4-(ARYLAMINOMETHYLENE)-2,4-DIHYDRO-3-PYRAZOLONES

The invention relates to 5-pyrazolinone deriva- tives of the general formula I: (I) in which R1 is benzyl; alkoxybenzyl with 1-3 C atoms in the alkyl moiety; phenyl; phenyl which is substituted once to three times by amino, halogen, NO2, CN, acyl, AO-, HSO3, CO2H, A-O-CO-, A-CO-NH-, A-CO-NA-, carbamoyl, N-alkylcarbamoyl, N, N- dialkylcarbamoyl (with 1-6 C atoms in the alkyl moiety), A-O-CO-NH-, A-O-CO-NA-, SO2NR4R5 ( R4 and R5 can be H or alkyl with 1-6 C atoms, or NR4R5 is a 5- or 6-membered ring, optionally with other heteroatoms such as N, S, O, which may be substituted by A), A-CO-NH-SO2-, A-CO-NA-SO2-, A-SO2-NH-, A-So2-NA-, (A-SO2-)2N-, tetrazolyl or phospho; or pyridyl R2 is alkyl with 1-5 C atoms, alkoxycarbonylalkyl, hydroxyalkyl, hydroxycarbonylalkyl R3 is H, straight-chain or branched alkyl with 1-5 C atoms, straight-chain or branched alkoxy with 1-5 C atoms, fluorine- or chlorine-substituted alkyl, aminoalkanoyl, aminoalkyl, carbamoyl, SO2NR4R5 (R4 and R5 can be H or alkyl with 1-6 C atoms, or NR4R5 is a 5- or 6-membered ring, optionally with other heteroatoms such N, S, O, which may be substituted by A), A is straight or branched alkyl with 1-6 C atoms or straight or branched flourine- or chlorine substituted alkyl with 1-6 C atoms, and the physiologically acceptable salts thereof. Part of the invention also comprises processes for the preparation of these compounds, but in particular their use as selective inhibitors of cGMP- specific phosphodiesterase (cGMP PDE) and thus as pharmaceutically active compounds.