2-amino-1-aryl-5- (3,3-dimethyl-2-oxobutylidene) -4-oxo-n- (thiazol-5-yl) -4,5-dihydro-1n-pyrrol-3-carboxamides, MANIFESTING ANTITUMOR AND ANTI-RADICAL ACTIVITY, METHOD FOR PRODUCING THEM AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS

摘要

1. A compound of general formula I wherein R is C6-C10 aryl, optionally substituted with one or more halogen atoms, or pharmaceutically acceptable salts thereof. A compound according to claim 1, wherein R is phenyl or naphthyl. 3. A compound according to claim 2, wherein phenyl is substituted with one or more halogen atoms. A compound according to claim 3, wherein phenyl is substituted with one or two bromine atoms. A compound according to claim 3, wherein phenyl is substituted with one or two chlorine atoms. A compound according to claim 1, which is a compound of formula 1a or 1b: 7. The compound according to any one of paragraphs. 1-6 in the form of a pharmaceutically acceptable salt. 8. A compound according to claim 7, wherein the pharmaceutical salt is hydrochloride, phosphate or acetate. A process for preparing a compound of general formula I wherein R is C6-C10 aryl, optionally substituted with one or more halogen atoms, or a pharmaceutically acceptable salt thereof, which comprises reacting 4-R-amino-2-tert-butyl-2,5-dihydro-5 -oxofuran-2-yl-acetate (III) and 2-cyano-N- (thiazol-2-yl) acetamide in the presence of triethylamine, according to the following scheme: 10. The method according to claim 9, wherein 4R-amino-2-tert-butyl-2,5-dihydro-5-oxofuran-2-yl acetate (III) and 2-cyano-N- (thiazol-2-yl) acetamide are taken in equimolar amount. 11. The method of claim 9 or 10, wherein the triethylamine is taken in an amount of 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-yl acetate. 12. The method of claim 9 or 10, wherein the reaction is carried out in a benzene environment. The method of claim 12, wherein the resulting product of the compound of formula I precipitates. The method of claim 12, wherein the precipitate is recrystallized. The method of claim 14, wherein benzene or ethanol is used as the solvent for recrystallization. Pharmaceutical composition