CRYSTALLINE FORMS OF FREE BASE Russian patent published in 2018 - IPC C07D487/14 A61K31/519 A61K31/57 

FIELD: chemistry.

SUBSTANCE: invention relates to the crystalline form of the free base (6aR, 9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine-4(2H)-one (Compound A), as shown by the following chemical formula: . Specified crystalline form shows a powder x-ray diffraction pattern, including at least five peaks with values of interatomic distance d, selected from the group consisting of 14.34, 11.65, 10.83, 5.82, 4.87, 4.64, 4.48, 4.23, 3.93 and 3.21 Å, where the powder x-ray diffractogram is measured on the diffractometer when using a copper anode, for example, at a wavelength of alpha1 1.5406 Å and a wavelength of alpha2 1.5444 Å. Also proposed are a number of crystalline forms of compound A, a method for producing a salt of compound A, a method for producing a crystalline monophosphate salt of Compound A, a crystalline salt of Compound A in the form of a hemifumarate salt or in the form of a non-solvated benzoate, a method for preparing a crystalline free base of compound A in solvated form and a method for producing a crystalline monophosphate salt of compound A.

EFFECT: crystalline free base form of compound A is more stable than the known compound and also contains less impurities.

43 cl, 18 dwg, 20 tbl, 16 ex