(3-Carbamimidoylphenyl) 2-oxopropanoate

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 英文名称: (3-Carbamimidoylphenyl) 2-oxopropanoate
• 英文别名: (3-carbamimidoylphenyl) 2-oxopropanoate
• 化学式: C₁₀H₁₀N₂O₃
• 分子量: 206.2
• InChiKey: VUSOEJJVEGEXJK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  15
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  93.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Opioid compositions resistant to overdose and abuse
  申请人：Elysium Therapeutics, Inc.

  公开号：US10335406B2

  公开（公告）日：2019-07-02

  The invention provides pharmaceutical compositions comprising macromolecular gastrointestinal enzyme-labile opioid prodrugs, co-formulated with small-molecule and/or macromolecular gastrointestinal enzyme inhibitors. The macromolecular constructs are minimally absorbed from the GI tract, and can produce non-linear pharmacokinetic profiles of the delivered opioid agonist following oral ingestion. An optional macromolecular opioid antagonist may also be present in compositions of the invention to discourage tampering by potential abusers.

  本发明提供了由大分子胃肠道酶抑制阿片类原药与小分子和/或大分子胃肠道酶抑制剂共同配制而成的药物组合物。大分子构建物从胃肠道的吸收率极低，口服后可产生所输送阿片类激动剂的非线性药代动力学特征。本发明的组合物中还可加入一种可选的大分子阿片拮抗剂，以防止潜在的滥用者篡改。
• OPIOID COMPOSITIONS RESISTANT TO OVERDOSE AND ABUSE
  申请人：Elysium Therapeutics, Inc.

  公开号：US20180085366A1

  公开（公告）日：2018-03-29

  The invention provides pharmaceutical compositions comprising macromolecular gastrointestinal enzyme-labile opioid prodrugs, co-formulated with small-molecule and/or macromolecular gastrointestinal enzyme inhibitors. The macromolecular constructs are minimally absorbed from the GI tract, and can produce non-linear pharmacokinetic profiles of the delivered opioid agonist following oral ingestion. An optional macromolecular opioid antagonist may also be present in compositions of the invention to discourage tampering by potential abusers.