PYRIMIDINE COMPOUND CRYSTAL Russian patent published in 2024 - IPC C07D487/04 A61K31/519 A61P35/00 

FIELD: chemistry; pharmaceutics.

SUBSTANCE: invention relates to a crystal having peaks at diffraction angles (2θ±0.2°) selected from 5.5°, 6.8°, 9.3°, 13.4°, 15.3°, 16.3°, 18.5°, 19.8°, 22.0° and 24.5° on powder X-ray diffraction spectrum, which is a crystal of type II 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide with fumaric acid, where the molar ratio is 1:1. Invention relates to a pharmaceutical composition having HER2 inhibitory activity, containing an effective amount of a crystal according to the invention. Invention also relates to an anticancer agent for treating a tumour associated with HER2, containing a crystal according to the invention.

EFFECT: crystal of 7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide with fumaric acid as a HER2 inhibitor, which has stability, good oral absorption.

6 cl, 32 dwg, 19 tbl, 27 ex