小分子ATM抑制剂作为潜在的癌症治疗:专利审查 (2003年至今)
Yan A Ivanenkov1,2, Alexander S Malyshev1,2, Victor A Terentiev1,2
1P. Hertsen Moscow Oncology Research Institute, Moscow, Russian Federation.
Expert opinion on therapeutic patents
|December 27, 2024
概括
ATAXIA-telangiectasia突变 (ATM) 激酶抑制剂是有前途的抗癌药物. 专利分析显示,imidazo[4,5-c]quinolinone支架是有效的,目前正在进行的临床试验正在探索它们与破坏DNA的疗法的结合.
科学领域:
- 在瘤学瘤学.
- 药用化学 医学化学
- 生物化学 生物化学
背景情况:
- ATAXIA telangiectasia突变 (ATM) 激酶对于DNA双链断裂 (DSB) 修复信号传递至关重要.
- 目前正在研究ATM抑制剂用于癌症治疗,特别是与破坏DNA的药物结合使用.
研究的目的:
- 为自2003年以来的ATM激酶小分子抑制剂提供专利和专利申请的全面审查.
- 分析专利ATM抑制剂的结构性质,活性和有效性.
- 讨论这些抑制剂的临床试验进展和发展史.
主要方法:
- 使用SciFinder,Cortellis药物发现情报和Espacenet进行了系统的文献搜索.
- 44项专利记录被确定并分析了结构特征,活性和有效性.
- 还审查了临床试验数据和发展史.
主要成果:
- 大多数已识别的ATM抑制剂都具有imidazo[4,5-c]quinolinone支架或其生物异构体.
- 这些支架显示出有利的ATM抑制活性和选择性.
- 临床试验正在评估与放射治疗和PARP抑制剂的组合.
结论:
- ATM 激酶抑制剂,特别是具有 imidazo[4,5-c]quinolinone 结构的激酶抑制剂,在癌症治疗中显示出显著的前景.
- 涉及ATM抑制剂的组合疗法正在通过临床试验取得进展.
- 这些新的治疗策略预计将很快进入制药市场.
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