1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide | 1246442-86-3

• 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: 1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide
• 英文别名: 1-(2,3-dihydroxypropyl)-N-[2-(2-fluoro-4-iodoanilino)-1,5-dimethyl-6-oxopyridin-3-yl]cyclopropane-1-sulfonamide
• CAS: 1246442-86-3
• 化学式: C₁₉H₂₃FIN₃O₅S
• 分子量: 551.378
• InChiKey: WVSQVXBSOUSZRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  30
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  127
• 氢给体数：
  4
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide 生成 1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide 、 1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide
  参考文献：
  名称：

  [EN] DIHYDROPYRIDIN SULFONAMIDES AND DIHYDROPYRIDIN SULFAMIDES AS MEK INHIBITORS
  [FR] DIHYDROPYRIDINE-SULFONAMIDES ET DIHYDROPYRIDINE-SULFAMIDES EN TANT QU'INHIBITEURS DE MEK

  摘要：

  本发明涉及N-(邻苯氨基二氢吡啶基)磺酰胺和N-(邻苯氨基二氢吡啶基)N'-烷基磺酰胺，它们是MEK抑制剂，可用于治疗癌症和其他过度增殖性疾病。

  公开号：

  WO2010108652A1
• 作为产物：
  描述：

  tert-butyl 1-(2,3-dihydroxypropyl)cyclopropylsulfonyl(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)carbamate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 以66%的产率得到1-(2,3-dihydroxypropyl)-N-(2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-1,6-dihydropyridin-3-yl)cyclopropane-1-sulfonamide
  参考文献：
  名称：

  [EN] NOVEL 6-ARYLAMINO PYRIDONE SULFONAMIDES AND 6-ARYLAMINO PYRAZINONE SULFONAMDIES AS MEK INHIBITORS
  [FR] NOUVEAUX SULFONAMIDES DE 6-ARYLAMINO-PYRIDONE ET SULFONAMIDES DE 6-ARYLAMINO-PYRAZINONE SERVANT D'INHIBITEURS DE MEK

  摘要：

  公开号：

  WO2010145197A8

文献信息

• DIHYDROPYRIDIN SULFONAMIDES AND DIHYDROPYRIDIN SULFAMIDES AS MEK INHIBITORS
  申请人：Vernier Jean-Michel

  公开号：US20120107307A1

  公开（公告）日：2012-05-03

  This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N′-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.

  该发明涉及N-(邻苯氨基二氢吡啶基)磺酰胺和N-(邻苯氨基二氢吡啶基)、N'-烷基磺酰胺，它们是MEK抑制剂，可用于治疗癌症和其他过度增殖性疾病。
• 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.
• US8673919B2
  申请人：——

  公开号：US8673919B2

  公开（公告）日：2014-03-18