abstract |
The present invention relates to benzoylpyridazines of formula I wherein R1 and R2 are independently H, OH, OR4, SR4, SOR4, SO2R4 or Hal, wherein R1 and R2 together may also represent -O-CH2-O, R3 is Hal, OH , OA, NO2, NH2, NHA1, NA1A2, CN, COOH, COOA1, CONH2, CONHA1, CONA1A2, NHCOA1, NHSO2A1, NHCOOA1, (a), (b), (c), (d), (e), ( f) or (g), R4 is A1 or C3-C7-cycloalkyl, C4-C8-alkylene-cycloalkyl or C2-C8-alkenyl, A1 and A2 are independently C1-C12-alkyl optionally substituted with 1-5 carbon atoms; fluorine and / or chlorine or hydroxy, wherein A1 and A2 may alternatively be cycloalkyl or cycloalkylene, having 3-7 ring members, wherein one or more methylene groups are -S-, -O-, -NH-, -NA1-, -NHCOA1- or -NCOOA1-, X is H or Hal, Hal is fluorine, chlorine, bromine or iodine, and Q is C 1 -C 15 alkyl or alkenyl wherein 1-5 methylene is replaced by -O-, -S-, -SO2-, -CH (Hal) -, -C (Hal) 2-, -CHA1-, -CA1A2-, - NH- or -NA1-. The compounds of the invention have PDE IV isozyme inhibitory activity. The invention also relates to the preparation of the compounds and to pharmaceutical compositions containing them. SHE |