1-[6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazol-5-yl]-2-methoxy ethanone | 606143-75-3

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 1-[6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazol-5-yl]-2-methoxy ethanone
• 英文别名: 1-[6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazol-5-yl]-2-methoxy-ethanone；1-[6-(4-bromo-2-chloroanilino)-7-fluoro-3H-benzimidazol-5-yl]-2-methoxyethanone
• CAS: 606143-75-3
• 化学式: C₁₆H₁₂BrClFN₃O₂
• 分子量: 412.646
• InChiKey: TYWZTXWVZYCZNW-UHFFFAOYSA-N

物化性质

• 沸点：
  556.7±50.0 °C(Predicted)
• 密度：
  1.664±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  24
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  67
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazole-5-carbaldehyde 、 methoxymethyllithium 生成 1-[6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazol-5-yl]-2-methoxy ethanone
  参考文献：
  名称：

  N3 alkylated benzimidazole derivatives as MEK inhibitors

  摘要：

  本发明涉及公式I的化合物及其药物可接受的盐和前药，其中W，R1，R2，R7，R8，R9和R10如规范中定义的那样。这些化合物是MEK抑制剂，对哺乳动物的高增殖性疾病，如癌症和炎症有用。本发明还公开了一种在哺乳动物的高增殖性疾病治疗中使用这些化合物的方法，以及含有这些化合物的制药组合物。

  公开号：

  US07425637B2

文献信息

• [EN] N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS<br/>[FR] DERIVES DE BENZIMIDAZOLE N3 ALKYLES UTILISES COMME INHIBITEURS DE MEK
  申请人：ARRAY BIOPHARMA INC

  公开号：WO2005023251A1

  公开（公告）日：2005-03-17

  Disclosed are compounds of the formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9, and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

  本发明揭示了公式I的化合物及其药学上可接受的盐和前药，其中W，R1，R2，R7，R8，R9和R10如规范中所定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物的高增殖性疾病，如癌症和炎症。本发明还揭示了使用这些化合物治疗哺乳动物的高增殖性疾病的方法，以及含有这些化合物的制药组合物。
• N3 alkylated benzimidazole derivatives as MEk inhibitors
  申请人：Wallace M. Eli

  公开号：US20050143438A1

  公开（公告）日：2005-06-30

  Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R 1 , R 2 , R 7 , R 8 , R 9 and R 10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

  本发明涉及公式I的化合物及其药学上可接受的盐和前药，其中W、R1、R2、R7、R8、R9和R10如规范中所定义。这些化合物是MEK抑制剂，对哺乳动物的高增殖性疾病，如癌症和炎症的治疗有用。本发明还涉及使用这些化合物治疗哺乳动物高增殖性疾病的方法，以及含有这些化合物的制药组合物。
• N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
  申请人：Wallace Eli M.

  公开号：US20080177082A1

  公开（公告）日：2008-07-24

  Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R 1 , R 2 , R 7 , R 8 , R 9 and R 10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.

  本发明涉及公式I的化合物及其药学上可接受的盐和前药，其中W，R1，R2，R7，R8，R9和R10如规范所定义。这些化合物是MEK抑制剂，在哺乳动物的治疗高增殖性疾病，如癌症和炎症中有用。本发明还涉及使用这些化合物治疗哺乳动物的高增殖性疾病的方法，以及含有这些化合物的药物组合物。
• COMPOSITIONS COMPRISING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS AND METHODS OF USE THEREOF
  申请人：Wallace Eli M.

  公开号：US20110158971A1

  公开（公告）日：2011-06-30

  Disclosed are pharmaceutical compositions comprising 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof. Also disclosed are methods of using such compositions for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals.

  本发明涉及一种制药组合物，包括6-(4-溴-2-氯苯氨基)-7-氟-3-甲基-3H-苯并咪唑-5-羧酸(2-羟基-乙氧基)-酰胺，或其药学上可接受的盐。本发明还涉及使用这种组合物的方法，用于抑制哺乳动物中的异常细胞生长或治疗增生性疾病。
• Method of treatment using N3 alkylated benzimidazole derivatives as MEK inhibitors
  申请人：Array Biopharma Inc.

  公开号：US08193229B2

  公开（公告）日：2012-06-05

  Disclosed are methods of treating a hyperproliferative disorder or a disease related to vasculogenesis or angiogenesis in a mammal, comprising administering to said mammal an effective amount of a compound of the formula or a pharmaceutically accepted salt thereof, wherein A, R1, R2, R7, R8, and R9 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals.

  本发明揭示了一种治疗哺乳动物的高增殖性疾病或与血管生成或血管新生有关的疾病的方法，包括向该哺乳动物内部给予公式化合物或其药学接受的盐的有效量，其中A，R1，R2，R7，R8和R9在说明书中定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物的高增殖性疾病，如癌症和炎症。