2-Methyl-7-(4-methylpiperazin-1-yl)-3,5-diphenylpyrazolo[1,5-a]pyrimidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 2-Methyl-7-(4-methylpiperazin-1-yl)-3,5-diphenylpyrazolo[1,5-a]pyrimidine
• 化学式: C₂₄H₂₅N₅
• mdl: MFCD06776075
• 分子量: 383.5
• InChiKey: NQQIOUQMTMUKLZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  29
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  36.7
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• [EN] COMPOSITIONS AND METHODS FOR SUBSTITUTED 7-(PIPERAZIN-1-YL)PYRAZOLO[1,5-A]PYRIMIDINE ANALOGS AS INHIBITORS OF KRAS<br/>[FR] COMPOSITIONS ET PROCÉDÉS POUR DES ANALOGUES DE 7-(PIPÉRAZIN-1-YL)PYRAZOLO [1,5-A]PYRIMIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE KRAS
  申请人：UNIV TEXAS

  公开号：WO2021119343A1

  公开（公告）日：2021-06-17

  In one aspect, the disclosure relates to compounds useful as inhibitors of mutant KRAS proteins, methods of making the same, pharmaceutical compositions comprising the same, and methods of treating cancers associated with mutated forms of KRAS using the same. 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，本公开涉及作为突变KRAS蛋白抑制剂有用的化合物，制备这些化合物的方法，包含这些化合物的药物组合物，以及使用这些化合物治疗与突变KRAS形式相关的癌症的方法。本摘要旨在作为在特定领域进行搜索的扫描工具，不打算限制本公开内容。
• 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.