AR03 | 510721-85-4

• 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: AR03
• 英文别名: 2,4,9-Trimethylbenzo[b][1,8]naphthyridin-5-amine
• CAS: 510721-85-4
• 化学式: C₁₅H₁₅N₃
• 分子量: 237.304
• InChiKey: WRUVTYDQVPMYDZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  51.8
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Small molecule toll-like receptor (TLR) antagonists
  申请人：Lipford B. Grayson

  公开号：US20050119273A1

  公开（公告）日：2005-06-02

  The invention provides methods and compositions useful for modulating signaling through Toll-like receptors. The methods involve contacting a TLR-expressing cell with a small molecule having a core structure including at least two rings. Certain of the compounds are 4-primary amino quinolines. Many of the compounds and methods are useful specifically for inhibiting immune stimulation involving at least one of TLR9, TLR8, TLR7, and TLR3. The methods may have use in the treatment of autoimmunity, inflammation, allergy, asthma, graft rejection, graft versus host disease, infection, sepsis, cancer, and immunodeficiency.

  本发明提供了用于调节通过Toll样受体信号传导的方法和组合物。该方法涉及使用含有至少两个环的核心结构的小分子与表达TLR的细胞接触。其中某些化合物是4-主氨基喹啉。许多化合物和方法特别适用于抑制涉及至少一个TLR9、TLR8、TLR7和TLR3的免疫刺激。该方法可用于治疗自身免疫、炎症、过敏、哮喘、移植排斥、移植物抗宿主病、感染、败血症、癌症和免疫缺陷。
• Activators and therapeutic applications thereof
  申请人：Johns Hopkins University

  公开号：EP2889297A2

  公开（公告）日：2015-07-01

  The present invention methods of identifying small molecule compounds that are activators of tumor suppressor p53, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways with the small molecules.

  本发明用于鉴定肿瘤抑制因子 p53 及其相关家族成员 p63 和 p73 功能激活剂的小分子化合物的方法。本发明进一步引出了用小分子化合物杀死肿瘤细胞和治疗需要激活 p53 家族成员通路的癌症或其他病症的方法。
• ACTIVATORS AND THERAPEUTIC APPLICATIONS THEREOF
  申请人：Johns Hopkins University

  公开号：EP2195316B1

  公开（公告）日：2015-08-12
• TLR INHIBITOR AND BRUTON'S TYROSINE KINASE INHIBITOR COMBINATIONS
  申请人：Pharmacyclics LLC

  公开号：EP3220912A1

  公开（公告）日：2017-09-27
• RNA COMBINATIONS AND COMPOSITIONS WITH DECREASED IMMUNOSTIMULATORY PROPERTIES
  申请人：CureVac AG

  公开号：EP4013880A1

  公开（公告）日：2022-06-22