CRYSTALLINE FORMS OF (S)-4-AMINO-N-(1-(4-CHLOROPHENYL)-3-HYDROXYPROPYL)-1-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)PIPERIDINE-4-CARBOXAMIDE Russian patent published in 2018 - IPC C07D487/04 A61K31/519 A61K9/20 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of B (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (compound (I), exhibiting inhibitory activity against PKB (protein kinase B). Compound can be used to treat cancer or to prepare a medicament for treatment PKB activity mediated, in particular, breast cancer, prostate cancer or stomach cancer. Invention also relates to a pharmaceutical composition useful for the treatment of cancer mediated by PKB activity, containing compound (I) in crystalline form B in a therapeutically effective amount, optionally together with microcrystalline cellulose, mannitol, croscarmellose sodium and magnesium stearate. Crystalline form B has an X-ray powder diffraction pattern with at least three characteristic peaks at a 2-theta of about 12.3, 15.0 and 19.2°, in particular, an X-ray powder diffraction pattern with characteristic peaks at 2-theta of about 10.0, 12.3, 15.0, 17.1, 19.2 and 24.4°.

EFFECT: crystalline form B is thermodynamically more stable than other crystalline forms, and is more preferable in terms of the shelf life of the product and minimising the variability in absorption.

9 cl, 8 dwg, 6 tbl, 3 ex