(4-Acetamido-phenyl)-2-oxo-thiazolidine-4-carboxylate | 1196659-78-5

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (4-Acetamido-phenyl)-2-oxo-thiazolidine-4-carboxylate
• 英文别名: (4-Acetamidophenyl) 2-oxo-1,3-thiazolidine-4-carboxylate
• CAS: 1196659-78-5
• 化学式: C₁₂H₁₂N₂O₄S
• 分子量: 280.304
• InChiKey: WDQHMRARFAJHPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-氧代-4-噻唑烷羧酸 、 草酰氯 、 对乙酰氨基酚 生成 (4-Acetamido-phenyl)-2-oxo-thiazolidine-4-carboxylate
  参考文献：
  名称：

  REVESZ, L.;PETCHER, T. J.

  摘要：

  DOI：

文献信息

• Acylaminophenol derivatives
  申请人：Sandoz Ltd.

  公开号：US04567192A1

  公开（公告）日：1986-01-28

  Compounds of formula I ##STR1## wherein n=1 to 5 possessing analgesic activity with reduced hepatoxicity as compared with paracetamol.

  化合物的化学式为I ##STR1## 其中n=1到5，具有与对乙酰氨基酚相比减少肝毒性的镇痛活性。
• HEPATOPROTECTANT ACETAMINOPHEN MUTUAL PRODRUGS
  申请人：Muhammad Naweed

  公开号：US20110263545A1

  公开（公告）日：2011-10-27

  The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.

  本发明提供了肝保护醋氨酚共价偶联物，其含有醋氨酚基团与第二基团共价结合，第二基团可能作为肝保护剂对抗醋氨酚肝毒性。此外，醋氨酚共价偶联物可能具有改善的水溶性，相对于醋氨酚的给药方式，更适合于静脉和其他剂型的使用。本发明还提供了使用肝保护醋氨酚共价偶联物治疗对醋氨酚具有反应的疾病或病况的方法（如发热、疼痛和缺血性损伤），以及套装和单元剂量。
• US4567192A
  申请人：——

  公开号：US4567192A

  公开（公告）日：1986-01-28
• US9951001B2
  申请人：——

  公开号：US9951001B2

  公开（公告）日：2018-04-24
• [EN] HEPATOPROTECTANT ACETAMINOPHEN MUTUAL PRODRUGS<br/>[FR] PROMÉDICAMENTS MUTUELS D'ACÉTAMINOPHÈNE ET D'HÉPATOPROTECTEUR
  申请人：NEUROGESX INC

  公开号：WO2009143299A1

  公开（公告）日：2009-11-26

  The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.