(4-{2-[(4-chlorophenyl)amino]-1-methylbenzimidazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide | 611213-73-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (4-{2-[(4-chlorophenyl)amino]-1-methylbenzimidazol-5-yloxy}-(2-pyridyl))-N-methylcarboxamide
• 英文别名: 4-[2-(4-chloroanilino)-1-methylbenzimidazol-5-yl]oxy-N-methylpyridine-2-carboxamide
• CAS: 611213-73-1
• 化学式: C₂₁H₁₈ClN₅O₂
• 分子量: 407.859
• InChiKey: BXZSTRBGJIHORE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  81.1
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• Substituted benz-azoles and methods of their use as inhibitors of Raf kinase
  申请人：Amiri Payman

  公开号：US20070299039A1

  公开（公告）日：2007-12-27

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  提供了新的取代苯唑化合物、组合物和抑制人或动物体内Raf激酶活性的方法。这些新化合物组合物可以单独使用，也可以与至少一种额外的药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。
• SUBSTITUTED BENZ-AZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
  申请人：Amiri Payman

  公开号：US20100196368A1

  公开（公告）日：2010-08-05

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  本发明提供了新的取代苯并唑化合物、组合物和抑制人类或动物主体中Raf激酶活性的方法。新的化合物组成物可以单独使用或与至少一种其他药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。
• SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE
  申请人：Amiri Payman

  公开号：US20120288501A1

  公开（公告）日：2012-11-15

  New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

  提供了新的取代苯唑化合物、组合物和抑制人类或动物主体中Raf激酶活性的方法。这些新的化合物组合物可以单独使用或与至少一种额外的药物联合使用，用于治疗Raf激酶介导的疾病，如癌症。
• Cancer treatment using combinations of ERK and RAF inhibitors
  申请人：BIOMED VALLEY DISCOVERIES, INC.

  公开号：US10668055B2

  公开（公告）日：2020-06-02

  The present invention provides, inter alia, methods of treating or ameliorating the effects of a cancer in a subject. The methods include administering to the subject an effective amount of (i) a first anti-cancer agent, which is BVD-523 or a pharmaceutically acceptable salt thereof and (ii) a second anti-cancer agent, which is a type 1 RAF inhibitor (such as dabrafenib) or another RAF inhibitor (such as regorafenib) or a pharmaceutically acceptable salt thereof, to treat or ameliorate the effects of the cancer. Also provided are pharmaceutical compositions and kits for treating or ameliorating the effects of a cancer in a subject.

  本发明特别提供了治疗或改善受试者癌症影响的方法。这些方法包括向受试者施用有效量的(i)第一种抗癌剂，即BVD-523或其药学上可接受的盐和(ii)第二种抗癌剂，即1型RAF抑制剂（如达拉菲尼）或另一种RAF抑制剂（如瑞戈非尼）或其药学上可接受的盐，以治疗或改善癌症的影响。还提供了用于治疗或改善受试者癌症影响的药物组合物和试剂盒。
• SUBSTITUTED BENZAZOLES AND USE THEREOF AS RAF KINASE INHIBITORS
  申请人：Novartis Vaccines and Diagnostics, Inc.

  公开号：EP1499311B1

  公开（公告）日：2009-11-04