THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION Russian patent published in 2002 - IPC

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to 4-(arylaminomethylene)-2,4-dihydropyrazole-3-ones of the general formula (I) where R¹ means benzyl, alkoxybenzyl with 1-3 carbon atoms in alkyl moiety that can be unsubstituted or substituted one-three-fold by amino-group, acyl-group, halogen atom, nitro-group, CN, AO-, carboxyl-group, carbamoyl group, N-alkylcarbamoyl, N,N-dialkylcarbamoyl (with 1-6 carbon atoms in alkyl moiety), A-CO-NH-, A-O-CO-NH-, A-O-CO-NA-, SO₂NR⁴R⁵; (R⁴ and R⁵ can mean H or alkyl with 1-6 carbon atoms, or NR⁴R⁵ means 5- or 6-membered ring with other heteroatoms, for example, N or O that can be substituted with A), A-CO-NH-SO₂-, A- CO-NA-SO₂-, (A-SO₂-)₂N-, tetrazolyl, phenyl; or pyridyl; R² means alkyl with 1-5 carbon atoms, ethoxycarbonylmethyl, hydroxycarbonylmethyl; R³ means unbranched or branched alkyl with 1-5 carbon atoms, unbranched or branched alkoxy-group with 1-5 carbon atoms or CF₃; A means unbranched or branched alkyl with 1-6 carbon atoms or CF₃ and to their salts also. Compounds are selective inhibitors of cGMP-specific phosphodiesterase. Invention relates to also a method of synthesis of these compounds and to pharmaceutical composition inhibiting activity of cGMP- specific phosphodiesterase that contains the compound of the formula (I) as an active component or one of its salts. Invention relates to also 4-4,5-dihydro-3-methyl-5-oxo-4-[2-(2-propinyloxy)anilinomethylene]-1H-pyrazole-1-yl- benzoic acid. EFFECT: improved method of synthesis, valuable biochemical property. 6 cl, 1 tbl, 72 ex