| abstract |
FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to 4-(arylaminomethylene)-2,4-dihydropyrazole-3-ones of the general formula (I) where R 1 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-, SO 2 NR 4 R 5 ; (R 4 and R 5 can mean H or alkyl with 1-6 carbon atoms, or NR 4 R 5 means 5- or 6-membered ring with other heteroatoms, for example, N or O that can be substituted with A), A-CO-NH-SO 2 -, A- CO-NA-SO 2 -, (A-SO 2 -) 2 N-, tetrazolyl, phenyl; or pyridyl; R 2 means alkyl with 1-5 carbon atoms, ethoxycarbonylmethyl, hydroxycarbonylmethyl; R 3 means unbranched or branched alkyl with 1-5 carbon atoms, unbranched or branched alkoxy-group with 1-5 carbon atoms or CF 3 ; A means unbranched or branched alkyl with 1-6 carbon atoms or CF 3 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 |