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    • 6. 发明专利
    • Purin-6-one-derivatives
    • AU2004228360A1
    • 2004-10-21
    • AU2004228360
    • 2004-03-02
    • ALTANA PHARMA AG
    • QUINTINI GIANLUCABAER THOMASTENOR HERMANNHATZELMANN ARMIN
    • A61K31/522A61P9/00C07D473/30
    • The compounds of a certain formula (I) in which e.g. R2, R3, R4 and R5 have the meanings as given below are novel effective PDE2 inhibitors. R2 is hydrogen, 1-4C-alkyl, 1-hydroxy-2-4C-alkyl, 1-4C-alkylcarbonyl or 1-(acetyloxy)-2-4C-alkyl and R3 is Arylbutyl, Heteroarylbutyl, Arylpropyl, Heteroarylpropyl, Arylethyl or Heteroarylethyl; wherein Aryl is phenyl, naphthalenyl or indanyl, each of which optionally substituted up to three times identically or differently by halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, Heteroaryl is pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, quinazolinyl, quinoxalinyl, cinnolinyl, quinolyl, isoquinolyl, naphthyridinyl, phthalazinyl, indolyl, isoindolyl, indazolyl, purinyl, pteridinyl, benzofuranyl, benzoxazolyl, benzothiazolyl, benzimidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, imidazolyl, pyrrolyl, pyrazolyl, furanyl or thiophenyl, each of which optionally substituted up to three times identically or differently by halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy or 1-4C-alkoxycarbonyl, R4 is 1-4C-alkoxy which is completely or predominantly substituted by fluorine and R5 is halogen, hydroxyl, nitro, trifluoromethyl, carboxyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, 1-4C-alkoxycarbonyl, amino, mono- or di-1-4C-alkylamino, aminocarbonyl, mono- or di-1-4C-alkylaminocarbonyl, 1-4C-alkylcarbonylamino, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonylamino, phenylcarbonylamino, phenylcarbonylamino substituted in the phenyl moiety by R6 and/or R7, benzylcarbonylamino, benzylcarbonylamino substituted in the phenyl moiety by R8 and/or R9, phenylsulfonylamino, phenylsulfonylamino substituted in the phenyl moiety by R10 and/or R11, benzylsulfonylamino or benzylsulfonylamino substituted in the phenyl moiety by R12 and/or R13.