3-[1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one

• 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: 3-[1-[[4-(2-phenylthieno[3,4-b]pyrazin-3-yl)phenyl]methyl]piperidin-4-yl]-1H-benzimidazol-2-one
• 化学式: C₃₁H₂₇N₅OS
• 分子量: 517.6
• InChiKey: UCOJJLRFYUCWKS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  38
• 可旋转键数：
  5
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.19
• 拓扑面积：
  89.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• Inhibitors of akt activity
  申请人：Duggan E Mark

  公开号：US20050288294A1

  公开（公告）日：2005-12-29

  The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

  本发明涉及含有与取代吡嗪分子融合的五元杂环的化合物，该化合物可抑制丝氨酸/苏氨酸蛋白激酶 Akt 的活性。本发明进一步涉及含有本发明化合物的化疗组合物和通过施用本发明化合物治疗癌症的方法。
• EP1558586A4
  申请人：——

  公开号：EP1558586A4

  公开（公告）日：2007-06-27
• INHIBITORS OF AKT ACTIVITY
  申请人：Merck & Co., Inc.

  公开号：EP1558586A2

  公开（公告）日：2005-08-03
• USE OF DIANHYDROGALACTITOL OR DERIVATIVES OR ANALOGS THEREOF FOR TREATMENT OF PEDIATRIC CENTRAL NERVOUS SYSTEM MALIGNANCIES
  申请人：DelMar Pharmaceuticals, Inc.

  公开号：US20180071244A1

  公开（公告）日：2018-03-15

  The use of dianhydrogalactitol provides a novel therapeutic modality for the treatment of malignancies of the central nervous system in pediatric patients, including glioblastoma multiforme (GBM) high grade glioma, and medulloblastoma. Dianhydrogalactitol acts as an alkylating agent on DNA that creates N 7 methylation and that can induce double-stranded breaks in DNA. Dianhydrogalactitol is effective in suppressing the growth of cancer stem cells and is active against tumors that are refractory to temozolomide, cisplatin, and tyrosine kinase inhibitors; the drug acts independently of the MGMT repair mechanism. Dianhydrogalactitol can be used together with other anti-neoplastic agents (e.g. cisplatin) and can possess additive or super-additive effects.
• US7399764B2
  申请人：——

  公开号：US7399764B2

  公开（公告）日：2008-07-15