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    • 1. 发明申请
    • PURIN-6-ONE-DERIVATIVES
    • 嘌呤-6-酮衍生物
    • WO2004089953A1
    • 2004-10-21
    • PCT/EP2004/050234
    • 2004-03-02
    • ALTANA PHARMA AGTENOR, HermannBAER, ThomasHATZELMANN, Armin
    • TENOR, HermannBAER, ThomasHATZELMANN, ArminQUINTINI, Gianluca
    • C07D473/30
    • C07D473/30
    • 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.
    • 某些式(I)的化合物,其中例如 R2,R3,R4和R5具有以下给出的含义是新型有效的PDE2抑制剂。 R2是氢,1-4C-烷基,1-羟基-24C-烷基,1-4C-烷基羰基或1-(乙酰氧基)-2-4C-烷基,R3是芳基丁基,异芳基丁基,芳基丙基,异芳基丙基,芳基乙基或 Heteroarylethyl; 其中芳基是苯基,萘基或茚满基,其中的每一个任选被卤素,羟基,硝基,三氟甲基,羧基,1-4C-烷基,1-4C-烷氧基或1-4C-烷氧基羰基相同或不同地取代三次, 杂芳基是吡啶基,吡嗪基,哒嗪基,嘧啶基,喹唑啉基,喹喔啉基,噌啉基,喹啉基,异喹啉基,萘啶基,喹喔啉基,吲哚基,异吲哚基,吲唑基,嘌呤基,蝶啶基,苯并呋喃基,苯并恶唑基,苯并噻唑基,苯并咪唑基,恶唑基,异恶唑基,噻唑基,异噻唑基, 咪唑基,吡咯基,吡唑基,呋喃基或噻吩基,其各自任选被卤素,羟基,硝基,三氟甲基,羧基,1-4C-烷基,1-4C-烷氧基或1-4C-烷氧基羰基 R4是完全或主要被氟取代的1-4C-烷氧基,R5是卤素,羟基,硝基,三氟甲基,羧基,1-4C-烷基,1-4C-烷氧基,1-4C-烷氧基,其完全或 predo 1-4位烷基羰基,1-4C-烷氧羰基,氨基,单 - 或二 - 1-4C-烷基氨基,氨基羰基,单 - 或二 - 1-4C-烷基氨基羰基,1-4C-烷基羰基氨基,1-4C-烷基羰氧基,1 由R 6和/或R 7在苯基部分取代的苯基羰基氨基,苯基羰基氨基,苯基羰基氨基,苄基羰基氨基,在苯基部分被R8和/或R9取代的苄基羰基氨基,苯基磺酰基氨基,在R10和/或R11在苯基部分取代的苯基磺酰基氨基, 由R12和/或R13在苯基部分取代的苄基磺酰基氨基或苄基磺酰基氨基。
    • 9. 发明公开
    • PURIN-6-ONE-DERIVATIVES
    • PURIN-6-ON DERIVATE
    • EP1601675A1
    • 2005-12-07
    • EP04716252.4
    • 2004-03-02
    • ALTANA Pharma AG
    • TENOR, HermannBAER, ThomasHATZELMANN, ArminQUINTINI, Gianluca
    • C07D473/30A61K31/522A61P9/00
    • C07D473/30
    • 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.