N-(1-benzylpiperidin-4-yl)-2-(4-methylpiperazin-1-yl)quinazoline-4-amine | 1435055-53-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-(1-benzylpiperidin-4-yl)-2-(4-methylpiperazin-1-yl)quinazoline-4-amine
• 英文别名: N-(1-benzylpiperidin-4-yl)-2-(4-methylpiperazin-1-yl)quinazolin-4-amine
• CAS: 1435055-53-0
• 化学式: C₂₅H₃₂N₆
• 分子量: 416.569
• InChiKey: JMQYVDHKMIHOPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  47.5
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  2,4-喹唑啉二酮 在 N,N-二异丙基乙胺 、 N,N-二乙基苯胺 、 三氯氧磷 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 0.5h， 生成 N-(1-benzylpiperidin-4-yl)-2-(4-methylpiperazin-1-yl)quinazoline-4-amine
  参考文献：
  名称：

  Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitors

  摘要：

  为了发现新的G9a抑制剂化合物，我们已经确定了一种新的喹啉抑制剂骨架，并更好地定义了中心杂环的药效特征。

  DOI：

  10.1039/c4md00274a

文献信息

• [EN] QUINAZOLINE COMPOUNDS AND THEIR USE IN THERAPY<br/>[FR] COMPOSÉS DE QUINAZOLINE ET LEUR UTILISATION THÉRAPEUTIQUE
  申请人：IMP INNOVATIONS LTD

  公开号：WO2013140148A1

  公开（公告）日：2013-09-26

  This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.

  本发明涉及式（I）的喹唑啉化合物，其为组蛋白赖氨酸甲基转移酶（HKMTase）EZH2的抑制剂，并且涉及使用这些化合物作为药物，特别是在治疗某种疾病或紊乱中，EZH2的抑制提供治疗或预防效果。
• Cellular Compositions Used To Restore Stem Cell or Progenitor Cell Function and Methods Related Thereto
  申请人：Emory University

  公开号：US20170157178A1

  公开（公告）日：2017-06-08

  This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, methods of treating or preventing vascular or diabetic diseases or conditions are contemplated. In certain embodiments, epigenetically reprogramming adult bone marrow-derived stem or progenitor cells including mesenchymal stem cells (MSCs) or endothelial progenitor cells (EPCs) for autologous treatments are contemplated.

  这份披露涉及化合物、组合物和改变细胞表观遗传的方法。在某些实施例中，该披露涉及将孤立细胞与此处披露的组合物混合，在条件下使得表观遗传改变的细胞形成的方法。在某些实施例中，考虑了治疗或预防血管性或糖尿病性疾病或症状的方法。在某些实施例中，考虑了对成年骨髓来源的干细胞或祖细胞进行表观遗传重编程，包括间充质干细胞（MSCs）或内皮祖细胞（EPCs），用于自体治疗。
• Quinazoline Compounds And Their Use In Therapy
  申请人：Imperial Innovations Limited

  公开号：US20150057263A1

  公开（公告）日：2015-02-26

  This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.

  本发明涉及公式（I）的喹嗪化合物，其是组蛋白赖氨酸甲基转移酶（HKMTase）EZH2的抑制剂，并且涉及将这些化合物用作药物的用途，特别是用于治疗抑制EZH2具有治疗或预防效果的疾病或障碍。
• Cellular compositions used to restore stem cell or progenitor cell function and methods related thereto
  申请人：Emory University

  公开号：US10828331B2

  公开（公告）日：2020-11-10

  This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, methods of treating or preventing vascular or diabetic diseases or conditions are contemplated. In certain embodiments, epigenetically reprogramming adult bone marrow-derived stem or progenitor cells including mesenchymal stem cells (MSCs) or endothelial progenitor cells (EPCs) for autologous treatments are contemplated.

  本公开涉及表观遗传转化细胞的化合物、组合物和方法。在某些实施方案中，本公开涉及产生表观遗传改变细胞的方法，包括在形成表观遗传改变细胞的条件下，将分离的细胞与本文公开的组合物混合。在某些实施方案中，考虑了治疗或预防血管或糖尿病疾病或病症的方法。在某些实施方案中，考虑了表观遗传重编程成人骨髓来源的干细胞或祖细胞，包括间充质干细胞（MSCs）或内皮祖细胞（EPCs），用于自体治疗。
• QUINAZOLINE COMPOUNDS AND THEIR USE IN THERAPY
  申请人：Imperial College Innovations Limited

  公开号：EP2828250B1

  公开（公告）日：2021-03-10