5- and 6-azaindole compounds for inhibition of bcr-abl tyrosine kinases
Compounds targeting specific Bcr-Abl mutations and fusion transcripts enhance the efficacy and tolerability of Bcr-Abl TKI treatment for CML by overcoming resistance and reducing side effects.
Patent Information
- Application Number
- TW114139084
- Authority / Receiving Office
- TW · TW
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-10-16
- Filing Date
- 2025-10-09
- Publication Date
- 2026-08-01
AI Technical Summary
Current Bcr-Abl tyrosine kinase inhibitors (TKIs) face challenges with resistance mutations, particularly the T315I mutation, leading to reduced efficacy and significant side effects, necessitating improved selectivity and tolerability for Philadelphia-positive neoplasias like CML.
Development of compounds and compositions that selectively inhibit Bcr-Abl tyrosine kinase, targeting specific mutations such as A337T, F359C, P465S, V299L, F359I, P465S, or S348L, and Bcr-Abl fusion transcripts other than e13a2 (b2a2) or e14a2 (b3a2), administered without fasting, to enhance therapeutic outcomes.
The compounds provide enhanced selectivity and efficacy against Bcr-Abl tyrosine kinase, overcoming resistance mutations and reducing side effects, thereby improving treatment compliance and patient quality of life.