6-(2-fluoro-4-iodo-phenylamino)-1-oxo-2,3-dihydro-1H-isoindole-5-carboxylic acid (2-hydroxy-ethoxy)-amide | 1203588-06-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-(2-fluoro-4-iodo-phenylamino)-1-oxo-2,3-dihydro-1H-isoindole-5-carboxylic acid (2-hydroxy-ethoxy)-amide
• 英文别名: 6-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1-oxo-2,3-dihydroisoindole-5-carboxamide
• CAS: 1203588-06-0
• 化学式: C₁₇H₁₅FIN₃O₄
• 分子量: 471.227
• InChiKey: DZRWYLSCZMVOSS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  26
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  99.7
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  6-(2-fluoro-4-iodo-phenylamino)-1-oxo-2,3-dihydro-1H-isoindole-5-carboxylic acid (2-vinyloxy-ethoxy)-amide 在 盐酸 作用下， 以 甲醇 、 水 为溶剂， 反应 0.5h， 以61%的产率得到6-(2-fluoro-4-iodo-phenylamino)-1-oxo-2,3-dihydro-1H-isoindole-5-carboxylic acid (2-hydroxy-ethoxy)-amide
  参考文献：
  名称：

  [EN] ISOINDOLONE DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE
  [FR] DÉRIVÉS D'ISOINDOLONE UTILISÉS EN TANT QU'INHIBITEURS DE KINASE MEK ET PROCÉDÉS D'UTILISATION CORRESPONDANTS

  摘要：

  公开号：

  WO2010003022A8

文献信息

• ISOINDOLONES DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE
  申请人：Gancia Emanuela

  公开号：US20110124622A1

  公开（公告）日：2011-05-26

  The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

  本发明涉及公式（I）的异吲哚酮，具有抗癌和/或抗炎活性，更具有MEK激酶抑制活性。本发明提供了用于抑制异常细胞生长，治疗增生性疾病或治疗哺乳动物炎症性疾病的组合物和方法。本发明还涉及使用该化合物进行哺乳动物细胞的体外，体内和原位诊断或治疗，或相关病理条件的方法。
• Isoindolones derivatives as MEK kinase inhibitors and methods of use
  申请人：Gancia Emanuela

  公开号：US08492427B2

  公开（公告）日：2013-07-23

  The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

  该发明涉及具有抗癌和/或抗炎活性的公式（I）的异吲哚酮，更具体地涉及MEK激酶抑制活性。该发明提供了用于抑制异常细胞生长、治疗增生性疾病或治疗哺乳动物的炎症性疾病的组合物和方法。该发明还涉及使用该化合物进行哺乳动物细胞的体外、体内诊断或治疗，或相关病理条件的方法。
• ISOINDOLONE DERIVATIVES AS MEK KINASE INHIBITORS AND METHODS OF USE
  申请人：Genentech, Inc.

  公开号：EP2307364B1

  公开（公告）日：2013-06-19
• 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.
• US8492427B2
  申请人：——

  公开号：US8492427B2

  公开（公告）日：2013-07-23