Polymorphs of n-[(6-cyano-2-fluoro)-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide as kallikrein inhibitors
AssigneeKalvista Pharmaceuticals Limited
InventorsHaydn BEATON, Jonathan Yates BOXHALL, David Malcolm CROWE
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Abstract
The invention provides new polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, pharmaceutical compositions containing them and their use in therapy.
Claims41
A crystalline form of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, that is:
- (a) crystalline Form 1, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 9.0±0.3, 14.3±0.3, 18.1±0.3, 19.6±0.3 and 24.0±0.3;
- or
- (b) crystalline Form 2, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 8.3±0.3, 10.5±0.3, 16.6±0.3, 19.6±0.3, and 23.8±0.3, or
- (c) crystalline Form 3, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 7.3±0.3, 10.2±0.3, 12.4±0.3, 12.9±0.3 and 18.1±0.3;
- or
- (d) crystalline Form 4, which exhibits at least X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at 9.0±0.3, 14.3±0.3, 15.0±0.3, 18.1±0.3, and 19.5±0.3.
A crystalline form 1 of N-[(6-cyano-2-fluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, which exhibits an endothermic peak in its DSC thermograph at 149±3° C.
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Dependencies are inferred from the claim text.