）日：2020-11-24

  The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.

  本发明提供了一种新型吡啶衍生物、其药学上可接受的盐、制备方法以及含有其作为活性成分的药物组合物。 根据本发明的吡啶衍生物可抑制 RAf 激酶（B-RAf、RAf-1 或 B-RAfV600E）和参与血管生成的血管内皮生长因子受体（VEGFR2），因此可用于预防或治疗由 RAS 突变诱发的黑色素瘤、结直肠癌、前列腺癌、甲状腺癌、肺癌、胰腺癌、卵巢癌等。
• PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYL SULFONAMIDE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION WITH INHIBITORY ACTIVITY AGAINST RAF KINASE, CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：Medpacto Inc.

  公开号：EP2647637B1

  公开（公告）日：2016-02-03
• Pyridine Derivative Inhibiting RAF Kinase and Vascular Endothelial Growth Factor Receptor, Method for Preparing Same, Pharmaceutical Composition Containing Same, and Use Thereof
  申请人：SAMJIN PHARMACEUTICAL CO., LTD.

  公开号：US20190300531A1

  公开（公告）日：2019-10-03

  The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.
• US9216981B2
  申请人：——

  公开号：US9216981B2

  公开（公告）日：2015-12-22