3-(2-fluoro-5-trifluoromethylphenyl)-5-(3-phenylpropionylamino)-4-(4-pyridyl)isoxazole | 1000188-25-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(2-fluoro-5-trifluoromethylphenyl)-5-(3-phenylpropionylamino)-4-(4-pyridyl)isoxazole
• 英文别名: N-[3-[2-fluoro-5-(trifluoromethyl)phenyl]-4-pyridin-4-yl-1,2-oxazol-5-yl]-3-phenylpropanamide
• CAS: 1000188-25-9
• 化学式: C₂₄H₁₇F₄N₃O₂
• 分子量: 455.411
• InChiKey: QXSMXFJEADZREG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  68
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• Pyridylisoxazole Derivatives
  申请人：Hasumi Koichi

  公开号：US20090306145A1

  公开（公告）日：2009-12-10

  This invention offers isoxazole derivatives represented by the following formula (I) in which R 1 and R 2 each stands for hydrogen, lower alkyl, amino and the like; R 3 stands for substituted or unsubstituted aryl or hetero aryl; R 4 stands for hydrogen or lower alkyl; R 5 stands for substituted or unsubstituted phenyl, furyl and the like; and Y stands for —CH 2 —, —CO—, —O—, —NH— and the like, or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.

  该发明提供了以下式（I）所表示的异唑啉衍生物，其中R1和R2分别代表氢，低碳基，氨基等; R3代表取代或未取代的芳基或杂环芳基; R4代表氢或低碳基; R5代表取代或未取代的苯基，呋喃基等; Y代表-CH2-，-CO-，-O-，-NH-等，或其药学上可接受的盐，具有出色的p38MAPkinase抑制作用，副作用减少，并且用于治疗慢性类风湿性关节炎，溃疡性结肠炎等疾病。
• PYRIDYLISOXAZOLE DERIVATIVE
  申请人：ASKA Pharmaceutical Co., Ltd.

  公开号：EP2036905A1

  公开（公告）日：2009-03-18

  This invention offers isoxazole derivatives represented by the following formula (I) in which R1 and R2 each stands for hydrogen, lower alkyl, amino and the like; R3 stands for substituted or unsubstituted aryl or hetero aryl; R4 stands for hydrogen or lower alkyl; R5 stands for substituted or unsubstituted phenyl, furyl and the like; and Y stands for -CH2-, -CO-, -O-, -NH- and the like, or pharmaceutically acceptable salts thereof which exhibit excellent p38MAPkinase-inhibiting action with reduced side-effects, and are useful for treating such diseases as chronic rheumatoid arthritis, ulcerative colitis and the like.

  本发明提供了由下式（I）表示的异噁唑衍生物 其中 R1 和 R2 分别代表氢、低级烷基、氨基等；R3 代表取代或未取代的芳基或杂芳基；R4 代表氢或低级烷基；R5 代表取代或未取代的苯基、呋喃基等；Y 代表-CH2-、-CO-、-O-、-NH-等、 或其药学上可接受的盐类，它们具有优异的 p38MAPkinase 抑制作用，且副作用较小，可用于治疗慢性类风湿性关节炎、溃疡性结肠炎等疾病。
• US8207203B2
  申请人：——

  公开号：US8207203B2

  公开（公告）日：2012-06-26