7-[(2-azaniumyl-2-phenylacetyl)amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 7-[(2-azaniumyl-2-phenylacetyl)amino]-3-chloro-8-oxo-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
• 化学式: C16H16ClN3O4
• 分子量: 349.77
• InChiKey: JAPHQRWPEGVNBT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  113
• 氢给体数：
  3
• 氢受体数：
  5

文献信息

• Active agent delivery systems and methods for protecting and administering active agents
  申请人：New River Pharmaceuticals Inc.

  公开号：US20040063628A1

  公开（公告）日：2004-04-01

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性物质输送系统，更具体地涉及包含氨基酸，作为单个氨基酸或肽的组成部分，与活性物质共价连接的组合物和用于给予共轭活性物质组合物的方法。
• ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
  申请人：Mickle Travis

  公开号：US20090253792A1

  公开（公告）日：2009-10-08

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂递送系统，更具体地涉及包含氨基酸（作为单个氨基酸或肽）与活性剂共价连接的组合物以及给予共轭活性剂组合物的方法。
• ACTIVE AGENT DELIVERY SYSTEMS AND METHODS FOR PROTECTING AND ADMINISTERING ACTIVE AGENTS
  申请人：Mickle Travis

  公开号：US20090306228A1

  公开（公告）日：2009-12-10

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂递送系统，更具体地涉及包含氨基酸，作为单个氨基酸或肽，与活性剂共价结合的组合物以及用于给予共轭活性剂组合物的方法。
• Sustained release matrix formulations
  申请人：ELI LILLY AND COMPANY

  公开号：EP0280571A2

  公开（公告）日：1988-08-31

  This invention provides a matrix composition for sustained drug delivery which is comprised of an active agent, a hydrophilic polymer and an enteric polymer. The enteric polymer is impermeable to gastric fluids and aids in retarding drug release in regions of low pH, thus allowing lower levels of hydrophilic polymer to be employed. At the pH range of intestinal fluids, this polymer will dissolve and thereby increase the permeability of the dosage form. This approach is useful in sustaining the release of numerous active agents whose solubility declines as the pH is increased, a characteristic of weakly basic drugs. By responding to changes in physiological pH, these sustained release dosage forms have acceptable performance, in spite of variability in the gastrointestinal transit times of the formulation.

  本发明提供了一种用于持续给药的基质组合物，它由活性剂、亲水性聚合物和肠道聚合物组成。肠道聚合物对胃液无渗透性，有助于延缓药物在低 pH 值区域的释放，从而允许使用较低含量的亲水性聚合物。在肠液的 pH 值范围内，这种聚合物会溶解，从而增加剂型的渗透性。这种方法适用于多种活性药物的持续释放，这些药物的溶解度会随着 pH 值的升高而降低，这是弱碱性药物的特点。通过对生理 pH 值的变化做出反应，这些缓释制剂具有可接受的性能，尽管制剂的胃肠道通过时间会发生变化。
• Active agent delivery sytems and methods for protecting and administering active agents
  申请人：Shire LLC

  公开号：EP2266590A2

  公开（公告）日：2010-12-29

  The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active agents and methods for administering conjugated active agent compositions.

  本发明涉及活性剂给药系统，更具体地说，涉及由与活性剂共价连接的氨基酸（作为单个氨基酸或肽）组成的组合物以及给药共轭活性剂组合物的方法。