METHOD FOR PRODUCING AN AMORPHOUS FORM OF N-[2-(DIETHYLAMINO)ETHYL]-5-[(Z)-(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOLE-3-YLIDENE)METHYL]-2,4-DIMETHYL-1H-PYRROL-3-CARBOXAMIDE MALATE, PRODUCT AND APPLICATION THEREOF FOR TREATING ONCOLOGICAL AND IMMUNOLOGICAL DISEASES Russian patent published in 2022 - IPC C07D403/06 A61K31/404 A61P35/00 

Abstract RU 2774382 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a method for producing an amorphous form of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrol-3-carboxamide malate. The method includes the following stages: (a) fusing crystalline N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide malate, D-fructose and urea in a mass ratio of 1:2:3, at a temperature of 60°C while stirring; (b) adding water to the resulting melt; (c) stirring the resulting mixture; (d) filtering the precipitate; (e) preparing a suspension of precipitate in water; (f) stirring the resulting suspension at a temperature of 20°C; (g) filtering the precipitate; (h) washing the precipitate with water on a filter; (i) drying the precipitate until a constant mass under vacuum at a temperature of 40°C.

EFFECT: production of an amorphous form of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indole-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide malate, containing a reduced amount of impurities.

2 cl, 8 dwg, 8 tbl, 12 ex

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RU 2 774 382 C1

Authors

Torchinov Georgij Yurevich

Dates

2022-06-20Published

2021-03-19Filed