7-Piperazin-1-ylpyrazolo[1,5-a]pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: 7-Piperazin-1-ylpyrazolo[1,5-a]pyrimidine
• 英文别名: 7-piperazin-1-ylpyrazolo[1,5-a]pyrimidine
• 化学式: C₁₀H₁₃N₅
• 分子量: 203.24
• InChiKey: UOONJLDISXKOQC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  45.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• AKT PROTEIN KINASE INHIBITORS
  申请人：Array BioPharma, Inc.

  公开号：US20140148436A1

  公开（公告）日：2014-05-29

  The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

  本发明提供了化合物，包括已分离的对映体、非对映异构体、溶剂化物和药学上可接受的盐，其化学式为A-L-CR，其中CR是一个环状核心基团，L是一个连接基团，A如本文所定义。本发明还提供了使用该化合物作为AKT蛋白激酶抑制剂和用于治疗高增殖性疾病，如癌症的方法。
• Methods and compositions for KRAS inhibitors
  申请人：The Board of Regents, The University of Texas System

  公开号：US11141418B1

  公开（公告）日：2021-10-12

  In one aspect, the disclosure relates to compounds that are inhibitors of KRAS, and the disclosed compounds are allosteric inhibitors of KRAS which render them extremely useful for therapeutic intervention in a variety of disorders and diseases in which inhibition of DHODH can be clinically useful, e.g., cancer. In various aspects, the disclosed compounds are substituted 7-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine analogs. In further aspects, the disclosed compounds can be used in methods of treating a cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

  在一个方面，本公开涉及的化合物是KRAS的抑制剂，所公开的化合物是KRAS的异构抑制剂，这使得它们在各种疾病的治疗干预中极为有用，在这些疾病中，抑制DHODH在临床上是有用的，例如癌症。在各个方面，所公开的化合物是取代的 7-(哌嗪-1-基)吡唑并[1,5-a]嘧啶类似物。在进一步的方面，所公开的化合物可用于治疗癌症的方法中。本摘要旨在作为在特定技术领域进行搜索的扫描工具，并非对本公开内容的限制。
• METHODS AND COMPOSITIONS FOR KRAS INHIBITORS
  申请人：The Board of Regents of the University of Texas System

  公开号：US20210401845A1

  公开（公告）日：2021-12-30

  In one aspect, the disclosure relates to compounds that are inhibitors of KRAS, and the disclosed compounds are allosteric inhibitors of KRAS which render them extremely useful for therapeutic intervention in a variety of disorders and diseases in which inhibition of DHODH can be clinically useful, e.g., cancer. In various aspects, the disclosed compounds are substituted 7-(piperazin-1-yl)pyrazolo[1,5-a]pyrimidine analogs. In further aspects, the disclosed compounds can be used in methods of treating a cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
• US8680114B2
  申请人：——

  公开号：US8680114B2

  公开（公告）日：2014-03-25