Preparation and use of pyrimidinothiopyranone pan-kras mutant protein inhibitors
By developing pyrimidinoid compounds, the problem of the lack of effective KRAS mutant protein inhibitors in the prior art, especially KRAS G12C mutations, has been solved, enabling effective treatment of KRAS-related cancers.
CN122145488APending Publication Date: 2026-06-05YAOYA TECH SHANGHAI CO LTD
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- YAOYA TECH SHANGHAI CO LTD
- Filing Date
- 2024-12-04
- Publication Date
- 2026-06-05
AI Technical Summary
Technical Problem
The lack of effective inhibitors for KRAS mutant proteins in existing technologies, especially the insufficient treatment methods for cancers with KRAS G12C mutations, leads to poor cancer treatment outcomes.
Method used
A novel pyrimidothiazolinone compound was developed to inhibit KRAS mutant proteins, including the KRAS G12C mutation, through specific structural design. Stereoisomers of the compound, pharmaceutically acceptable salts, and prodrugs are provided for the preparation of pharmaceutical compositions.
Benefits of technology
Effective inhibition of KRAS mutant proteins, especially KRAS G12C mutations, provides new cancer treatment options and improves the therapeutic effect on KRAS-related cancers.
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Figure CN122145488A_ABST
Abstract
The compound has good activity of inhibiting tumor growth and good safety. The application discloses preparation and application of a Kras inhibitor, and particularly provides a compound shown in formula (I) and a pharmaceutically acceptable salt of the compound, a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt, and application of the compound or the pharmaceutically acceptable salt in treating or preventing a Kras kinase related disease, particularly a tumor, which is a kind of heterocyclic compound, and a preparation method of the pharmaceutical composition of the compound or the pharmaceutically acceptable salt is disclosed. Wherein each substituent group of the general formula (I) is the same as defined in the specification.
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