Heterocyclic compounds as PI3kα inhibitors

Heterocyclic compounds selectively inhibit PI3Ka to overcome the limitations of current PI3K inhibitors, enhancing tumor treatment efficacy while minimizing side effects.

WO2026128684A1PCT designated stage Publication Date: 2026-06-18PIKAVATION THERAPEUTICS INC

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
PIKAVATION THERAPEUTICS INC
Filing Date
2025-12-11
Publication Date
2026-06-18

AI Technical Summary

Technical Problem

Current PI3K inhibitors face challenges in achieving sufficient target inhibition in tumors while avoiding toxicity in cancer patients due to their lack of isoform selectivity, leading to side effects such as hyperglycemia and rash, diarrhea, myelosuppression, and transaminitis.

Method used

Development of heterocyclic compounds that selectively inhibit PI3Ka, reducing the risk of toxicity by targeting mutant PI3Ka without affecting wild-type PI3Ka, thereby minimizing side effects like hyperglycemia and hyperinsulinemia.

🎯Benefits of technology

The heterocyclic compounds provide enhanced selectivity for mutant PI3Ka, increasing the therapeutic window and allowing effective tumor inhibition with reduced adverse effects.

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Abstract

The present application provides heterocyclic compounds of formula I that modulate the activity of the PI3Ka, which are useful in the treatment of various diseases, including cancer.
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