(4-Azidomethylphenyl)methyl Ketone

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 直链 1,3-二芳基丙烷
• 英文名称: (4-Azidomethylphenyl)methyl Ketone
• 英文别名: 1,3-Bis[4-(azidomethyl)phenyl]propan-2-one；1,3-bis[4-(azidomethyl)phenyl]propan-2-one
• 化学式: C₁₇H₁₆N₆O
• 分子量: 320.354
• InChiKey: NPKGFYQZPYHUOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  45.8
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Piperazine compounds and medicinal use thereof
  申请人：Adachi Kunitomo

  公开号：US20060167014A1

  公开（公告）日：2006-07-27

  The present invention relates to a piperazine compound of the formula wherein R 1 and R 2 are each hydrogen, halogen, lower alkyl, lower alkoxy, amino, substituted amino, nitro, hydroxy or cyano, R 3 , R 4 and R 5 are each hydrogen, halogen, lower alkyl, lower alkoxy, nitro, amino, substituted amino or hydroxy, R 6 and R 7 are each hydrogen, lower alkyl, lower alkyl substituted by halogen, aralkyl, acyl or lower acyl substituted by halogen, R 8 and R 9 are each hydrogen or lower alkyl, Y is lower alkylene and the like, and ring A is phenyl, pyrimidyl, thiazolyl, pyridyl, pyrazyl or imidazolyl, a pharmaceutically acceptable salt thereof and pharmaceutical agents containing these compounds. The compound of the present invention has superior TNF-α production inhibitory effect and/or IL-10 production promoting effect, and, since it is free of or shows only strikingly reduced expression of an effect on the central nervous system, the compound is useful as a highly safe and superior TNF-α production inhibitor an/or IL-10 production promoter and is useful as an agent for the prophylaxis or treatment of various diseases caused by abnormal TNF-α production, diseases curable with IL-10, such as chronic inflammatory diseases, acute inflammatory diseases, inflammatory diseases due to infection, autoimmune diseases, allergic diseases, and TNF-α mediated diseases.

  本发明涉及一种哌嗪化合物，其化学式为其中R1和R2分别为氢、卤素、低碳基、低烷氧基、氨基、取代氨基、硝基、羟基或氰基，R3、R4和R5分别为氢、卤素、低碳基、低烷氧基、硝基、氨基、取代氨基或羟基，R6和R7分别为氢、低碳基、被卤素取代的低烷基、芳基烷基、酰基或被卤素取代的低酰基，R8和R9分别为氢或低碳基，Y为低碳基亚烷基等，环A为苯基、嘧啶基、噻唑基、吡啶基、吡唑基或咪唑基，以及其药学上可接受的盐和含有这些化合物的药物制剂。本发明化合物具有优异的TNF-α产生抑制作用和/或IL-10产生促进作用，由于其不含或仅表现出在中枢神经系统上明显减弱的作用，因此该化合物可用作高度安全和优异的TNF-α产生抑制剂和/或IL-10产生促进剂，可用于预防或治疗由异常TNF-α产生引起的各种疾病，可用于治疗可用IL-10治愈的疾病，例如慢性炎症性疾病、急性炎症性疾病、由感染引起的炎症性疾病、自身免疫性疾病、过敏性疾病和TNF-α介导的疾病。
• US6455528B1
  申请人：——

  公开号：US6455528B1

  公开（公告）日：2002-09-24