3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-5-hydroxyaminomethyl-N-(2-hydroxy-ethoxy)-benzamide | 874100-61-5

• 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: 3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-5-hydroxyaminomethyl-N-(2-hydroxy-ethoxy)-benzamide
• 英文别名: 3,4-difluoro-2-(2-fluoro-4-iodoanilino)-5-[(hydroxyamino)methyl]-N-(2-hydroxyethoxy)benzamide
• CAS: 874100-61-5
• 化学式: C₁₆H₁₅F₃IN₃O₄
• 分子量: 497.213
• InChiKey: PSTWTOLKKIGGNK-UHFFFAOYSA-N

物化性质

• 密度：
  1.817±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  103
• 氢给体数：
  5
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  (E)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-(hydroxyimino-methyl)-benzamide 、 二氯乙酸 以to give 3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-5-hydroxyaminomethyl-N-(2-hydroxy-ethoxy)-benzamide (28.14 mg, 81%)的产率得到3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-5-hydroxyaminomethyl-N-(2-hydroxy-ethoxy)-benzamide
  参考文献：
  名称：

  5-Substituted-2-Phenylamino Benzamides as Mek Inhibitors

  摘要：

  本发明的目标是提供具有强MEK抑制活性、在体内稳定且可溶于水的化合物，这些化合物可用作增生性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由以下公式(1)表示：[其中R1、R2、R3、R4和X的定义与本专利申请中定义的相同]。

  公开号：

  US20100197676A1

文献信息

• 5-Substituted-2-Phenylamino Benzamides as MEK Inhibitors
  申请人：Isshiki Yoshiaki

  公开号：US20090233915A1

  公开（公告）日：2009-09-17

  An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R 1 , R 2 , R 3 , R 4 , and X are the same as defined in the present patent application].

  本发明的目标是提供一种具有强烈MEK抑制活性、在体内稳定且可溶于水的化合物，可用作增生性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由以下公式（1）表示：[其中，R1、R2、R3、R4和X的定义与本专利申请中定义的相同]。
• 5-Substituted-2-phenylamino benzamides as MEK inhibitors
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：US07745663B2

  公开（公告）日：2010-06-29

  An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

  本发明的目标是提供一种表现出强烈的MEK抑制活性并在体内稳定且可溶于水的化合物，可用作增生性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由以下公式(1)表示：[其中R1、R2、R3、R4和X的定义与本专利申请中定义的相同]。
• 5-substituted-2-phenylamino benzamides as MEK inhibitors
  申请人：Isshiki Yoshiaki

  公开号：US08575391B2

  公开（公告）日：2013-11-05

  An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

  本发明的目标是提供具有强MEK抑制活性、在体内稳定且可溶于水的化合物，可作为增生性疾病的预防或治疗剂。本发明的化合物及其药学上可接受的盐由以下式子（1）表示：[其中R1、R2、R3、R4和X的定义与本专利申请中的定义相同]。
• 5-SUBSTITUTED-2-PHENYLAMINO-BENZAMIDE AS MEK INHIBITOR
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1780197A1

  公开（公告）日：2007-05-02

  An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].

  本发明的目的是提供具有强 MEK 抑制活性、在体内稳定且可溶于水的化合物，这些化合物可用作增殖性疾病的预防或治疗剂。 本发明的化合物及其药学上可接受的盐由下式（1）表示： [其中 R1、R2、R3、R4 和 X 与本专利申请中所定义的相同]。
• 5-SUBSTITUTED-2-PHENYLAMINO BENZAMIDES AS MEK INHIBITORS
  申请人：CHUGAI SEIYAKU KABUSHIKI KAISHA

  公开号：EP1780197B1

  公开（公告）日：2010-10-20