POLYMORPHIC MODIFICATIONS OF N-[(3-FLUORO-4-METHOXYPYRIDINE-2-YL)METHYL]-3-(METHOXYMETHYL)-1-({ 4-[(2-OXOPYRIDINE-1-YL)METHYL]PHENYL} METHYL)PYRAZOLE-4-CARBOXAMIDE AND THEIR SALTS Russian patent published in 2021 - IPC C07D401/10 A61K31/4439 A61P27/02 

FIELD: medicine.

SUBSTANCE: invention relates to a solid form of N-[(3-fluoro-4-methoxypyridine-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridine-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, which shows at least following characteristic peaks of X-ray powder diffraction (Kα-radiation Cu expressed in degrees 2θ) approximately at 11.2, 12.5, 13.2, 14.5 and 16.3, and to a solid form of sulfate of N-[(3-fluoro-4-methoxypyridine-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridine-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide, which shows at least following characteristic peaks of X-ray powder diffraction (Kα-radiation Cu expressed in degrees 2θ) approximately at 5.1, 7.5, 12.0, 15.2 and 17.9. the invention also relates to a pharmaceutical composition intended for the treatment of diseases or pathological conditions mediated with plasma kallikrein based on the specified forms.

EFFECT: technical result is that new solid forms of N-[(3-fluoro-4-methoxypyridine-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridine-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and pharmaceutical composition based on them are obtained, which can be used in medicine for the treatment of diseases or pathological conditions mediated with plasma kallikrein.

25 cl, 47 dwg, 21 tbl, 27 ex