Crystalline form of lorlatinib free base
AssigneePfizer Inc.
InventorsKlimentina Dimitrova Pencheva, Melissa J. Birch
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Abstract
This invention relates to a crystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h] [2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
Claims20
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, having a powder X-ray diffraction (PXRD) pattern comprising peaks at 2θ values of:
- 9.6, 10.1 and 16.2 °2θ±0.2 °2θ.
A crystalline form of lorlatinib free base, having a Raman spectrum comprising wavenumber (cm−1) values of:
- 2229 and 2240 cm−1±2 cm−1.
A crystalline form of lorlatinib free base, having a 13C solid state NMR spectrum comprising two or more resonance (ppm) values of:
- 39.1 and 142.1 ppm±0.2 ppm.
A crystalline form of lorlatinib free base, having a 19F solid state NMR spectrum comprising a resonance (ppm) value selected from the group consisting of:
- −108.2 and −115.2 ppm±0.2 ppm.
Dependencies are inferred from the claim text.