NEW SALT OF CONDENSED PYRIMIDINE COMPOUND AND CRYSTAL THEREOF Russian patent published in 2019 - IPC C07D487/04 C07C57/15 A61K31/519 A61P35/00 A61P19/02 A61P37/08 C07C51/41 

FIELD: chemistry.

SUBSTANCE: invention relates to novel mono- or hemisalt (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(benzo[d]oxazol-2-yl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide with fumaric acid. Hemifumarate (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(benzo[d]oxazol-2-yl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide can be a crystal having diffraction angle (2θ±0.1°) with peaks selected from 4.5°, 5.8°, 11.2°, 12.1°, 12.4°, 13.4°, 16.6°, 17.3°, 18.2°, 20.2°, 26.4° and 27.1°, in the powder X-ray diffraction spectrum and the peak temperature on the differential scanning calorimetry (DSC) curve with the endothermic peak in range from 197 °C to 199 °C. Monofumarate (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(benzo[d]oxazol-2-yl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide can be a crystal having diffraction angle (2θ±0.1°) with at least two or more peaks selected from 7.2°, 12.4°, 14.4°, 15.0°, 15.6°, 19.0°, 22.3°, 22.6°, 23.4°, 25.5°, 25.9° and 27.6°, in the X-ray powder diffraction spectrum and having a peak temperature on the differential scanning calorimetry curve (DSC) with an endothermic peak in range of 219 °C to 224 °C.

EFFECT: salts have the properties of a selective BTK inhibitor and can be used as an active ingredient for an antitumour agent, particularly against a haematological tumor or as an active ingredient of a preventive and/or therapeutic agent for allergic rhinitis, pollen allergy, atopic dermatitis, rheumatoid arthritis, systemic lupus erythematosus, contact dermatitis or uveitis; salts do not have channel-type hydrate properties and possess stable absorption properties.

32 cl, 11 dwg, 9 tbl, 15 ex