8-fluoro-5-(2-fluoro-4-iodo-phenylamino)-imidazo[1,5-a]pyridine-6-carboxylic acid (2-hydroxy-ethoxy)-amide | 1168091-94-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 8-fluoro-5-(2-fluoro-4-iodo-phenylamino)-imidazo[1,5-a]pyridine-6-carboxylic acid (2-hydroxy-ethoxy)-amide
• 英文别名: 8-fluoro-5-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)imidazo[1,5-a]pyridine-6-carboxamide
• CAS: 1168091-94-8
• 化学式: C₁₆H₁₃F₂IN₄O₃
• 分子量: 474.206
• InChiKey: FGTGVNVJPGUWKH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 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：
  87.9
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  8-fluoro-5-(2-fluoro-4-iodo-phenylamino)-imidazo[1,5-a]pyridine-6-carboxylic acid (2-vinyloxy-ethoxy)-amide 在 甲醇 、 氨 、 resultant product 、 乙酸乙酯 、 碳酸氢钠 、 Brine 、 magnesium sulfate 作用下， 以 甲醇 为溶剂， 以to yield the title compound as a white solid (88 mg, 39%)的产率得到8-fluoro-5-(2-fluoro-4-iodo-phenylamino)-imidazo[1,5-a]pyridine-6-carboxylic acid (2-hydroxy-ethoxy)-amide
  参考文献：
  名称：

  5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE

  摘要：

  本发明涉及一种方法，用于抑制哺乳动物中的异常细胞生长或治疗增生性疾病，其包括向该哺乳动物施用具有抗增生活性的I型咪唑吡啶化合物的治疗有效量。

  公开号：

  US20110158990A1

文献信息

• [EN] 5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE<br/>[FR] 5-ANILINOIMIDAZOPYRIDINES ET PROCÉDÉS D'UTILISATION
  申请人：GENENTECH INC

  公开号：WO2009085983A1

  公开（公告）日：2009-07-09

  The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or 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/或抗炎活性的式I的咪唑吡啶化合物，更具体地涉及抑制MEK激酶活性的咪唑吡啶化合物。该发明提供了用于抑制异常细胞生长或治疗哺乳动物体内的增生性疾病或治疗炎症性疾病的组合物和方法。该发明还涉及使用这些化合物进行哺乳动物细胞的体外、体内和体内诊断或治疗，或相关病理条件的方法。
• 5-ANILINOIMIDAZOPYRIDINES AND METHODS OF USE
  申请人：Price Stephen

  公开号：US20100004269A1

  公开（公告）日：2010-01-07

  The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or 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.

  本发明涉及具有抗癌和/或抗炎活性的式I的咪唑吡啶，更具体地涉及抑制MEK激酶活性的咪唑吡啶。本发明提供了用于抑制异常细胞生长或治疗哺乳动物的增殖性疾病或治疗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、原位和体内诊断或治疗，或相关病理条件的方法。
• 5-anilinoimidazo[1,5-a]-pyridines inhibitors of MEK kinase
  申请人：Genentech, Inc.

  公开号：US07923456B2

  公开（公告）日：2011-04-12

  The invention relates to imidazopyridines of formula I with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or 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的咪唑吡啶化合物，其具有抗癌和/或抗炎活性，更具体地，涉及抑制MEK激酶活性的咪唑吡啶化合物。本发明提供了用于抑制异常细胞生长或治疗哺乳动物的增生性疾病或治疗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、体内诊断或治疗，或相关病理条件的方法。
• 5-Anilinoimidazopyridines and Methods of Use
  申请人：Genentech, Inc.

  公开号：EP2690101A1

  公开（公告）日：2014-01-29

  The invention relates to imidazopyridines of formula 1 with anti-cancer and/or anti-inflammatory activity and more specifically to imidazopyridines which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or 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.

  本发明涉及具有抗癌和/或抗炎活性的式 1 的咪唑吡啶，更具体地说，涉及抑制 MEK 激酶活性的咪唑吡啶。本发明提供了用于抑制异常细胞生长或治疗过度增殖性疾病或治疗哺乳动物炎症疾病的组合物和方法。本发明还涉及使用这些化合物体外、原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
• METHODS OF TREATING CANCER USING PD-1 AXIS BINDING ANTAGONISTS AND MEK INHIBITORS
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3563870A1

  公开（公告）日：2019-11-06

  The present invention describes combination treatment comprising a PD-1 axis binding antagonist and a MEK inhibitor and methods for use thereof, including methods of treating conditions where enhanced immunogenicity is desired such as increasing tumor immunogenicity for the treatment of cancer.

  本发明描述了由PD-1轴结合拮抗剂和MEK抑制剂组成的组合治疗及其使用方法，包括治疗需要增强免疫原性的病症的方法，如增加肿瘤免疫原性以治疗癌症。