2-AMINO-1-ARYL-5-(3,3-DIMETHYL-2-OXOBUTYLIDENE)-4-OXO-N-(THIAZOL-5-YL)-4,5-DIHYDRO-1H-PYRROLE-3-CARBOXAMIDES, EXHIBITING ANTITUMOUR AND ANTIRADICAL ACTIVITY, SYNTHESIS METHOD THEREOF AND PHARMACEUTICAL COMPOSITION BASED THEREON Russian patent published in 2016 - IPC C07D417/12 A61K31/427 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula I, where R represents a C6-C10 aryl, optionally substituted with one or more halogen atoms, or its pharmaceutically acceptable salts. Compounds of general formula I are obtained by reacting 4-R-amino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate (III) and 2-cyano-N-(thiazol-2-yl)acetamide in the presence of triethylamine. Initial reagents 4R-amino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate (III) and 2-cyano-N-(thiazol-2-yl)acetamide are taken in equimolar amount. Triethylamine is taken in an amount from equimolar to two-fold excess with respect to 2-cyano-N-(thiazol-2-yl)acetamide and 4R-2-tert-butyl-2,5-dihydro-5-oxofuran-2-ylacetate. Reaction takes place in a medium of benzene. Invention also relates to a pharmaceutical composition having antitumour and antiradical activity, containing as an active ingredient a compound of general formula I or its pharmaceutically acceptable salt in a pharmaceutically active amount and a pharmaceutically acceptable filler. Compounds of formula I are intended for producing drug preparations for treating oncological diseases.

EFFECT: 2-amino-1-aryl-5-(3,3-dimethyl-2-oxobutylidene)-4-oxo-N-(thiazol-5-yl)-4,5-dihydro-1H-pyrrol-3-carboxamides, exhibiting antitumour and antiradical activity.

17 cl, 2 tbl, 2 dwg, 5 ex