NEW CRYSTALS OF URACIL COMPOUND Russian patent published in 2019 - IPC C07D239/54 A61K31/505 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a novel crystalline form of (R)-N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulphanilamide of general formula (1).

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which inhibits deoxyuridine triphosphate and potentiates anticancer effects of anti-cancer agents. New crystalline form of compound (I), denoted as crystalline form II, has at least five or more diffraction peaks (2θ±0.2°) selected from 7.3°, 11.8°, 14.5°, 14.8°, 16.8°, 17.5°, 18.6°, 19.5°, 20.4°, 23.9°, 24.4°, 25.7°, 26.8° and 31.5° on the powder X-ray diffraction spectrum; endothermic peak at 108 °C±5 °C at differential scanning calorimetry; and the following crystalline data obtained by analyzing the monocrystal: crystalline system - rhombic system; spatial group: P2₁2₁2₁ (No. 19); lattice constant: a = 9.3998(5) Å; b = 10.3585(5) Å; c = 23.5111(10) Å; unit cell volume: 2289.22(19) ų; Z value: 4. Disclosed crystalline form II has higher stability compared to the other crystalline form during storage, which is confirmed by the indices given in Tables 2 and 3, and simultaneously has higher oral adsorption capacity (see Table 1).

EFFECT: compound can be used for the pharmaceutical composition as an active ingredient and is suitable as an anticancer effect intensifier.

5 cl, 6 dwg, 3 tbl, 3 ex