6,8-dibromo-3-methylimidazo[1,2-a]pyrazine | 1289082-40-1

• 英文名称: 6,8-dibromo-3-methylimidazo[1,2-a]pyrazine
• CAS: 1289082-40-1
• 化学式: C₇H₅Br₂N₃
• 分子量: 290.945
• InChiKey: YMUNPZUNSSNOAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(4-吗啉基)苯胺 、 6,8-dibromo-3-methylimidazo[1,2-a]pyrazine 在 N,N-二异丙基乙胺 作用下， 以 N-甲基吡咯烷酮 为溶剂， 反应 0.5h， 生成
  参考文献：
  名称：

  Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells

  摘要：

  Co-crystallisation of the imidazo[1,2-a]pyrazine derivative 15 (3-chloro-N-(4-morpholinophenyl)-6-(pyridin-3-yl)imidazo[1,2-a]pyrazin-8-amine) with Aurora-A provided an insight into the interactions of this class of compound with Aurora kinases. This led to the design and synthesis of potent Aurora-A inhibitors demonstrating up to 70-fold selectivity in cell-based Aurora kinase pharmacodynamic biomarker assays.

  DOI：

  10.1016/j.bmcl.2010.08.091

文献信息

• [EN] CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED BY TERTIARY HYDROXY GROUPS AS PI3K-GAMMA INHIBITORS<br/>[FR] DÉRIVÉS D'IMIDAZOLE CONDENSÉS, SUBSTITUÉS PAR DES GROUPES HYDROXY TERTIAIRES, UTILISÉS COMME INHIBITEURS DE PI3K-GAMMA
  申请人：INCYTE CORP

  公开号：WO2019079469A1

  公开（公告）日：2019-04-25

  This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-y which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

  这种应用涉及到式(I)的化合物或其药用可接受的盐，这些化合物是PI3K-y的抑制剂，对于治疗自身免疫疾病、癌症、心血管疾病和神经退行性疾病等疾病是有用的。
• [EN] BICYCLIC COMPOUNDS<br/>[FR] COMPOSÉS BICYCLIQUES
  申请人：KALYRA PHARMACEUTICALS INC

  公开号：WO2016183094A1

  公开（公告）日：2016-11-17

  Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

  本文披露了含氮的双环化合物，以及使用本文描述的一个或多个化合物改善和/或治疗本文描述的癌症的药物组合物和方法。
• CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED BY TERTIARY HYDROXY GROUPS AS PI3K-GAMMA INHIBITORS
  申请人：Incyte Corporation

  公开号：EP4006034A1

  公开（公告）日：2022-06-01

  This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which are inhibitors of PI3K-y which are useful for the treatment of disorders such as autoimmune diseases, cancer, cardiovascular diseases, and neurodegenerative diseases.

  本申请涉及式 (I) 化合物： 或其药学上可接受的盐，它们是 PI3K-y 的抑制剂，可用于治疗自身免疫性疾病、癌症、心血管疾病和神经退行性疾病等疾病。
• BICYCLIC COMPOUNDS
  申请人：KALYRA PHARMACEUTICALS, INC.

  公开号：US20180201614A1

  公开（公告）日：2018-07-19

  Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.