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    PYRIDAZINONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS
    1.
    发明公开
    PYRIDAZINONE DERIVATIVES AND THEIR USE AS PDE4 INHIBITORS 审中-公开
    哒嗪酮衍生物及其作为PDE4抑制剂的用途

    公开(公告)号：EP1716123A1

    公开(公告)日：2006-11-02

    申请号：EP05707902.2

    申请日：2005-02-01

    申请人： Altana Pharma AG

    发明人： MENGE, Wiro M. P. B. ,  STERK, Geert Jan ,  HATZELMANN, Armin ,  BARSIG, Johannes ,  MARX, Degenhard ,  KLEY, Hans-Peter ,  CHRISTIAANS, Johannes A. M.

    IPC分类号： C07D237/04 ,  C07D401/12 ,  C07D403/12 ,  A61K31/50 ,  A61K31/501 ,  A61P11/08

    CPC分类号： C07D237/04 ,  C07D401/12 ,  C07D403/12

    摘要： Compounds of formula (1) are effective PDE4 inhibitors in which R1 is 1-4C-alkyl and R2 is 1-4C-alkyl, R3 represents a phenyl dervative of formulae (a) or (b) wherein R4 is 1-4C-alkoxy or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R5 is 1-8C-alkoxy, 3-7C-cycloalkoxy, 3-7C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R6 is 1-4C-alkoxy, 3-5C-cycloalkoxy, 3-5C-cycloalkylmethoxy, or 1-4C-alkoxy which is completely or predominantly substituted by fluorine, R7 is 1-4C-alkyl and R8 is hydrogen or 1-4C-alkyl, or wherein R7 and R8 together and with inclusion of the two carbon atoms, to which they are bonded, form a spiro-linked 5-, 6- or 7-membered hydrocarbon ring, optionally interrupted by an oxygen or sulphur atom and R9 is hydroxyl, halogen, nitro, cyano, 1-4C-alkyl, trifluoromethyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, hydroxycarbonyl, hydroxycarbonyl-1-4C-alkyl, 1-4C-alkoxycarbonyl, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonyl, benzyloxy, -C(O)R10, -S(O)2-R11, -O(CH2)n-C(O)-R12, -(CH2), -C(O)-R26 or -N(R29)R30.