Therapeutically active compositions and application methods thereof
By developing compounds of structural formula I to inhibit the activity of mutant IDH1, the problem of mutant IDH1 in cancer is solved, the level of R(-)-2-hydroxyglutarate is reduced, and the progression of cancer is slowed down.
Patent Information
- Application Number
- CN201110172169.1
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2011-06-17
- Publication Date
- 2012-12-19
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
Mutations in the IDH1 gene in certain cancer cells result in an enzyme with a novel ability to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate, thereby promoting cancer formation and progression. , it is difficult to effectively inhibit the activity of this mutant IDH1 with existing technology.
A class of compounds of structural formula I has been developed, which inhibit mutant IDH1 with novel α-hydroxyl activity, especially R132X mutant IDH1, and are used to prepare pharmaceutical compositions for the treatment of cancers characterized by the presence of mutant IDH1.
Effectively inhibits the activity of mutant IDH1 and reduces the level of R(-)-2-hydroxyglutarate in the body, thereby slowing or preventing the development and progression of cancer, providing a potential treatment.