Crystalline form of lorlatinib free base hydrate
AssigneePfizer Inc.
InventorsPaul Bowles, Peter Robert Rose
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Abstract
This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base hydrate (Form 24). This invention also relates to pharmaceutical compositions comprising Form 24, and to methods of using Form 24 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
Claims13
A crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile (lorlatinib) free base hydrate, having a powder X-ray diffraction (PXRD) pattern comprising peaks at 2θ values of:
- 8.8, 9.7, 17.6 and 18.8 °2θ±0.2 °2θ.
A crystalline form of lorlatinib free base hydrate, having a 13C solid state NMR spectrum comprising two or more resonance (ppm) values of:
- 40.2, 41.2 and 136.2 ppm±0.2 ppm.
A crystalline form of lorlatinib free base hydrate, having a 19F solid state NMR spectrum comprising a resonance (ppm) value of:
- −104.0 ppm±0.2 ppm.
Dependencies are inferred from the claim text.