1-(1-methylethyl)-N-[(6-methyl-2-oxo-4-propyl-1,2-dihydro-3-pyridinyl)methyl]-6-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indole-4-carboxamide | 1346572-13-1

• 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-[2-(4-methyl-1-piperazinyl)-4-pyridinyl]-1H-indole-4-carboxamide
• 英文别名: N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindole-4-carboxamide
• CAS: 1346572-13-1
• 化学式: C₃₂H₄₀N₆O₂
• 分子量: 540.709
• InChiKey: XTCIYPDQRLMSDH-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。
• INDOLES
  申请人：GlaxoSmithKline LLC

  公开号：US20130345200A1

  公开（公告）日：2013-12-26

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

  本文公开了式(I)中各个基团的定义，并且这些化合物对于治疗癌症是有用的。
• 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。
• INDOLE DERIVATIVES FOR THE TREATMENT OF CANCER
  申请人：GlaxoSmithKline LLC

  公开号：EP3246027A1

  公开（公告）日：2017-11-22

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

  这里公开了式 (I) 的吲哚 其中各基团在本文中定义，可用于治疗癌症。
• Methods of treating cancers overexpressing CARM1 with EZH2 inhibitors and platinum-based antineoplastic drugs
  申请人：The Wistar Institute of Anatomy and Biology

  公开号：US10987353B2

  公开（公告）日：2021-04-27

  In some embodiments, therapeutic treatments for a disease such as a cancer are disclosed, including pharmaceutical compositions and methods of using pharmaceutical compositions for treating the cancer wherein the cancer cells overexpress arginine methyltransferase CARM1. In some embodiments, the therapeutic treatments disclosed include methods comprising the step of administering a therapeutically effective dose of an enhancer of zeste homolog 2 (EZH2) inhibitor to a subject, including a human subject, wherein the cancer cells of the subject overexpress arginine methyltransferase CARM1. In some embodiments, the EZH2 inhibitors are administered in conjunction with platinum-based antineoplastic drugs.

  在一些实施方案中，公开了癌症等疾病的治疗方法，包括药物组合物和使用药物组合物治疗癌症的方法，其中癌细胞过度表达精氨酸甲基转移酶CARM1。在一些实施方案中，所公开的治疗方法包括向受试者（包括人类受试者）施用治疗有效剂量的泽斯特同源增强子2（EZH2）抑制剂的步骤，其中受试者的癌细胞过度表达精氨酸甲基转移酶CARM1。 在一些实施方案中，EZH2抑制剂与铂类抗肿瘤药物联合施用。