Chromone mTOR inhibitor as well as pharmaceutical composition and application thereof

• Main Authors: ZHANG JIQUAN, LU JIANGRONG, SUN QIWEN, CHEN RUI, ZHANG NANA
• Format: Patent
• Language: Chinese; English
• Published: 01.08.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention discloses a chromone mTOR inhibitor and a pharmaceutical composition and application thereof, and the chromone mTOR inhibitor comprises a substituted compound with a general formula (I), a stereoisomer, a hydrate or a pharmaceutically acceptable salt thereof, the chromone mTOR inhibitor and the pharmaceutical composition containing the chromone mTOR inhibitor provided by the invention can be used for inhibiting mTOR kinase, have excellent inhibitory activity and selectivity on mTOR kinase, are novel in structure and remarkable in anti-tumor activity, can be potentially applied to drugs for prevention, treatment and adjuvant therapy of related tumors, and have broad application prospects. The active anti-proliferative disease effect is realized. 本发明公开了一种色原酮类mTOR抑制剂及其药物组合物和应用，其中，所述色原酮类mTOR抑制剂包括具有通式(Ⅰ)的取代化合物，其立体异构体，水合物或药学上可接受的盐，所述通式(Ⅰ)结构如下：本发明所提供一种色原酮类mTOR抑制剂、包含其的药物组合物能够用于抑制mTOR激酶，对mTOR激酶有优异的抑制活性和选择性，结构新颖、抗肿瘤活性显著，可潜在用于相关肿瘤的预防、治疗、辅助治疗药物，具有积极的抗增殖性疾病效果。