primaquine hydrochloride | 86166-06-5

• 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
• 英文名称: primaquine hydrochloride
• 英文别名: N¹-(6-methoxy-[8]quinolyl)-1-methyl-butanediyldiamine; hydrochloride；N¹-(6-Methoxy-[8]chinolyl)-1-methyl-butandiyldiamin; Hydrochlorid；primaquine HCl salt；4-N-(6-methoxyquinolin-8-yl)pentane-1,4-diamine;hydrochloride
• CAS: 86166-06-5
• 化学式: C₁₅H₂₁N₃O*ClH
• 分子量: 295.812
• InChiKey: KITVDTRJECUXAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  20
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  60.2
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  primaquine hydrochloride 、 FmocAsp(OBt)OBu^t 在 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 、 二氯甲烷 为溶剂， 反应 0.41h， 生成 tert-butyl N2-[(9H-fluoren-9-ylmethoxy)carbonyl]-N4-(4-[(6-methoxyquinolin-8-yl)amino]-pentyl)-L-asparaginate
  参考文献：
  名称：

  Chloroquine combination drugs and methods for their synthesis

  摘要：

  这项发明揭示了氯喹偶联活性药剂的组合物，包括其制备方法。先前的技术已经表明，以足够高浓度给予氯喹作为游离药物，可以增强细胞内体内各种药剂从细胞内体释放到细胞质中。这些组合物的目的是在传递活性药剂的相同部位提供受控量的氯喹，从而减少所需的总剂量。这些组合物包括将氯喹物质直接或通过各种药用载体物质偶联到活性药剂。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产生治疗效果的物质。这些组合物还可以包括用于携带和释放活性药剂以用于治疗或其他医疗用途的生物可降解连接。该发明还揭示了与靶向分子偶联的载体组合物，用于将氯喹物质和活性药剂定位传递到它们的作用部位。

  公开号：

  US20070060499A1

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。
• Chloroquine coupled antibodies and other proteins with methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20070166281A1

  公开（公告）日：2007-07-19

  This invention discloses compositions of chloroquine-coupled active agents such as therapeutic antibodies or insulin, 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 drug is delivered, thereby reducing the overall dosage needed. The compositions comprise a chloroquine substance coupled to a drug 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 the drug 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 antibody or insulin to their site of action.
• 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.
• Chloroquine combination drugs and methods for their synthesis
  申请人：Kosak M. Kenneth

  公开号：US20070060499A1

  公开（公告）日：2007-03-15

  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.

  这项发明揭示了氯喹偶联活性药剂的组合物，包括其制备方法。先前的技术已经表明，以足够高浓度给予氯喹作为游离药物，可以增强细胞内体内各种药剂从细胞内体释放到细胞质中。这些组合物的目的是在传递活性药剂的相同部位提供受控量的氯喹，从而减少所需的总剂量。这些组合物包括将氯喹物质直接或通过各种药用载体物质偶联到活性药剂。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产生治疗效果的物质。这些组合物还可以包括用于携带和释放活性药剂以用于治疗或其他医疗用途的生物可降解连接。该发明还揭示了与靶向分子偶联的载体组合物，用于将氯喹物质和活性药剂定位传递到它们的作用部位。