BENZOXAZOLE DERIVATIVE CRYSTAL Russian patent published in 2023 - IPC C07D487/08 A61K31/4995 

FIELD: biotechnology.

SUBSTANCE: invention relates to crystals of 1-((2-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluor-2-methylpropane-2-ol characterized by the formula (1). A crystal of type I of 1-((2-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluor-2-methylpropane-2-ol has, on X-ray powder diffraction pattern, characteristic peaks with diffraction angles (2θ±0.2°) equal to 7.7°, 14.5°, 17.0°, 18.9°, 19.4°, 23.3°, and 25.7°. A crystal of type II of 1-((2-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluor-2-methylpropane-2-ol has, on X-ray powder diffraction pattern, characteristic peaks with diffraction angles (2θ±0.2°) equal to 7.8°, 14.7°, 15.7°, 19.3°, and 25.0°. The invention also relates to a pharmaceutical composition having an inhibitory effect on phosphodiesterase (PDE) 4, including a crystal of 1-((2-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluor-2-methylpropane-2-ol characterized by the formula (1) as an active principle.

EFFECT: crystal forms of 1-((2-(3,6-diazabicyclo[3.1.1]heptane-3-yl)-7-(thiazole-2-yl)benzo[d]oxazole-4-yl)oxy)-1,1-difluor-2-methylpropane-2-ol, having a stability property.

6 cl, 3 dwg, 2 tbl, 4 ex