N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}-4-hydrazino-4-oxobutanamide | 895522-02-8

• 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
• 英文名称: N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}-4-hydrazino-4-oxobutanamide
• 英文别名: N-[1-[4-amino-2-(ethoxymethyl)imidazo[4,5-c]quinolin-1-yl]-2-methylpropan-2-yl]-4-hydrazinyl-4-oxobutanamide
• CAS: 895522-02-8
• 化学式: C₂₁H₂₉N₇O₃
• 分子量: 427.506
• InChiKey: PKQNXWYELNXBKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  31
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  150
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  甲基胂酸 、 tert-butyl 2-[4-({2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}amino)-4-oxobutanoyl]hydrazinecarboxylate 在 三氟乙酸 作用下， 以 甲醇 、 二氯甲烷 、 氯仿 、 水 为溶剂， 生成 N-{2-[4-amino-2-(ethoxymethyl)-1H-imidazo[4,5-c]quinolin-1-yl]-1,1-dimethylethyl}-4-hydrazino-4-oxobutanamide
  参考文献：
  名称：

  IMMUNE RESPONSE MODIFIER CONJUGATES

  摘要：

  本发明提供了IRM共轭物，其中包括一个IRM基团和一个第二活性基团，该第二活性基团与IRM基团以共价键连接，且该共价键不依赖于紫外辐射。

  公开号：

  US20090035323A1

文献信息

• Compositions and methods for targeted delivery of immune response modifiers
  申请人：Alkan Sefik

  公开号：US20060142202A1

  公开（公告）日：2006-06-29

  The present invention provides immunomodulatory compositions include an immune response modifier moiety coupled to a targeting moiety. In another aspect, the invention provides methods of providing targeted delivery of an IRM, generating a localized immune response, and treating a condition in a subject. Generally, the methods include administering to the subject an immunomodulatory composition that includes an immune response modifier moiety coupled to a targeting moiety that recognizes a delivery target.

  本发明提供的免疫调节组合物包括将免疫反应修饰物与靶向修饰物耦合在一起。在另一个方面，本发明提供提供定向输送IRM、生成局部免疫反应和治疗受体的方法。通常，这些方法包括向受体注射免疫调节组合物，该组合物包括将免疫反应修饰物与能识别输送目标的靶向修饰物耦合在一起。
• Immune response modifier conjugates
  申请人：Stoermer Doris

  公开号：US08951528B2

  公开（公告）日：2015-02-10

  The present invention provides IRM conjugates that includes an IRM moiety and a second active moiety covalently linked to the IRM moiety in which the covalent link does not depend on UV irradiation.

  本发明提供了IRM偶联物，包括一个IRM基团和第二个活性基团，该第二个活性基团与IRM基团共价连接，而该共价连接不依赖于紫外线辐射。
• HETEROBIFUNCTIONAL LINKERS WITH POLYETHYLENE GLYCOL SEGMENTS AND IMMUNE RESPONSE MODIFIER CONJUGATES MADE THEREFROM
  申请人：3M INNOVATIVE PROPERTIES COMPANY

  公开号：US20140227317A1

  公开（公告）日：2014-08-14

  Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula (I): wherein A is CH or N, p is in a range from 1 to 50, R″ is a bond or -alkylene-O—, R′ is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.

  本文揭示了一种免疫应答调节剂、连接剂和抗原的共轭体。连接剂由式(I)表示：其中A为CH或N，p在1到50的范围内，R″为键或-烷基-O-，R′为烷基，可选地中断或终止于一个或多个酰胺或醚基团，E为胺基或硫醇反应基团。还揭示了含有该化合物或共轭体的制药组合物，制备共轭体的方法，以及将化合物或共轭体用作免疫调节剂在动物体内诱导细胞因子生物合成和预防动物的方法。还揭示了由连接剂修饰的抗原。
• Heterobifunctional linkers with polyethylene glycol segments and immune response modifier conjugates made therefrom
  申请人：3M INNOVATIVE PROPERTIES COMPANY

  公开号：US10723731B2

  公开（公告）日：2020-07-28

  Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula: wherein A is CH or N, p is in a range from 1 to 50, R″ is a bond or -alkylene-O—, R′ is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.

  本发明公开了一种免疫反应调节剂、一种连接体和一种抗原的共轭物。连接物由式表示： 其中A是CH或N，p在1至50的范围内，R″是键或-亚烷基-O-，R′是任选用一个或多个酰胺或醚基团间断或终止的亚烷基，E是胺或硫醇反应基团。还公开了含有化合物或共轭物的药物组合物、共轭物的制造方法以及化合物或共轭物作为免疫调节剂用于诱导动物体内细胞因子的生物合成和为动物接种疫苗的使用方法。还公开了经连接体修饰的抗原。
• US8951528B2
  申请人：——

  公开号：US8951528B2

  公开（公告）日：2015-02-10