POLYMORPHS OF 2-(4-(2-(1-ISOPROPYL-3-METHYL-1H-1,2,4-TRIAZOL-5-YL)-5,6-DIHYDROBENZOFIMIDAZO1,2-D1,4OXAZEPIN-9-YL)-1H-PYRAZOL-1-YL)-2-METHYLPROPANAMIDE, METHODS OF PRODUCTION AND PHARMACEUTICAL USES THEREOF

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a process for the preparation of the crystalline polymorph of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), comprising heating the suspension in isoamyl alcohol and cooling the mixture, whereby a crystalline polymorph is formed, characterized by an X-ray powder diffraction pattern, having characteristic peaks expressed in 2-theta degrees at approximately 9.40, 10.84, 16.72, 18.7 and 26.60.;EFFECT: method for preparing the crystalline polymorph of 2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, which has hygroscopicity, physical stability, chemical stability in the solid state.;1 cl, 21 dwg, 15 tbl, 13 ex