7-(2-Fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylic acid cyclopropylmethoxy-amide | 1193487-54-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 7-(2-Fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylic acid cyclopropylmethoxy-amide
• 英文别名: 7-(2-Fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylicacid cyclopropylmethoxy-amide；N-(cyclopropylmethoxy)-7-(2-fluoro-4-iodoanilino)-5-oxo-2,3-dihydro-1H-indolizine-8-carboxamide
• CAS: 1193487-54-5
• 化学式: C₁₉H₁₉FIN₃O₃
• 分子量: 483.281
• InChiKey: ZRPBRAJUTBCJGK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  70.7
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  7-(2-fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylic acid 、 O-环丙基甲基羟胺盐酸盐 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 18.5h， 以25%的产率得到7-(2-Fluoro-4-iodo-phenylamino)-5-oxo-1,2,3,5-tetrahydro-indolizine-8-carboxylic acid cyclopropylmethoxy-amide
  参考文献：
  名称：

  Heterocyclic Compounds as MEK Inhibitors

  摘要：

  本发明涉及公式I的化合物和药用盐。这些化合物可以作为潜在的MEK抑制剂，用于治疗癌症和炎症等过度增殖性疾病。本发明还揭示了其制备方法。

  公开号：

  US20090275606A1

文献信息

• HETEROCYCLIC COMPOUNDS AS MEK INHIBITORS
  申请人：Novartis AG

  公开号：EP2421612A1

  公开（公告）日：2012-02-29
• METHOD OF REDUCING ADVERSE EFFECTS IN A CANCER PATIENT UNDREGOING TREATMENT WITH A MEK INHIBITOR
  申请人：THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERV

  公开号：US20150265679A1

  公开（公告）日：2015-09-24

  What is described is a method for treating an adverse side effect of MEK inhibitors by administering a pharmaceutical composition comprising IFNγ to a cancer patient being treated by a MEK-inhibitor. The applicants discovered that MEK inhibitors produce unwanted visual disturbances as an adverse side effect in a significant fraction of cancer patients being treated by the drug, and that the side effect causes retinal detachment due to fluid accumulation in the eye. The method treats the retinal detachment caused by the anticancer therapeutic by providing a means of decreasing the amount of fluid present in the retina and/or subretinal space of the eye by administering the pharmaceutical composition comprising IFNγ to the basolateral side of the retinal pigment epithelium, preferably by administering the pharmaceutical composition to the anterior surface of the eye in liquid droplets.
• [EN] HETEROCYCLIC COMPOUNDS AS MEK INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES COMME INHIBITEURS DE MEK
  申请人：NOVARTIS AG

  公开号：WO2010121646A1

  公开（公告）日：2010-10-28

  The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts. These compounds can act as potential MEK inhibitors in the treatment of hyperproliferative diseases, like cancer and inflammation. The present invention also reveals methods of preparation thereof.