9-氧代-10H-吖啶-4-甲酰胺 | 37760-72-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 9-氧代-10H-吖啶-4-甲酰胺
• 英文名称: 9,10-dihydro-9-oxo-4-acridinecarboxamide
• 英文别名: 9-oxo-9,10-dihydro-acridine-4-carboxylic acid amide；Acridon-carbonsaeure-(4)-amid；9(10H)-Acridone carboxamide；9-oxo-10H-acridine-4-carboxamide
• CAS: 37760-72-8
• 化学式: C₁₄H₁₀N₂O₂
• 分子量: 238.246
• InChiKey: UWRRBLDAEWEWRC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  72.2
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  氯甲酸乙酯 、 9-氧代-10H-吖啶-4-甲酰胺 反应 48.0h， 以88%的产率得到2H-pyrimido<5,6,1-d,e>acridine-1,3,7-trione
  参考文献：
  名称：

  Antonini, Ippolito; Martelli, Sante, Journal of Heterocyclic Chemistry, 1992, vol. 29, # 2, p. 471 - 473

  摘要：

  DOI：
• 作为产物：
  描述：

  9-chloro-4-aminocarbonylacridine 在 盐酸 作用下， 以 甲醇 为溶剂， 生成 9-氧代-10H-吖啶-4-甲酰胺
  参考文献：
  名称：

  Antonini, Ippolito; Martelli, Sante, Journal of Heterocyclic Chemistry, 1992, vol. 29, # 2, p. 471 - 473

  摘要：

  DOI：

文献信息

• Chloroquine coupled nucleic acids and methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20060040879A1

  公开（公告）日：2006-02-23

  This invention discloses compositions and methods for preparing chloroquine-coupled nucleic acid compositions. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the nucleic acid needs to be released, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a nucleic acid directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

  本发明披露了制备氯喹偶联核酸组合物的组成和方法。先前的研究表明，以足够高的浓度给予氯喹作为自由药物，可以增强细胞内体内各种物质从内体泡中释放到细胞质中。这些组合物的目的是在核酸需要释放的同一位置提供受控量的氯喹，从而降低所需的总剂量。该组合物包括直接或通过各种药物载体物质偶联的氯喹物质和核酸。载体物质包括多糖、合成聚合物、蛋白质、胶束和其他用于在体内携带和释放氯喹组合物以达到治疗效果的物质。该组合物还可以包括生物可降解连接来携带和释放用于治疗或其他医疗用途的核酸。本发明还披露了偶联到靶向分子的核酸载体组合物，用于将核酸传递到其作用位置。
• Nucleic acid carrier compositions and methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20050153913A1

  公开（公告）日：2005-07-14

  This invention discloses compositions and methods for preparing pharmaceutical nucleic acid carriers. The compositions comprise a carrier substance coupled to a nucleic acid intercalator whereby the intercalator is coupled by intercalation to the nucleic acid. The compositions can also include a biocleavable linkage for carrying and releasing nucleic acids for therapeutic or other medical uses. The invention also discloses nucleic acid carrier compositions that are coupled to targeting molecules for targeting the delivery of nucleic acids to their site of action.

  本发明公开了制备药物核酸载体的组合物和方法。这些组合物包括与核酸插层物耦合的载体物质，其中插层物通过插层与核酸耦合。这些组合物还可以包括生物可裂解连接，用于携带和释放核酸，以用于治疗或其他医疗用途。本发明还公开了与靶向分子偶联的核酸载体组合物，用于将核酸靶向递送至其作用位点。
• [EN] METHODS OF NAD+-DEPENDENT DEACETYLASE INHIBITORS<br/>[FR] METHODES D'UTILISATION D'INHIBITEURS DE DESACETYLASE NAD+ DEPENDANTE
  申请人：GUILFORD PHARM INC

  公开号：WO2005053609A3

  公开（公告）日：2005-09-01
• ACRIDINE DERIVATIVES
  申请人：LABORATOIRES GLAXO SA

  公开号：EP0569380A1

  公开（公告）日：1993-11-18
• Chloroquine drug compositions and methods for their synthesis
  申请人：Kosak Kenneth M.

  公开号：US20080051323A1

  公开（公告）日：2008-02-28

  This invention discloses compositions of chloroquine-coupled active agents, including methods for their preparation. The prior art has shown that chloroquines given as free drug in high enough concentration, enhances the release of various agents from cellular endosomes into the cytoplasm. The purpose of these compositions is to provide a controlled amount of chloroquine at the same site where the active agent is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to an active agent directly or through a variety of pharmaceutical carrier substances. The carrier substances include polysaccharides, synthetic polymers, proteins, micelles and other substances for carrying and releasing the chloroquine compositions in the body for therapeutic effect. The compositions can also include a biocleavable linkage for carrying and releasing active agents for therapeutic or other medical uses. The invention also discloses carrier compositions that are coupled to targeting molecules for targeting the delivery of chloroquine substances and active agents to their site of action.