| abstract |
The 4- (arylaminomethylene) -2,4-dihydropyrazol-3-one derivative of formula (I) wherein R 1 is benzyl, C 1-3 alkoxybenzyl, phenyl optionally substituted with 1, 2 or 3 amino, halogen, NO 2, CN, AO-, carboxyl, sulfonyl, AO-CO-, A-CO-NH-, A-CO-NA-, carbamoyl, N-C 1-6 alkylcarbamoyl, N, N-diC 1-6 alkylcarbamoyl, AO-CO-NH-, AO -CO-NA-, A-SO 2 -, SO 2 NR 4 R 5, wherein R 4 and R 5 are H or C 1-6 alkyl, or NR 4 R 5 is a 5- or 6-membered ring optionally having 1 to 2 heteroatoms such as N, S, or O substituted with optionally A A-CO-NH-SO2, A-CO-NA-SO2-, A-SO2-NH-, A-SO2-NA, (A-SO2) 2N, tetrazolyl and phosphonyl; or is pyridyl, R 2 C 1-5 alkyl, C 1-4 alkoxycarbonylC 1-4 alkyl, hydroxyC 1-4 alkyl, hydroxycarbonylC 1-4 alkyl, R 3 C 1-5 alkyl, C 1-5 alkoxy, F or Cl substituted alkyl, A C 1-6 alkyl, F or Cl substituted C 1-6 alkyl , and salts thereof, are useful as selective inhibitors of cGMP specific phosphodiesterases for the preparation of pharmaceutical compositions, in particular for the treatment of cardiovascular diseases and cardiac insufficiency. |