3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-thieno[3,2-d]pyrimidin-4-one | 1029280-04-3

• 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: 3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-thieno[3,2-d]pyrimidin-4-one
• 英文别名: 3-phenyl-2-[1-(7H-purin-6-ylamino)ethyl]thieno[3,2-d]pyrimidin-4-one
• CAS: 1029280-04-3
• 化学式: C₁₉H₁₅N₇OS
• 分子量: 389.44
• InChiKey: OMURHYASVBANRY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  127
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-(1-aminoethyl)-3-phenyl-3H-thieno[3,2-d]pyrimidin-4-one 、 6-溴嘌呤 在 N,N-二异丙基乙胺 作用下， 反应 96.0h， 生成 3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-thieno[3,2-d]pyrimidin-4-one
  参考文献：
  名称：

  WO2008/64018

  摘要：

  公开号：

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。
• THIENOPYRIMIDIONES FOR TREATMENT OF INFLAMMATORY DISORDERS AND CANCERS
  申请人：White Stephen L.

  公开号：US20100216820A1

  公开（公告）日：2010-08-26

  The current invention provides compounds of formula (1): wherein: one of Q 1 , Q 2 and Q 3 is S, and the other of two of Q 1 , Q 2 and Q 3 are —CR 1 —, which are inhibitors of PI3K-delta. These compounds are useful for treatment of conditions mediated by PI3K-delta, such as hematopoietic cancers, immune disorders, and bone resorption disorders. The invention further provides pharmaceutical compositions comprising a compound of formula (1) and methods of using these compounds and compositions to treat conditions mediated by PI3K-delta.

  当前的发明提供了式（1）的化合物：其中：Q1、Q2和Q3中的一个是S，而Q1、Q2和Q3中的另外两个是—CR1—，这些化合物是PI3K-delta的抑制剂。这些化合物对于治疗由PI3K-delta介导的疾病，如造血系统癌症、免疫系统疾病和骨吸收障碍等，是有用的。该发明还提供了包含式（1）化合物的制药组合物以及使用这些化合物和组合物治疗由PI3K-delta介导的疾病的方法。
• TREATMENT OF LIVER DISORDERS WITH P13K INHIBITORS
  申请人：Ulrich Roger G.

  公开号：US20120178767A1

  公开（公告）日：2012-07-12

  The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.

  本发明提供了通过给予抑制PD K同工酶特别是δ同工酶的化合物来治疗某些肝脏疾病的方法。它还提供了用于这些方法的特定化合物和识别适合接受这些治疗的受试者的方法。
• Thienopyrimidinones for treatment of inflammatory disorders and cancers
  申请人：Eli Lilly & Co.

  公开号：EP2441768A1

  公开（公告）日：2012-04-18

  The current invention provides compounds of formula (I); wherein one of Q1, Q2 and Q3 is S, and the other of two of Q1, Q2 and Q3 are -CR1-, which are inhibitors of P13K-delta. These compounds are useful for treatment of conditions mediated by P13K-delta, such as hematopoietic cancers, immune disorders, and bone resorption disorders. The invention further provides pharmaceutical compositions comprising a compound of formula (I) and methods of using these compounds and compositions to treat conditions mediated by P13K-delta.

  本发明提供了式(I)化合物；其中Q1、Q2和Q3中的一个是S，Q1、Q2和Q3中的两个的另一个是-CR1-，它们是P13K-delta的抑制剂。这些化合物可用于治疗由 P13K-delta 介导的疾病，如造血癌症、免疫紊乱和骨吸收紊乱。本发明进一步提供了包含式（I）化合物的药物组合物，以及使用这些化合物和组合物治疗由 P13K-delta 介导的疾病的方法。
• THIENOPYRIMIDINONES FOR TREATMENT OF INFLAMMATORY DISORDERS AND CANCERS
  申请人：Eli Lilly & Co.

  公开号：EP2097422A1

  公开（公告）日：2009-09-09