STABLE CRYSTALLINE FORM OF TYPIRACYL HYDROCHLORIDE AND METHOD FOR ITS CRYSTALLIZATION Russian patent published in 2018 - IPC C07D403/06 A61K31/506 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a new crystalline form of hydrochloride of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)pyrimidinedione of the formula (I)

indicated below. The crystalline form of the compound of the formula (1) shows characteristic peaks of powder X-ray diffraction at 11.6°, 17.2°, 17.8°, 23.3°, 27.1° and 29.3° angles, as the diffraction angle (2θ±0.1°) in anhydrous form and an endothermic peak determined by thermogravimetry and differential thermal analysis at a temperature of about 262 °C. The crystal shows, following crystal data in the analysis of single crystals: crystal system: monoclinic system, spatial group: P2_l/n (No. 14), the crystal lattice constant: a=11.6006 (9) , b=10.3106 (11) , c=10.3036 (10) , α=90°, β=101.951 (7)°, γ=90° and unit lattice cell volume: 1205.7 (2) .

EFFECT: compound has the properties of a thymidine phosphorylase inhibitor and can be used as an antitumor agent.

13 cl, 3 dwg, 3 tbl, 7 ex