4-AMINOPYRIDINES AND A PHARMACEUTICAL COMPOSITION Russian patent published in 1999 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to new 4-aminopyridines of the general formula (I): where R¹ means groups R⁶-SO₂-NR⁷-, R⁶-NR⁷-SO₂-, R⁶-SO₂-O-, R⁶-O-SO₂-; R² means hydrogen or halogen atom, cyano-, alkyl-, alkoxyl- or halogenalkyl-group; X means oxygen or sulfur atom or NH-group; R³ and R⁴ are similar or distinct and mean hydrogen atoms or alkyl-groups; R⁵ means hydrogen atom, alkyl- or aralkyl-group; R⁶ means alkyl-, cycloalkyl-, aryl-, heteroaryl-, aralkyl- or heteroarylalkyl-group; aryl- or heteroaryl-groups can be substituted mono- or multiplied with nitro-group, halogen, hydroxyl, amino-group, carboxyl, halogenalkyl, alkoxycarbonyl, aralkoxycarbonyl, alkyl, cycloalkyl, alkoxyl, alkylamino-group or one or some groups -Y--CO₂R⁸, -O-Y--CO₂R⁸; alkyl groups can be mono- or multiplied substituted with halogen; R⁷ means hydrogen, alkyl, cycloalkyl or alkenyl residues and these residues can be mono- or multiplied substituted with halogen, hydroxyl, alkoxyl, amino-group or alkylcarbonyl, or means cyanoalkyl, heteroaryl, aryl or aralkyl residues; aryl or heteroaryl residues can be mono- or multiplies substituted with carboxy-group, or means residue -Y--CO₂R⁸ or -Y--CONR⁸R⁹; Y means linear or branched alkylene chain; R⁸ and R⁹ are similar or distinct and mean hydrogen or alkyl-groups that can be mono- or multiplied substituted with hydroxyl, alkoxyl, amino-group or carboxyl, or R⁸ and R⁹ together with N-atom with which they are bound form saturated ring that can has additionally oxygen, sulfur or nitrogen atom, and their physiologically acceptable salts also. 4-Aminopyridine of the formula (I) according p. 1 where R¹ means groups R⁶-SO₂-O-, R⁶-O-SO₂-; R⁶-NR⁷-SO₂-; R² means hydrogen or halogen atom, alkyl, alkoxyl or trifluoromethyl-group; X means oxygen atom or NH-group; R³ and R⁴ are similar or distinct and mean hydrogen atom or alkyl-groups; R⁵ means hydrogen, R⁶ means alkyl, cycloalkyl, aryl, heteroaryl or aralkyl groups and aryl or heteroaryl groups can be mono- or multiplied substituted with halogen, alkyl, trifluoromethyl, alkoxyl, hydroxyl, carboxyl, hydroxyalkyl, carboxyalkyl, alkoxycarbonyl, amino-group, alkylamino-group; R⁷ means hydrogen, alkyl, cycloalkyl, alkenyl, carboxyalkyl, heteroaryl, alkylhydroxycarbonylalkyl, aryl or aralkyl residues; aryl residue can be mono- or multiplied substituted with alkoxyl, carboxyl, carboxyalkyl, alkoxycarbonyl groups, alkylcarbonyl-amino-group or formylamino-group, and their physiologically acceptable salts and a pharmaceutical composition based on components said. Indicated compounds show biological activity and capability to inhibit platelets. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 14 cl, 1 tbl, 128 ex