11-chloro-8H-benzimidazo[2,1-a]phenanthro[3,4,5-defg]isoquinolin-8-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 芘
• 英文名称: 11-chloro-8H-benzimidazo[2,1-a]phenanthro[3,4,5-defg]isoquinolin-8-one
• 英文别名: 7-chloro-3,10-diazaheptacyclo[20.3.1.02,10.04,9.012,25.015,24.018,23]hexacosa-1(26),2,4(9),5,7,12(25),13,15(24),16,18(23),19,21-dodecaen-11-one
• 化学式: C₂₄H₁₁ClN₂O
• 分子量: 378.8
• InChiKey: WDPLIRXDZQTPOG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.5
• 重原子数：
  28
• 可旋转键数：
  0
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  34.9
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Compounds and methods to suppress autoimmune response
  申请人：Oregon State University

  公开号：US10308649B2

  公开（公告）日：2019-06-04

  A composition and method for treating autoimmune disease includes administering an effective amount of an aryl hydrocarbon receptor (AhR) ligand. The AhR ligand includes 11-Cl-BBQ, 10-Cl-BBQ, an analog of 11-Cl-BBQ, or combination thereof. The AhR ligand is administered topically, orally, transdermally, intravenously, subcutaneously, or with a nanoparticle. The AhR ligand induces regulatory T cells (AhR-Tregs). AhR-Treg cells block the differentiation of cytotoxic T-lymphocytes (CTL). The AhR ligand activates AhR in CD4+ T cells to induce CD4+ AhR-Tregs that suppress the development of effector CTL, thereby suppressing the development of CTL that attack host cells in graft versus host disease (GVHD) or β-cells in the pancreas in diabetes mellitus type 1 (T1DM). The AhR ligand can also suppress development of CTL independently of Foxp3+ regulatory T cell induction. The AhR ligand can therefore be used to treat autoimmune diseases characterized by an absence of functional Foxp3+ regulatory T cell.

  一种治疗自身免疫性疾病的组合物和方法包括施用有效量的芳基烃受体（AhR）配体。AhR 配体包括 11-Cl-BBQ、10-Cl-BBQ、11-Cl-BBQ 的类似物或其组合。AhR 配体可局部给药、口服、透皮给药、静脉注射、皮下注射或用纳米颗粒给药。AhR 配体可诱导调节性 T 细胞（AhR-Tregs）。AhR-Treg细胞可阻止细胞毒性T淋巴细胞（CTL）的分化。AhR 配体激活 CD4+ T 细胞中的 AhR，诱导 CD4+ AhR-Tregs，抑制效应 CTL 的发育，从而抑制 CTL 的发育，CTL 会攻击移植物抗宿主疾病（GVHD）中的宿主细胞或 1 型糖尿病（T1DM）胰腺中的β细胞。AhR 配体还能抑制 CTL 的发展，而不依赖于 Foxp3+ 调节性 T 细胞的诱导。因此，AhR 配体可用于治疗以缺乏功能性 Foxp3+ 调节性 T 细胞为特征的自身免疫性疾病。
• COMPOUNDS TO SUPPRESS AUTOIMMUNE RESPONSE
  申请人：OREGON STATE UNIVERSITY

  公开号：EP3212634B1

  公开（公告）日：2021-04-21
• COMPOUNDS AND METHODS TO SUPPRESS AUTOIMMUNE RESPONSE
  申请人：Oregon State University

  公开号：US20180030048A1

  公开（公告）日：2018-02-01

  A composition and method for treating autoimmune disease includes administering an effective amount of an aryl hydrocarbon receptor (AhR) ligand. The AhR ligand includes 11-Cl-BBQ, 10-Cl-BBQ, an analog of 11-Cl-BBQ, or combination thereof. The AhR ligand is administered topically, orally, transdermally, intravenously, subcutaneously, or with a nanoparticle. The AhR ligand induces regulatory T cells (AhR-Tregs). AhR-Treg cells block the differentiation of cytotoxic T-lymphocytes (CTL). The AhR ligand activates AhR in CD4+ T cells to induce CD4+ AhR-Tregs that suppress the development of effector CTL, thereby suppressing the development of CTL that attack host cells in graft versus host disease (GVHD) or β-cells in the pancreas in diabetes mellitus type 1 (T1DM). The AhR ligand can also suppress development of CTL independently of Foxp3+ regulatory T cell induction. The AhR ligand can therefore be used to treat autoimmune diseases characterized by an absence of functional Foxp3+ regulatory T cell.