1-(5-Azido-2-nitrobenzoyl)pyrrolidine-2,5-dione

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-(5-Azido-2-nitrobenzoyl)pyrrolidine-2,5-dione
• 化学式: C11H7N5O5
• 分子量: 289.2
• InChiKey: VMQVFYDKJKVZLI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  115
• 氢给体数：
  0
• 氢受体数：
  7

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。
• Ultra-stable protein ionic liquids
  申请人：Government of the United States, as represented by the Secretary of the Air Force

  公开号：US10463733B1

  公开（公告）日：2019-11-05

  A method for creating a stable protein/antibody ionic liquid, comprising: (a) cationizing aqueous proteins/antibodies by addition of an excess of a positively-charged crosslinker in the presence of a coupling reagent; (b) purifying the cationized proteins/antibodies; (c) titrating the cationized proteins/antibodies with a corresponding biologically-compatible counter anionic polymer to create at least one protein/antibody cation/anion pair in aqueous solution until the cation/anion pair solution becomes negative by zeta potential measurement; (d) repeatedly dialyzing the protein/antibody cation/anion pair in water to remove excess anionic polymer using at least one molecular weight cutoff 7000 dialysis membrane; (e) lyophilizing the protein/antibody cation/anion pair to remove most of the water, forming a lyophilized solid; and (f) heating the lyophilized solid until a protein/antibody ionic liquid is generated. The antibody may be any desired antibody, and the anion may be any biologically-compatible anion.

  一种制造稳定的蛋白质/抗体离子液体的方法，包括(a) 在偶联试剂存在下，加入过量带正电荷的交联剂，使水溶液中的蛋白质/抗体阳离子化； (b) 纯化阳离子化的蛋白质/抗体； (c) 将阳离子化的蛋白质/抗体与相应的生物相容性反阴离子聚合物滴定，在水溶液中形成至少一对蛋白质/抗体阳离子/阴离子对，直到通过 zeta 电位测量阳离子/阴离子对溶液变为负值；(d) 在水中反复透析蛋白质/抗体阳离子/阴离子对，使用至少一种分子量截止值为 7000 的透析膜去除多余的阴离子聚合物； (e) 冻干蛋白质/抗体阳离子/阴离子对，去除大部分水分，形成冻干固体；以及 (f) 加热冻干固体，直至生成蛋白质/抗体离子液体。抗体可以是任何所需的抗体，阴离子可以是任何与生物相容的阴离子。
• Ultrastable antibody ionic liquids
  申请人：Government of the United States, as represented by the Secretary of the Air Force

  公开号：US11058770B1

  公开（公告）日：2021-07-13

  A stable protein ionic liquid, comprising an anti-hemoglobin cation/anion pair. The anti-hemoglobin cation/anion pair may be an anionic polymer of poly(ethylene glycol) 4-nonylphenyl 3-sulfopropyl ether. The anti-hemoglobin cation/anion pair may further comprise a cationized anti-hemoglobin antibody, single-chain antibodies from camelids, antibody fragments, polyclonal Anti-horse spleen ferritin antibodies, monoclonal Anti-Flag antibodies, monoclonal Anti-HRP2 to Plasmodium falciparum, polyclonal Anti-neuropeptide Y, polyclonal Anti-human troponin, isotypes of antibodies, or combinations of multiple antibodies.

  一种稳定的蛋白质离子液体，由抗血红蛋白阳离子/阴离子对组成。抗血红蛋白阳离子/阴离子对可以是聚乙二醇 4-壬基苯基 3-磺丙基醚的阴离子聚合物。抗血红蛋白阳离子/阴离子对可进一步包括阳离子化抗血红蛋白抗体、来自驼科动物的单链抗体、抗体片段、多克隆抗马脾铁蛋白抗体、单克隆抗Flag抗体、单克隆抗恶性疟原虫HRP2抗体、多克隆抗神经肽Y抗体、多克隆抗人肌钙蛋白抗体、同种抗体或多种抗体的组合。
• Biocleavable micelle compositions for use as drug carriers
  申请人：——

  公开号：US20010021703A1

  公开（公告）日：2001-09-13

  This invention discloses compositions and methods for preparing biocleavable or biodegradable micelle compositions for carrying and releasing drugs and other active agents for therapeutic or other medical uses. Methods are also disclosed for preparing biocleavable cyclodextrin micelle carriers that release drugs under controlled conditions. The invention also discloses biocleavable or biodegradable micelle compositions that are coupled to biorecognition molecules for targeting the delivery of drugs to their site of action.

  本发明公开了制备可生物裂解或可生物降解胶束组合物的组合物和方法，该组合物可携带和释放用于治疗或其他医疗用途的药物和其他活性剂。本发明还公开了制备可在受控条件下释放药物的可生物裂解环糊精胶束载体的方法。 本发明还公开了生物可裂解或生物可降解胶束组合物，这些组合物与生物识别分子耦合，用于将药物靶向输送到其作用部位。