6-[(2,2,2-trifluoroethyl)amino]pyrido[4,3-c]-1,6-naphthyridin-1(2H)-one | 1058125-81-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: 6-[(2,2,2-trifluoroethyl)amino]pyrido[4,3-c]-1,6-naphthyridin-1(2H)-one
• 英文别名: 6-(2,2,2-trifluoroethylamino)-2H-pyrido[4,3-c][1,6]naphthyridin-1-one
• CAS: 1058125-81-7
• 化学式: C₁₃H₉F₃N₄O
• 分子量: 294.236
• InChiKey: FVEDKTZRULIYGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  66.9
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1
  申请人：Siu Tony

  公开号：US20100160309A1

  公开（公告）日：2010-06-24

  The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.

  本发明提供了抑制JAK2酪氨酸激酶和/或PDK1的化合物。本发明还提供了包含这些抑制化合物的组合物，并通过将该化合物给予需要治疗或预防骨髓增生性疾病或癌症的患者来抑制JAK2酪氨酸激酶活性和/或PDK1激酶抑制活性的方法。
• 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.
• US8329722B2
  申请人：——

  公开号：US8329722B2

  公开（公告）日：2012-12-11
• [EN] INHIBITORS OF JANUS KINASES AND/OR 3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASE-1<br/>[FR] INHIBITEURS DE JANUS KINASES ET/OU PROTÉINE KINASE-1 DÉPENDANT DE LA 3-PHOSPHOINOSITIDE
  申请人：MERCK & CO INC

  公开号：WO2008112217A1

  公开（公告）日：2008-09-18

  [EN] The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDKl. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDKl kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.
  [FR] L'invention concerne des composés qui inhibent la tyrosine kinase JAK2 et/ou PDK1. L'invention concerne également des compositions comprenant de tels composés inhibiteurs, et des procédés d'inhibition de l'activité de la tyrosine kinase JAK2 et/ou de l'activité d'inhibition de la kinase PDK1 par l'administration du composé à un patient qui nécessite des soins ou la prévention de troubles associés à une myéloprolifération ou un cancer.