(4-叠氮基苯基)-甲氧基甲亚胺 | 74676-96-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: (4-叠氮基苯基)-甲氧基甲亚胺
• 英文名称: Methyl-4-azido-benzoimidat
• 英文别名: methyl-4-azidobenzoimidate；Methyl 4-azidobenzimidate；methyl 4-azidobenzenecarboximidate
• CAS: 74676-96-3
• 化学式: C₈H₈N₄O
• 分子量: 176.178
• InChiKey: JZLFUUHOTZKEFU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  47.4
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• 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。
• 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。
• Pre-S gene coded peptide hepatitis B immunogens, vaccines, diagnostics, and synthetic lipid vesicle carriers
  申请人：New York Blood Center, Inc.

  公开号：EP0154902A2

  公开（公告）日：1985-09-18

  A hepatitis B vaccine containing a peptide with an amino acid chain of at least six consecutive amino acids within the pre-S gene coded region of the envelope of hepatitis B virus. The vaccine being free of an amino acid sequence corresponding to the naturally occuring evelope proteins of hepatitis B virus and a physiologically acceptable diluent. The peptide being free or linked to a carrier. The carrier being a conventional carrier or a novel carrier including a lipid vesicle stabilized by cross-linking and having covalently bonded active sites on the outer surface thereon. Such novel carrier being useful not only to link the novel peptide containing an amino acid chain with amino acids within the pre-S gene coded region of the surface antigen of hepatitis B virus, but can also be used to bind synthetic peptide analogues of other viral proteins, as well as bacterial, allergen and parasitic proteins of man and animals. The peptides of the invention can be utilized in diagnostics for the detection of antigens and antibodies.

  一种乙型肝炎疫苗，含有乙型肝炎病毒包膜前 S 基因编码区内至少六个连续氨基酸链的多肽。该疫苗不含与天然存在的乙型肝炎病毒包膜蛋白相对应的氨基酸序列和生理上可接受的稀释剂。多肽不含载体或与载体相连。载体可以是传统载体，也可以是新型载体，包括通过交联稳定的脂质囊泡，其外表面具有共价键活性位点。这种新型载体不仅可用于将含有氨基酸链的新型多肽与乙型肝炎病毒表面抗原前 S 基因编码区内的氨基酸连接起来，还可用于结合其他病毒蛋白的合成多肽类似物，以及人和动物的细菌、过敏原和寄生虫蛋白。本发明的多肽可用于抗原和抗体的诊断检测。
• Magnetische Microspheres
  申请人：BAYER AG

  公开号：EP0184710A2

  公开（公告）日：1986-06-18

  Die Erfindung betrifft magnetische Microspheres (MIMS), ein Verfahren zu ihrer Herstellung sowie ihre Verwendung zur Trennung und Isolierung biologischer Partikeln, insbesondere natürlicher oder artifizieller Zellen. Die mit dem erfindungsgemäßen Verfahren erhaltenen magnetischen Microspheres sind durch Quervernetzung stabilisiert und tragen an der Oberfläche funktionelle Gruppen, die die kovalente Bindung von biologisch aktiven Liganden erlauben.

  本发明涉及磁性微球（MIMS）、其生产工艺及其用于分离生物颗粒，特别是天然或人工细胞的用途。 根据本发明的方法获得的磁性微球通过交联稳定，表面具有官能团，可与生物活性配体共价结合。
• Pre-s gene codes peptide hepatitis b immunogens, vaccines, diagnostics, and synthetic lipid vesicle carriers
  申请人：New York Blood Center, Inc.

  公开号：EP0243913A2

  公开（公告）日：1987-11-04

  A hepatitis B vaccine containing a peptide with an amino acid chain of at least six consecutive amino acids within the pre-S gene coded region of the envelope of hepatitis 8 virus. The vaccine being free of an amino acid sequence corresponding to the naturally occurring envelope proteins of hepatitis B virus and a physiologically acceptable diluent. The peptide being free or linked to a carrier. The carrier being a conventional carrier or a novel carrier including a lipid vesicle stabilized by cross-linking and having covalently bonded active sites on the outer surface thereon. Such novel carrier being useful not only to link the novel peptide containing an amino acid chain with amino acids within the pre-S gene coded region of the surface antigen of hepatitis B virus, but can also be used to bind synthetic peptide analogues of other viral proteins, as well as bacterial, allergen and parasitic proteins of man and animals. The peptides of the invention can be utilized in diagnostics for the detection of antigens and antibodies.

  一种乙型肝炎疫苗，其中含有一种多肽，该多肽的氨基酸链至少有六个连续的氨基酸位于八型肝炎病毒包膜的前 S 基因编码区内。该疫苗不含与天然存在的乙型肝炎病毒包膜蛋白相对应的氨基酸序列和生理上可接受的稀释剂。多肽不含载体或与载体相连。载体可以是传统载体，也可以是新型载体，包括通过交联稳定的脂质囊泡，其外表面具有共价键活性位点。这种新型载体不仅可用于将含有氨基酸链的新型多肽与乙型肝炎病毒表面抗原前 S 基因编码区内的氨基酸连接起来，还可用于结合其他病毒蛋白的合成多肽类似物，以及人和动物的细菌、过敏原和寄生虫蛋白。本发明的多肽可用于抗原和抗体的诊断检测。