6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide | 606143-88-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 6-(4-bromo-2-chloro-phenylamino)-7-fluoro-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide
• 英文别名: N-desmethylselumetinib；N-Desmethyl selumetinib；6-(4-bromo-2-chloroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3H-benzimidazole-5-carboxamide
• CAS: 606143-88-8
• 化学式: C₁₆H₁₃BrClFN₄O₃
• 分子量: 443.66
• InChiKey: UBEOBEUUUKHITB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  99.3
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• 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。
• Methods of Treating a Hyperproliferative Disorder or Inhibiting Cell Growth in a Mammal
  申请人：Wallace Eli M.

  公开号：US20120277277A1

  公开（公告）日：2012-11-01

  Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy.

  本发明公开了一种用于抑制哺乳动物中异常细胞生长或治疗增生性疾病的方法，包括向该哺乳动物投与一种药物组合物，该药物组合物包括6-(4-溴-2-氟苯基氨基)-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，与一种有效量的抗肿瘤剂或与放射治疗相结合。
• METHOD OF TREATMENT USING N3 ALKYLATED BENZIMIDAZOLE DERIVATIVES AS MEK INHIBITORS
  申请人：Wallace Eli M.

  公开号：US20100267793A1

  公开（公告）日：2010-10-21

  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, R 1 , R 2 , R 7 , R 8 , and R 9 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.

  本发明涉及一种治疗哺乳动物中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，包括向该哺乳动物施用一种公式的化合物或其药学上接受的盐的有效量，其中A，R1，R2，R7，R8和R9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中的高增殖性疾病，例如癌症和炎症。
• N3 alkylated benzimidazole derivatives as mek inhibitors
  申请人：Array Biopharma, Inc.

  公开号：EP2130536A1

  公开（公告）日：2009-12-09

  Disclosed are compounds of the formula I and pharmaceutically acceptable salts 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.

  公开了式 I 的化合物 及其药学上可接受的盐类、 其中 W、R1、R2、R7、R8、R9 和 R10 如说明书中所定义。 此类化合物是 MEK 抑制剂，可用于治疗哺乳动物的过度增殖性疾病，如癌症和炎症。