(isopropylsulfonyl)-6-methoxy-2-[[(3.5-dimethyl-4-methoxy-pyridin-2-yl)methyl]sulfinyl]-1H-benzimidazole | 259183-22-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: (isopropylsulfonyl)-6-methoxy-2-[[(3.5-dimethyl-4-methoxy-pyridin-2-yl)methyl]sulfinyl]-1H-benzimidazole
• 英文别名: (isopropylsulfonyl)-6-methoxy-2-[[(3.5-dimethyl-4-methoxy-2-pyridyl)methyl]sulfinyl]-1H-benzimidazole；6-Methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1-propan-2-ylsulfonylbenzimidazole
• CAS: 259183-22-7
• 化学式: C₂₀H₂₅N₃O₅S₂
• 分子量: 451.568
• InChiKey: WGUWIIFBFFSECY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  128
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  异丙基磺酰氯 、 奥美拉唑 在 三乙胺 作用下， 以 氯仿 为溶剂， 生成 (isopropylsulfonyl)-6-methoxy-2-[[(3.5-dimethyl-4-methoxy-pyridin-2-yl)methyl]sulfinyl]-1H-benzimidazole
  参考文献：
  名称：

  Prodrugs of proton pump inhibitors

  摘要：

  该类型的吡啶甲基亚砜基苯并咪唑类质子泵抑制剂药物的前药，其将可水解的芳基磺酰基或杂环芳基磺酰基连接到咪唑类氮原子上。本发明的前药在生理条件下水解，提供半衰期可在小时内测量的质子泵抑制剂，并能够提供比目前使用的药物更长时间的持续血浆浓度。在生理条件下从本发明的前药生成质子泵抑制剂药物，可更有效地治疗由胃酸分泌引起的多种疾病和症状。

  公开号：

  US06559167B1

文献信息

• PRODRUGS OF PROTON PUMP INHIBITORS
  申请人：Partnership of Michael E. Garst, George Sachs and Jai Moo Shin

  公开号：EP1105387A1

  公开（公告）日：2001-06-13
• [EN] PRODRUGS OF PROTON PUMP INHIBITORS<br/>[FR] PROMEDICAMENTS D'INHIBITEURS DE LA POMPE A PROTONS
  申请人：PARTNERSHIP OF MICHAEL E GARST

  公开号：WO2000009498A1

  公开（公告）日：2000-02-24

  Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable sulfinyl or arylsulfonyl group attached to the benzimidazole nitrogen, or include a group that forms a Mannich base with the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.
• Prodrugs of proton pump inhibitors
  申请人：Regents of the University of California

  公开号：US06559167B1

  公开（公告）日：2003-05-06

  Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.

  该类型的吡啶甲基亚砜基苯并咪唑类质子泵抑制剂药物的前药，其将可水解的芳基磺酰基或杂环芳基磺酰基连接到咪唑类氮原子上。本发明的前药在生理条件下水解，提供半衰期可在小时内测量的质子泵抑制剂，并能够提供比目前使用的药物更长时间的持续血浆浓度。在生理条件下从本发明的前药生成质子泵抑制剂药物，可更有效地治疗由胃酸分泌引起的多种疾病和症状。