madrasin | 374913-63-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: madrasin
• 英文别名: 2-((7-methoxy-4-methylquinazolin-2-yl)amino)-5,6-dimethylpyrimidin-4(3H)-one；Madrasin；2-[(7-methoxy-4-methylquinazolin-2-yl)amino]-4,5-dimethyl-1H-pyrimidin-6-one
• CAS: 374913-63-0
• 化学式: C₁₆H₁₇N₅O₂
• 分子量: 311.343
• InChiKey: QQJIYKXTEMDJFM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  88.5
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  madrasin 在 三溴化硼 作用下， 以 1,2-二氯乙烷 为溶剂， 反应 20.0h， 以42%的产率得到2-((7-hydroxy-4-methylquinazolin-2-yl)amino)-5,6-dimethylpyrimidin-4(3H)-one
  参考文献：
  名称：

  WO2020099650A5

  摘要：

  公开号：

  WO2020099650A5
• 作为产物：
  描述：

  7-甲氧基-2,2,4-三甲基-1,2-二氢喹啉 在 盐酸 、 碳酸氢钠 作用下， 以 1,4-二氧六环 、 二甲基亚砜 为溶剂， 反应 96.5h， 生成 madrasin
  参考文献：
  名称：

  WO2020099650A5

  摘要：

  公开号：

  WO2020099650A5

文献信息

• PIM kinase inhibitors in combination with RNA splicing modulators/inhibitors for treatment of cancers
  申请人：UNIVERSITY OF MARYLAND, BALTIMORE COUNTY

  公开号：US10842785B2

  公开（公告）日：2020-11-24

  The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes of mRNA splicing in combination with a compound that modulates/inhibits activity of an RNA splicing factor protein. Further, changes in splicing of mRNAs and phosphorylation of RNA splicing factors can be used as biomarkers for patient responsiveness to anti-PIM treatment and also suggest effective combinatorial therapies, including synergistic combination.

  本发明提供了一种治疗癌症和/或减少癌细胞增殖的方法，该方法包括向需要这种治疗的受试者施用一种组合物，该组合物包含一种PIM激酶抑制剂，该PIM激酶抑制剂与一种调节/抑制RNA剪接因子蛋白活性的化合物相结合，可显示出mRNA剪接的变化。此外，mRNA 的剪接变化和 RNA 剪接因子的磷酸化可用作患者对抗 PIM 治疗反应性的生物标志物，还可提示有效的组合疗法，包括协同组合疗法。
• PIM KINASE INHIBITORS IN COMBINATION WITH RNA SPLICING MODULATORS/INHIBITORS FOR TREATMENT OF CANCERS
  申请人：University of Maryland, Baltimore County

  公开号：EP3432886B1

  公开（公告）日：2021-06-02
• [EN] PIM KINASE INHIBITORS IN COMBINATION WITH RNA SPLICING MODULATORS/INHIBITORS FOR TREATMENT OF CANCERS<br/>[FR] INHIBITEURS DE KINASE PIM EN COMBINAISON AVEC DES MODULATEURS/INHIBITEURS D'ÉPISSAGE D'ARN POUR LE TRAITEMENT DE CANCERS
  申请人：UNIV MARYLAND

  公开号：WO2017165495A1

  公开（公告）日：2017-09-28

  The present invention provides for a method of treating cancer and/or reducing proliferation of cancer cells, the method comprising administering to a subject in need of such treatment a composition comprising a PIM kinase inhibitor that exhibits changes of mRNA splicing in combination with a compound that modulates/inhibits activity of an RNA splicing factor protein. Further, changes in splicing of mRNAs and phosphorylation of RNA splicing factors can be used as biomarkers for patient responsiveness to anti-PIM treatment and also suggest effective combinatorial therapies, including synergistic combination.
• [EN] MADRASIN-DERIVATIVE COMPOUNDS, COMPOSITION AND USES THEREOF FOR TREATING CANCER<br/>[FR] COMPOSÉS DÉRIVÉS DE MADRASINE, COMPOSITION ET LEURS UTILISATIONS POUR TRAITER LE CANCER
  申请人：ROUSSY INST GUSTAVE

  公开号：WO2020099650A1

  公开（公告）日：2020-05-22

  The present invention relates to the fields of medicine and in particular cancer treatment. The invention more specifically relates to new compounds which are typically for use as a medicament. In particular, the invention relates to the use of these new compounds for increasing the presentation, typically the production and presentation, of Pioneer Translation Products (PTPs)-derived antigens by cells, in particular cancer cells, or changing the immunopeptidome, in a subject, and inducing or stimulating an immune response in the subject. The present disclosure also relates to uses of such compounds, in particular to prepare a pharmaceutical composition and/or to allow or improve the efficiency of a therapy in a subject in need thereof. The invention also discloses methods for treating a disease, in particular cancer, for preventing or treating cancer metastasis and/or cancer recurrence, in a subject. The present invention in addition provides kits suitable for preparing a composition according to the present invention and/or for implementing the herein described methods.
• WO2020099650A5
  申请人：——

  公开号：WO2020099650A5

  公开（公告）日：2022-11-24