3-(2-butyl-1-(2-ethylaminoethyl)-1H-benzimidazol-5-yl)-N-hydroxyacrylamide | 929017-34-5

• 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: 3-(2-butyl-1-(2-ethylaminoethyl)-1H-benzimidazol-5-yl)-N-hydroxyacrylamide
• 英文别名: (E)-3-[2-butyl-1-(2-ethylamino-ethyl)-1H-benzimidazol-5-yl]-N-hydroxy-acrylamide；Pracinostat metabolite M1；(E)-3-[2-butyl-1-[2-(ethylamino)ethyl]benzimidazol-5-yl]-N-hydroxyprop-2-enamide
• CAS: 929017-34-5
• 化学式: C₁₈H₂₆N₄O₂
• 分子量: 330.43
• InChiKey: ADLOOPCDYMHBCL-CSKARUKUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  24
• 可旋转键数：
  9
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  79.2
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• Heterocyclic Compounds
  申请人：Chen Dizhong

  公开号：US20090048300A1

  公开（公告）日：2009-02-19

  The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.

  本发明涉及一种组合物，该组合物是组蛋白去乙酰化酶的抑制剂。更具体地，本发明涉及杂环化合物及其制备方法。这些化合物可能作为药物用于治疗增殖性疾病以及涉及、与或与组蛋白去乙酰化酶（HDAC）活性有关的其他疾病。
• COMBINATION OF BENZIMIDAZOLE ANTI-CANCER AGENT AND A SECOND ANTI-CANCER AGENT
  申请人：Goh Kay Lin

  公开号：US20100098691A1

  公开（公告）日：2010-04-22

  The present invention relates to a pharmaceutical composition for the treatment of cancer as well as methods of treatment of cancer that are based on the finding that certain benzimidazole based anti-cancer agents can be used in combination with a second anti-cancer agent to achieve desirable therapeutic outcomes. More specifically the present invention relates to a pharmaceutical composition including a benzimidazole based anti-cancer agent and a second anti-cancer agent. The invention also relates to methods of treatment of cancer including administration of a benzimidazole based anti-cancer agent and a second anti-cancer agent to a patient in need thereof.

  本发明涉及一种用于癌症治疗的制药组合物，以及基于发现某些基于苯并咪唑的抗癌药物可以与第二种抗癌药物结合使用以达到理想的治疗效果的癌症治疗方法。更具体地，本发明涉及一种包括基于苯并咪唑的抗癌药物和第二种抗癌药物的制药组合物。本发明还涉及癌症治疗方法，包括向需要治疗的患者施用基于苯并咪唑的抗癌药物和第二种抗癌药物。
• COMBINATION OF AZACITIDINE AND PRACINOSTAT TO TREAT MYELODYSPLASTIC SYNDROME (MDS)
  申请人：MEI Pharma, Inc.

  公开号：EP3662911A1

  公开（公告）日：2020-06-10

  Provided herein are methods of treating and sensitizing cancer comprising administering a heterocyclic compound and a DNA hypomethylating agent.

  本文提供了治疗和敏化癌症的方法，包括施用杂环化合物和 DNA 低甲基化剂。
• HETEROCYCLIC COMPOUNDS
  申请人：S*BIO Pte Ltd

  公开号：EP1937650A1

  公开（公告）日：2008-07-02
• COMBINATION THERAPIES
  申请人：MEI PHARMA, INC.

  公开号：US20150258068A1

  公开（公告）日：2015-09-17

  Provided herein are methods of treating a disease or disorder associated with dysregulation of histone deacetylase, and more specifically sensitizing and treating chemoresistant cancer comprising administering a therapeutically effective amount of a combination comprising a benzimidazole compound and a DNA hypomethylating agent and kits containing said combination. The preferred DNA hypomethylating agent used in the method is 5-azacitidine azacitidine.