6-(4-((1s,3s)-1-amino-3-hydroxycyclobutyl)phenyl)-5-phenyl-3-(2,2,2-trifluoroethyl)furo[2,3-d]pyrimidin-4(3H)-one | 1459229-90-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃
• 英文名称: 6-(4-((1s,3s)-1-amino-3-hydroxycyclobutyl)phenyl)-5-phenyl-3-(2,2,2-trifluoroethyl)furo[2,3-d]pyrimidin-4(3H)-one
• CAS: 1459229-90-3
• 化学式: C₂₄H₂₀F₃N₃O₃
• 分子量: 455.436
• InChiKey: HBVKQOVBBGTPQW-LBEPJEHYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.19
• 重原子数：
  33.0
• 可旋转键数：
  4.0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  94.28
• 氢给体数：
  2.0
• 氢受体数：
  6.0

文献信息

• [EN] 6- (4- (1 -AMINO- 3 -HYDROXYCYCLOBUTYL) PHENYL) - 5 - PHENYL (FURO, THIENO OR PYRROLO) [2, 3-D] PYRIMIDIN- 4 - ONE DERIVATIVES FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE 6-(4-(1-AMINO-3-HYDROXYCYCLOBUTYL)PHÉNYL)-5-PHÉNYL(FURO, THIÉNO OU PYRROLO)[2,3-D]PYRIMIDIN-4-ONE POUR LE TRAITEMENT D'UN CANCER
  申请人：ALMAC DISCOVERY LTD

  公开号：WO2013140189A1

  公开（公告）日：2013-09-26

  The present invention relates to compounds of Formula (I) that are useful as inhibitors of the activity of one or more isoforms of the serine / threonine kinase AKT. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

  本发明涉及一种化合物，其化学式为（I），可用作抑制丝氨酸/苏氨酸激酶AKT的一个或多个亚型的活性的抑制剂。本发明还涉及包括这些化合物的药物组合物，以及使用这些化合物治疗癌症的方法和治疗癌症的方法。
• PHARMACEUTICAL COMPOUNDS
  申请人：Almac Discovery Limited

  公开号：US20150045377A1

  公开（公告）日：2015-02-12

  The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of the serine/threonine kinase, AKT. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.

  本发明涉及一种化合物，其作为丝氨酸/苏氨酸激酶AKT的一个或多个亚型的活性抑制剂是有用的。本发明还涉及包含这些化合物的药物组合物以及使用这些化合物治疗癌症和治疗癌症的方法。
• 6-(4-(1-AMINO-3-HYDROXYCYCLOBUTYL)PHENYL)-5-PHENYL(FURO, THIENO OR PYRROLO)[2,3-D]PYRIMIDIN-4-ONE DERIVATIVES FOR THE TREATMENT OF CANCER
  申请人：Almac Discovery Limited

  公开号：EP2838901B1

  公开（公告）日：2016-11-02
• 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.
• US9156853B2
  申请人：——

  公开号：US9156853B2

  公开（公告）日：2015-10-13