CRYSTALLINE FORMS OF THE DIHYDROPYRIMIDIN DERIVATIVES Russian patent published in 2018 - IPC C07D417/04 C07D417/14 A61K31/506 A61P31/12 

FIELD: chemistry.

SUBSTANCE: invention refers to the crystalline form of the formula (I) compound, wherein the crystalline form is form B, form C, form H or form I. Crystalline form B has the X-ray powder diffraction (XRPD) model, which includes peaks that are expressed in degrees 2θ at 6.68°±0.2°, 13.39°±0.2°, 19.65°±0.2°, 20.26°±0.2°, 22.45°±0.2°, 24.80°±0.2°, 25.01°±0.2°, 26.19°±0.2°, 26.61°±0.2° and 28.79°±0.2°. Crystalline form C has the X-ray powder diffraction (XRPD) model, which includes peaks that are expressed in degrees 2θ at 5.39°±0.2°; 13.25°±0.2°; 16.00°±0.2°; 17.27°±0.2°; 21.33°±0.2°; 21.92°±0.2°; 22.53°±0.2°; 23.47°±0.2°; 26.56°±0.2°; 26.87°±0.2°; 29.41°±0.2° and 32.22°±0.2°. Crystalline form of H has the X-ray powder diffraction (XRPD) model, which includes peaks that are expressed in degrees 2θ at 7.58°±0.2°; 10.29°±0.2°; 12.00°±0.2°; 19.07°±0.2°; 19.93°±0.2°; 20.78°±0.2°; 21.33°±0.2°; 21.48°±0.2°; 24.76°±0.2°; 25.59°±0.2°; 25.82°±0.2°; 26.01°±0.2° and 26.58°±0.2°. Crystalline form is Form I, has a powder X-ray diffraction (XRPD) model including peaks expressed in degrees 2θ at 9.41°±0.2°; 17.59°±0.2°; 21.37°±0.2°; 21.72°±0.2°; 22.15°±0.2°; 22.50°±0.2°; 23.90°±0.2°; 24.59°±0.2°; 24.99°±0.2°; 26.32°±0.2°; 27.09°±0.2°; 29.68°±0.2° and 30.53°±0.2°.

EFFECT: crystalline forms of the mesylate salt of 6-[R,S]-ethyl-6-(2-bromo-4-fluorophenyl)-4-(morpholinomethyl)-2-(thiazol-2-yl)-1,6-dihydropyrimidin-5-carboxylate, which are characterized by excellent solubility, stability.

15 cl, 12 dwg, 3 tbl, 9 ex