1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide | 1346572-71-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide
• 英文别名: 1-isopropyl-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide；EZ-21；N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindole-4-carboxamide
• CAS: 1346572-71-1
• 化学式: C₃₂H₄₀N₆O₂
• 分子量: 540.709
• InChiKey: SXAHDROJSOYBGU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  40
• 可旋转键数：
  8
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  82.5
• 氢给体数：
  2
• 氢受体数：
  5

文献信息

• [EN] INDOLES<br/>[FR] INDOLES
  申请人：GLAXOSMITHKLINE LLC

  公开号：WO2011140324A1

  公开（公告）日：2011-11-10

  herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.

  本文揭示了式(I)中吲哚的各种基团的定义，并且这些吲哚对治疗癌症有用。
• [EN] EZH2 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS D'EZH2 ET LEURS UTILISATIONS
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2016073956A1

  公开（公告）日：2016-05-12

  The present disclosure provides compounds of any one of Formulae (I) and (II). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. Further provided in the present disclosure are methods of identifying EZH1and/or EZH2 inhibitors.

  本公开提供了任一式（I）和（II）中的化合物。本文描述的化合物是组蛋白甲基转移酶抑制剂（例如增强子齿同源蛋白1（EZH1）和增强子齿同源蛋白2（EZH2）），可用于治疗和/或预防广泛范围的疾病（例如增生性疾病）。本公开还提供了包括或使用本文描述的化合物的药物组合物、试剂盒、方法和用途。本公开还提供了识别EZH1和/或EZH2抑制剂的方法。
• [EN] USE OF COMPOSITIONS MODULATING CHROMATIN STRUCTURE FOR GRAFT VERSUS HOST DISEASE (GVHD)<br/>[FR] UTILISATION DE COMPOSITIONS MODULANT LA STRUCTURE DE LA CHROMATINE CONTRE LA MALADIE DU GREFFON CONTRE L'HÔTE (GVHD)
  申请人：DANA FARBER CANCER INST INC

  公开号：WO2016073903A1

  公开（公告）日：2016-05-12

  In some aspects, the instant disclosure relates to methods of treating chronic graft versus host disease (cGVHD). In some embodiments, the method comprises administering to a subject in need thereof a EZH2 inhibitor, a Bcl6 inhibitor and/or BRD4 inhibitor. The present disclosure is based, at least in part, on the discovery that enhancer of zeste homolog 2 (EZH2) inhibitors, B-cell lymphoma 6 protein (Bcl6) inhibitors and/or bromodomain-containing protein 4 (BRD4) inhibitors can be used to treat chronic graft versus host disease (cGVHD).

  在某些方面，瞬时披露涉及治疗慢性移植物抗宿主病（cGVHD）的方法。在某些实施例中，该方法包括向需要该方法的受试者施用EZH2抑制剂、Bcl6抑制剂和/或BRD4抑制剂。本公开至少部分地基于发现，增强子of zeste同源物2（EZH2）抑制剂、B细胞淋巴瘤6蛋白（Bcl6）抑制剂和/或含有bromodomain的蛋白4（BRD4）抑制剂可用于治疗慢性移植物抗宿主病（cGVHD）。
• INDOLES
  申请人：Brackley, III James

  公开号：US20130053397A1

  公开（公告）日：2013-02-28

  Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful in treating cancer.

  本文披露了式(I)中各种基团的吲哚类化合物（见下文定义），这些化合物在治疗癌症方面具有用途。
• METHOD OF TREATMENT
  申请人：GlaxoSmithKline Intellectual Property (No. 2) Limited

  公开号：US20160074394A1

  公开（公告）日：2016-03-17

  The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.

  本发明涉及一种治疗T细胞介导的炎症免疫性疾病或T细胞介导的过敏性疾病的方法，包括向需要治疗的人类施用一种有效量的抑制EZH2和/或EZH1的化合物或其药学可接受的盐。