SOLID FORMS OF GYRASE INHIBITOR (R)-1-ETHYL-3-[6-FLUORO-5-[2-(1-HYDROXY-1-METHYL-ETHYL) PYRIMIDIN-5-YL]-7-(TETRAHYDROFURAN-2-YL)-1H-BENZIMIDAZOL-2-YL] UREA Russian patent published in 2017 - IPC C07D413/14 A61K31/506 A61P31/04 

FIELD: chemistry.

SUBSTANCE: compounds can be used for controlling, treating or reducing the progression, severity or effects of nosocomial or non-nosocomial bacterial infection. Compound solid forms of formula (I), represent a crystalline Form I or amorphous Form III. Crystalline Form I is characterized by X-ray powder diffractogram (XRPD), comprising at least three positions of closely located peaks (2θ±0.2 in degrees) when measured using Cu K_α radiation, selected from the group consisting of 9.3, 11.7, 12.1, 12.4, 14.5, 15.9, 16.3, 16.6, 18.5, 19.4, 21.5 22.3, 22.8, 23.8, 24.5, 25.7, 28.1, 28.4, 30.3 and 33.4 in the case when XRPD is collected in the angular range of two-theta (2θ) from about 5 to about 38 degrees. The amorphous form III is characterized by X-ray powder diffraction (XRPD), obtained using Cu K_α radiation, which has a diffuse halogen peak in the absence of a clearly distinguishable diffraction peak. A method for producing crystalline Form I comprises suspending of the free base solid material in a solvent system containing alcohol and ether, and extraction of the solid material. A process for producing amorphous Form III comprises lyophilization, spray drying, drum drying or impulse conversion drying of the compound 6-fluoro-benzimidazolyl-urea solution.

EFFECT: improved properties of compounds.

13 cl, 10 dwg, 9 tbl, 2 ex