N-(4-((4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl)methyl)benzyl)acetamide

• 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: N-(4-((4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl)methyl)benzyl)acetamide
• 英文别名: N-[[4-[(4-amino-2-butylimidazo[4,5-c]quinolin-1-yl)methyl]phenyl]methyl]acetamide
• 化学式: C₂₄H₂₇N₅O
• 分子量: 401.511
• InChiKey: JILRNRLMDYOARY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  85.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  tert-butyl (4-(((3-amino-2-chloroquinolin-4-yl)amino)methyl)benzyl)carbamate 在 三乙胺 、 N,N-二异丙基乙胺 、 三苯基膦 、 sodium hydroxide 作用下， 以 四氢呋喃 、 乙醇 、 二甲基亚砜 、 N,N-二甲基甲酰胺 为溶剂， 反应 41.5h， 生成 N-(4-((4-amino-2-butyl-1H-imidazo[4,5-c]quinolin-1-yl)methyl)benzyl)acetamide
  参考文献：
  名称：

  [EN] TLR7/8 AGONISTS AND LIPOSOME COMPOSITIONS
  [FR] AGONISTES DE TLR7/8 ET COMPOSITIONS LIPOSOMALES

  摘要：

  本公开涉及一种利用远程加载的方法将调节剂（TLR）7/8激动剂装载到脂质体中，以及适用于通过该方法将TLR7/8激动剂装载到脂质体的部件套件。本公开进一步涉及包含TLR7/8激动剂盐的脂质体，并且利用该脂质体用于刺激免疫反应和/或治疗临床疾病。最后，本公开涉及一种适合远程装载到脂质体中的TLR7/8激动剂。

  公开号：

  WO2020023680A1

文献信息

• TOLL-LIKE RECEPTOR-7 AND -8 MODULATORY 1H IMIDAZOQUINOLINE DERIVED COMPOUNDS
  申请人：David Sunil A.

  公开号：US20120294885A1

  公开（公告）日：2012-11-22

  The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

  本公开提供了新型咪唑喹啉衍生化合物，其衍生物，类似物，以及其药用盐，并提供了制备和使用这些化合物的方法。本公开还提供了TLR7激动剂和TLR7/TLR8双激动剂，探针，组织特异性分子，佐剂，免疫原性组合物，治疗组合物，以及包括咪唑喹啉衍生化合物，其衍生物，类似物和药用盐的自佐剂疫苗。咪唑喹啉衍生化合物的衍生物还包括咪唑喹啉衍生化合物的树枝状分子和二聚体，以及制备和使用这些树枝状和二聚体咪唑喹啉衍生化合物的方法。本公开还提供了包括本公开的咪唑喹啉衍生化合物的双TLR2/TLR7混合激动剂。
• Toll-like receptor-7 and -8 modulatory 1H imidazoquinoline derived compounds
  申请人：The University of Kansas

  公开号：US10208037B2

  公开（公告）日：2019-02-19

  The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeric and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

  本公开提供了新型咪唑喹啉衍生化合物、其衍生物、其类似物、其药学上可接受的盐，以及制造和使用此类化合物的方法。本公开还提供了 TLR7 激动剂和 TLR7/TLR8 双激动剂、探针、组织特异性分子、佐剂、免疫原性组合物、治疗组合物和自佐剂疫苗，包括咪唑喹啉衍生化合物、其衍生物、其类似物和其药学上可接受的盐。咪唑喹啉衍生化合物的衍生物还包括咪唑喹啉衍生化合物的树枝状分子和二聚体，以及树枝状和二聚体咪唑喹啉衍生化合物的制造和使用方法。本公开还提供了双重TLR2/TLR7混合激动剂，其中包括本公开的咪唑喹啉衍生化合物。
• TLR7/8 AGONISTS AND LIPOSOME COMPOSITIONS
  申请人：Torque Therapeutics, Inc.

  公开号：US20210213010A1

  公开（公告）日：2021-07-15

  The present disclosure relates to a method of loading a toll like receptor (TLR)7/8 agonist into a liposome using remote loading and a kit of parts suitable for the loading of a TLR7/8 agonist into a liposome by said method. The present disclosure further relates to a liposome comprising a salt of a TLR7/8 agonist in the liposome interior and to the use of said liposome for stimulation of an immune response and/or treatment of a clinical condition. Finally, the present disclosure relates to a TLR7/8 agonist which is suitable for being remotely loaded into a liposome.
• AROMATIC RING SUBSTITUTED AMPHIPHILIC POLYMERS AS DRUG DELIVERY SYSTEMS
  申请人：Avldea Technologies, Inc.

  公开号：US20210393523A1

  公开（公告）日：2021-12-23

  An amphiphilic block copolymer having any one of the formulas S-[B]-H, S-[B]-H(D), D-[B]-H, S-B(D)-H, S-[B]-H-[B]-S, S-[B]-H(D)-[B]-S, D-[B]-H-[B]-S, D-[B]-H-[B]-D, S-B(D)-H-[B]-S or S-B(D)-H-B(D)-S; wherein S is a hydrophilic surface stabilizing group; B is a spacer group; H is a hydrophobic polymer or oligomer; D is a drug molecule; ( ) denotes that the group is bonded directly or indirectly as a side chain or as part of a side chain group to the adjacent group; [ ] denotes that the group is optional; and - denotes that each of the adjacent S, B, H or D are linked directly to one another or indirectly to one another via a linker group.
• [EN] TLR7/8 AGONISTS AND LIPOSOME COMPOSITIONS<br/>[FR] AGONISTES DE TLR7/8 ET COMPOSITIONS LIPOSOMALES
  申请人：TORQUE THERAPEUTICS INC

  公开号：WO2020023680A1

  公开（公告）日：2020-01-30

  The present disclosure relates to a method of loading a toll like receptor (TLR)7/8 agonist into a liposome using remote loading and a kit of parts suitable for the loading of a TLR7/8 agonist into a liposome by said method. The present disclosure further relates to a liposome comprising a salt of a TLR7/8 agonist in the liposome interior and to the use of said liposome for stimulation of an immune response and/or treatment of a clinical condition. Finally, the present disclosure relates to a TLR7/8 agonist which is suitable for being remotely loaded into a liposome.

  本公开涉及一种利用远程加载的方法将调节剂（TLR）7/8激动剂装载到脂质体中，以及适用于通过该方法将TLR7/8激动剂装载到脂质体的部件套件。本公开进一步涉及包含TLR7/8激动剂盐的脂质体，并且利用该脂质体用于刺激免疫反应和/或治疗临床疾病。最后，本公开涉及一种适合远程装载到脂质体中的TLR7/8激动剂。