N-(3,5-bis-trifluoromethyl-phenyl)-4-hydroxy-isophthalamide

• 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: N-(3,5-bis-trifluoromethyl-phenyl)-4-hydroxy-isophthalamide
• 英文别名: 1-N-[3,5-bis(trifluoromethyl)phenyl]-4-hydroxybenzene-1,3-dicarboxamide
• 化学式: C₁₆H₁₀F₆N₂O₃
• 分子量: 392.25
• InChiKey: MXKSZIWYDIPQAW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  27
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  N-(3,5-bis(trifluoromethyl)phenyl)-5-cyano-2-hydroxybenzamide 、 sodium hydroxide 、 双氧水 、 chloroform methanol 以 乙醇 、 二甲基亚砜 为溶剂， 反应 16.0h， 以to give 149 mg of the target compound (yield: 95%)的产率得到N-(3,5-bis-trifluoromethyl-phenyl)-4-hydroxy-isophthalamide
  参考文献：
  名称：

  2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient

  摘要：

  本发明涉及2-羟基芳酰胺衍生物或其药学上可接受的盐，其制备方法以及包含其作为活性成分的用于预防或治疗癌症的药物组合物。本发明制备的2-羟基芳酰胺衍生物在抑制TMPRSS4丝氨酸蛋白酶活性和抑制TMPRSS4表达的癌细胞浸润方面表现出色，因此可以作为一种用于通过抑制在癌细胞中过度表达的TMPRSS4来预防或治疗癌症的组合物，特别是结肠癌、肺癌、乳腺癌、前列腺癌、卵巢癌、胰腺癌或胃癌细胞。

  公开号：

  US09266872B2

文献信息

• 2-HYDROXYARYLAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CANCER CONTAINING SAME AS ACTIVE INGREDIENT
  申请人：Korea Research Institute of Bioscience and Biotechnology

  公开号：US20140221411A1

  公开（公告）日：2014-08-07

  The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.

  本发明涉及一种2-羟基芳酰胺衍生物或其药用可接受的盐，其制备方法，以及作为活性成分的预防或治疗癌症的药物组合物。本发明制备的2-羟基芳酰胺衍生物在抑制TMPRSS4丝氨酸蛋白酶的活性和抑制TMPRSS4表达的癌细胞浸润方面表现出色，因此可以作为一种通过抑制癌细胞中TMPRSS4过度表达的组合物，特别是结肠癌、肺癌、乳腺癌、前列腺癌、卵巢癌、胰腺癌或胃癌细胞的预防或治疗癌症的组合物。
• US9266872B2
  申请人：——

  公开号：US9266872B2

  公开（公告）日：2016-02-23
• 2-hydroxyarylamide derivative or pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition for preventing or treating cancer containing same as active ingredient
  申请人：KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY

  公开号：US09266872B2

  公开（公告）日：2016-02-23

  The present invention relates to a 2-hydroxyarylamide derivative or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition for preventing or treating cancer comprising the same as an active ingredient. The 2-hydroxyarylamide derivative prepared by the present invention is excellent in the inhibition of the activity of TMPRSS4 serine protease and the suppression of the infiltration of TMPRSS4-expressed cancer cells, and thus can be useful as a composition for preventing or treating cancer by inhibiting TMPRSS4 over-expressed in cancer cells, particularly, colorectal cancer, lung cancer, breast cancer, prostate cancer, ovarian cancer, pancreatic cancer, or stomach cancer cells.

  本发明涉及2-羟基芳酰胺衍生物或其药学上可接受的盐，其制备方法以及包含其作为活性成分的用于预防或治疗癌症的药物组合物。本发明制备的2-羟基芳酰胺衍生物在抑制TMPRSS4丝氨酸蛋白酶活性和抑制TMPRSS4表达的癌细胞浸润方面表现出色，因此可以作为一种用于通过抑制在癌细胞中过度表达的TMPRSS4来预防或治疗癌症的组合物，特别是结肠癌、肺癌、乳腺癌、前列腺癌、卵巢癌、胰腺癌或胃癌细胞。