CRYSTAL (6S,9AS)-N-BENZYL-8-({6-[3-(4-ETHYLPIPERAZIN-1-YL)AZETIDIN-1-YL]PYRIDIN-2-YL}METHYL)-6-(2-FLUORINE-4-HYDROXYBENZYL)-4,7-DIOXO-2-(PROP-2-EN-1-YL)HEXAHYDRO-2H-PYRAZINO[2,1-C][1,2,4]TRIAZINE-1(6H)-CARBOXAMIDE Russian patent published in 2020 - IPC C07D487/04 A61K31/53 A61P35/00 

Abstract RU 2723551 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to crystalline (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazin-1(6H)-carboxamide, which is characterized by diffraction peaks at diffraction angle (2θ±0.2°) 5.8°, 6.4°, 8.0°, 10.1°, 12.8°, 14.2°, 16.0°, 18.9°, 19.7°and 23.1° according to measurement by means of powder X-ray diffraction. Invention also relates to said compound having different characteristics, and to a pharmaceutical composition.

EFFECT: obtaining a novel crystalline form (6S,9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl}methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxo-2-(prop-2-en-1-yl)hexahydro-2H-pyrazino[2,1-c][1,2,4]triazin-1(6H)-carboxamide, having activity with respect to Wnt path modulation.

5 cl, 1 tbl, 21 ex, 6 dwg

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RU 2 723 551 C2

Authors

Kushida Ikuo

Ito Yoko

Dates

2020-06-16Published

2016-06-21Filed