Crystalline forms of N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl)pyrazin-2-yl]amino}ethyl]phenyl}-5-methylpyridine-3-carboxamide and related products and methods
AssigneeGB002, Inc.
InventorsMarcus Schestopol, Beili Zhang, David Paisner, Nicole White, Esmir Gunic
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Abstract
Crystalline forms of N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl)pyrazin-2-yl]amino}ethyl]-phenyl}-5-methylpyridine-3-carboxamide are provided. Pharmaceutical compositions and dosage forms containing the crystal forms are also provided, including related methods for modulating kinases generally, and specifically to treatment of PAH.
Claims57
A solid crystalline form of N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl) pyrazin-2-yl]amino}ethyl]phenyl}-5-methylpyridine-3-carboxamide, wherein the crystalline form is Form A characterized by an XRPD pattern having peaks at 5.5, 7.8, 11.0, 12.3 and 15.6±0.2 degrees 2-theta, or wherein the crystalline form is Form B characterized by an XRPD pattern having peaks at 5.2, 6.1, 7.6, 11.5 and 12.3±0.2 degrees 2-theta or a mixture thereof.
A method for preparing Form B of N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl) pyrazin-2-yl] amino}ethyl] phenyl}-5-methylpyridine-3-carboxamide comprising slurrying Form A of N-{3-[(1S)-1-{[6-(3,4-dimethoxyphenyl) pyrazin-2-yl]amino} ethyl]phenyl}-5-methylpyridine-3-carboxamide in ethyl acetate and holding its temperature from about 10° C. to about 45° C. for a period of time from about 1 minute to 90 hours, wherein Form A is characterized by an XRPD pattern having peaks at 5.5, 7.8, 11.0, 12.3 and 15.6±0.2 degrees 2-theta, and Form B is characterized by an XRPD pattern having peaks at 5.2, 6.1, 7.6, 11.5 and 12.3±0.2 degrees 2-theta.
Dependencies are inferred from the claim text.