2-{6-[2-(difluoromethyl)benzimidazol-1-yl]-2-morpholin-4-ylpurin-9-yl}ethan-1-ol | 1204411-58-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 2-{6-[2-(difluoromethyl)benzimidazol-1-yl]-2-morpholin-4-ylpurin-9-yl}ethan-1-ol
• 英文别名: 2-[6-[2-(Difluoromethyl)benzimidazol-1-yl]-2-morpholin-4-ylpurin-9-yl]ethanol
• CAS: 1204411-58-4
• 化学式: C₁₉H₁₉F₂N₇O₂
• 分子量: 415.402
• InChiKey: QFOCMNUYDYTUPQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.37
• 拓扑面积：
  94.1
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• Use of Inhibitors of the Activity or Function of PI3K
  申请人：NOVARTIS AG

  公开号：US20150342951A1

  公开（公告）日：2015-12-03

  The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.

  该发明涉及PI3K抑制剂的新用途，其中所述抑制剂对PI3K同工酶δ具有抑制作用，用于治疗患有疟疾、利什曼病、锥虫病、弓形虫病和/或神经囊虫病等疾病或紊乱的受试者的免疫病理学，通过对感染受试者的TLR9的功能抑制。
• P13K ISOFORM SELECTIVE INHIBITORS
  申请人：Liang Congxin

  公开号：US20110130395A1

  公开（公告）日：2011-06-02

  2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.

  2-吗啡啉-4-基-9H-嘌呤和5-吗啡啉-4-基-3H-[1,2,3]三唑[4,5-d]嘧啶衍生物，特别是那些被6-杂环芳基取代的衍生物，是意外的PI3K酶亚型选择性抑制剂，具有良好的药物特性，并可用于治疗与异常PI3K活性相关的疾病，如癌症、免疫障碍、心血管疾病、病毒感染、炎症、代谢/内分泌障碍和神经系统疾病。
• Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
  申请人：Race Oncology Ltd.

  公开号：US10548876B2

  公开（公告）日：2020-02-04

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to bisantrene or derivatives, analogs, or prodrugs thereof.

  本发明描述了通过提高单一疗法的疗效或减少副作用来改善以前因治疗效果不理想而受到限制的治疗剂的疗效的方法和组合物。这些方法和组合物尤其适用于双蒽或其衍生物、类似物或原药。
• Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
  申请人：Race Oncology Ltd.

  公开号：US11147800B2

  公开（公告）日：2021-10-19

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to bisantrene or derivatives, analogs, or prodrugs thereof.

  本发明描述了通过提高单一疗法的疗效或减少副作用来改善以前因治疗效果不理想而受到限制的治疗剂的疗效的方法和组合物。这些方法和组合物尤其适用于双蒽或其衍生物、类似物或原药。
• PI3K ISOFORM SELECTIVE INHIBITORS
  申请人：Xcovery Holding Company LLC

  公开号：EP2307414A2

  公开（公告）日：2011-04-13