Diaryl macrocyclic polymorphs and methods for preparing the same
A crystalline polymorph form of the compound addresses issues of crystallinity and solubility, enhancing stability and efficacy in treating cancers and other diseases mediated by tyrosine kinases.
Patent Information
- Application Number
- CN202110623105.2
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- Priority Date
- 2015-09-15
- Filing Date
- 2016-07-05
- Publication Date
- 2024-12-31
- Estimated Expiration
- 2036-07-05
AI Technical Summary
Existing forms of the compound (7S,13R)-11-fluoro-7,13-dimethyl-6,7,13,14-tetrahydro-1,15-ethylene-bridged pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecene-4(5H)-one lack improved crystallinity, solubility, and reduced hygroscopicity while maintaining chemical and enantiomeric stability for effective treatment of diseases mediated by tyrosine kinases.
Development of a crystalline polymorph form of the compound with specific powder X-ray diffraction patterns, including peaks at 9.4±0.1, 16.1±0.1, 16.5±0.1, 18.8±0.1, 21.2±0.1, 22.8±0.1, and 27.4±0.1 degrees, and its use in pharmaceutical compositions for targeted cancer therapy.
The crystalline polymorph form exhibits enhanced stability and solubility, providing effective treatment of cancers and other diseases mediated by ALK, ROS1, TRK, JAK2, SRC, and FAK kinases, with improved therapeutic outcomes.
Smart Images
Figure CN113354653B_ABST