4-(2,4-Dichlorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (2-hydroxyethoxy)-amide | 853107-19-4

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 4-(2,4-Dichlorophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (2-hydroxyethoxy)-amide
• 英文别名: 4-(2,4-dichloroanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide
• CAS: 853107-19-4
• 化学式: C₁₆H₁₇Cl₂N₃O₄
• 分子量: 386.235
• InChiKey: XTRCRDNRVUEOTF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  25
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  90.9
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• HETEROCYCLIC INHIBITORS OF MEK AND METHODS OF USE THEREOF
  申请人：Marlow Allison L.

  公开号：US20090215834A1

  公开（公告）日：2009-08-27

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

  本发明涉及公式V的化合物，以及其药学上可接受的盐和前药，其中R1、R2、R7、R8和R9以及W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，以及炎症状况。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和炎症状况的方法，以及含有这些化合物的制药组合物。
• Heterocyclic inhibitors of MEK and methods of use thereof
  申请人：Marlow L. Allison

  公开号：US20070112038A1

  公开（公告）日：2007-05-17

  Disclosed are compounds of the Formulas I and V and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X and Y 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, and inflammatory conditions. Also disclosed are methods 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和公式V的化合物及其药学上可接受的盐和前药，其中R1、R2、R7、R8和R9、W、X和Y在规范中定义。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，以及炎症病状。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和包含这些化合物的制药组合物。
• Novel 4-Arylamino Pyridone Derivatives as Mek Inhibitors for the Treatment of Hyper-Proliferative Disorders
  申请人：Abel Ulrich

  公开号：US20070293544A1

  公开（公告）日：2007-12-20

  The invention provides novel, substituted 4-arylamino pyridone compounds (formula (I)), pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R 1, R2, R9, R 10, R 11, R 12, R 13, R 14 and L are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.

  本发明提供了一种新型的取代的4-芳基氨基吡啶酮化合物（式（I）），其药学上可接受的盐、溶剂化物和前药化合物，其中W、R1、R2、R9、R10、R11、R12、R13、R14和L如规范中所定义。这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症、再狭窄和炎症。还揭示了在哺乳动物，特别是人类中使用这些化合物治疗过度增殖性疾病以及含有这些化合物的制药组合物的用途。
• Heterocyclic Inhibitors of MEK and Methods of Use Thereof
  申请人：Marlow Allison L.

  公开号：US20110288092A1

  公开（公告）日：2011-11-24

  Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 7 , R 8 , R 9 and W are as defined in the specification.

  本发明涉及治疗增殖过度性疾病的方法、治疗炎症性疾病的方法以及抑制哺乳动物中MEK活性的方法，其中包括向哺乳动物中给予一种或多种Formula Vor化合物或其药学上可接受的盐的有效量，其中R1、R2、R7、R8、R9和W如规范中所定义。
• Combinations Comprising Heterocyclic Inhibitors of MEK and Methods of Use Thereof
  申请人：Marlow Allison L.

  公开号：US20120263679A1

  公开（公告）日：2012-10-18

  Disclosed are combinations comprising (a) a compound of the Formula: wherein R 1 , R 2 , R 7 , R 8 , R 9 and W are as defined in the specification, and (b) at least one additional therapeutic agent. Such combinations are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, and inflammatory conditions in mammals. Also disclosed are methods of using such combinations in the treatment of hyperproliferative diseases and inflammatory conditions in mammals.

  本发明涉及一种组合物，包括（a）式中的化合物，其中R1、R2、R7、R8、R9和W如规范中定义，以及（b）至少一种额外的治疗剂。这种组合物对于治疗哺乳动物的高增殖性疾病，如癌症和炎症，以及炎症状况非常有用。本发明还涉及使用这种组合物治疗哺乳动物的高增殖性疾病和炎症状况的方法。