2-Propenamide, N-hydroxy-3-(4-(((2-hydroxyethyl)(2-(1H-indol-2-yl)ethyl)amino)methyl)phenyl)- | 591207-53-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: 2-Propenamide, N-hydroxy-3-(4-(((2-hydroxyethyl)(2-(1H-indol-2-yl)ethyl)amino)methyl)phenyl)-
• 英文别名: (E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-2-yl)ethyl]amino]methyl]phenyl]prop-2-enamide
• CAS: 591207-53-3
• 化学式: C₂₂H₂₅N₃O₃
• 分子量: 379.5
• InChiKey: FGJCGXHQLHHNFO-MDZDMXLPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  28
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  88.6
• 氢给体数：
  4
• 氢受体数：
  4

文献信息

• Method of treating cancers with SAHA and pemetrexed
  申请人：Pluda James

  公开号：US20070117815A1

  公开（公告）日：2007-05-24

  The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of an anti-cancer agent. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

  本发明涉及一种治疗需要的受试者癌症的方法，通过向需要的受试者施用一定量的组蛋白去乙酰化酶（HDAC）抑制剂或其药用可接受的盐或水合物的第一量，以及一定量的抗癌药物。HDAC抑制剂和抗癌药物可以被施用以包含治疗有效量。在各种方面，HDAC抑制剂和抗癌药物的效果可能是相加的或协同的。
• Methods of treating cancer with HDAC inhibitors
  申请人：——

  公开号：US20040127523A1

  公开（公告）日：2004-07-01

  The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

  本发明涉及治疗癌症的方法，例如淋巴瘤。更具体地说，本发明涉及通过给予含有HDAC抑制剂的药物组合物，例如suberoylanilide羟肟酸（SAHA），治疗弥漫性大B细胞淋巴瘤（DLBCL）的方法。这些药物组合物的口服制剂具有良好的药代动力学特性，例如高生物利用度，并且令人惊讶地在延长的时间内产生高水平的活性化合物血浓度。本发明还提供了这些药物组合物的安全、每日剂量方案，易于遵循，并在体内产生治疗有效量的HDAC抑制剂。
• CYCLOPROPYLAMINES AS LSD1 INHIBITORS
  申请人：GlaxoSmithKline Intellectual Property (No.2) Limited

  公开号：US20140371176A1

  公开（公告）日：2014-12-18

  This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.

  本发明涉及使用环丙胺衍生物来调节，特别是抑制赖氨酸特异性去甲基化酶1（LSD1）的活性。适当地，本发明涉及使用环丙胺衍生物治疗癌症。
• Combination methods of treating cancer
  申请人：Bacopoulos G. Nicholas

  公开号：US20070190022A1

  公开（公告）日：2007-08-16

  The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

  本发明涉及一种治疗癌症的方法，通过在第一次治疗过程中向需要治疗的对象给予一定量的组蛋白去乙酰化酶（HDAC）抑制剂或其药学上可接受的盐或水合物，以及在第二次治疗过程中给予一定量的抗癌剂。第一次和第二次给予的药量加起来构成治疗上有效的药量。HDAC抑制剂和抗癌剂的作用可能是加成或协同的。
• COMBINATION METHODS OF TREATING CANCER
  申请人：Bacopoulos Nicholas G.

  公开号：US20100273732A1

  公开（公告）日：2010-10-28

  The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.

  本发明涉及一种治疗需要治疗的主体癌症的方法，包括在第一治疗程序中向需要治疗的主体中给予一定量的组蛋白去乙酰化酶（HDAC）抑制剂或其药学上可接受的盐或水合物，以及在第二治疗程序中给予一定量的抗癌药物。第一和第二剂量共同组成治疗有效量。HDAC抑制剂和抗癌药物的作用可能是相加或协同的。