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    1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MUDULATORS FOR THE TREATMENT OF CNS DISORDERS
    2.
    发明申请
    1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MUDULATORS FOR THE TREATMENT OF CNS DISORDERS 有权
    1,5-二羟基吡唑并（3,4-D）嘧啶-4-酮衍生物及其用作治疗CNS疾病的PDE9A制剂

    公开(公告)号：US20110015193A1

    公开(公告)日：2011-01-20

    申请号：US12744750

    申请日：2008-11-27

    申请人： Christian Eickmeier ,  Cornelia Dorner-Ciossek ,  Dennis Fiegen ,  Thomas Fox ,  Klaus Fuchs ,  Riccardo Giovannini ,  Niklas Heine ,  Martin Hendrix ,  Holger Rosenbrock ,  Gerhard Schaenzle

    发明人： Christian Eickmeier ,  Cornelia Dorner-Ciossek ,  Dennis Fiegen ,  Thomas Fox ,  Klaus Fuchs ,  Riccardo Giovannini ,  Niklas Heine ,  Martin Hendrix ,  Holger Rosenbrock ,  Gerhard Schaenzle

    IPC分类号： A61K31/5377 ,  C07D487/04 ,  A61K31/519 ,  C07D413/14 ,  A61P25/00

    CPC分类号： C07D487/04

    摘要： The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterised by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyI, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C1-C6-alkylsulphonyl-amino, C1-C6-alkylsulphonyl and C1-C6-alkylthio; The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving, perception, concentration, learning and/or memory in patients in need thereof.

    摘要翻译： 本发明涉及新的取代吡唑并嘧啶。 在化学上，化合物的特征在于通式（I）：其中R 1为苯基或吡啶基，其中任何一个被1至4个，优选1至3个取代基X取代; X独立地选自C 2 -C 6 - 烷基或C 1 -C 6 - 烷氧基，其中C 2 -C 6 - 烷基和C 1 -C 6 - 烷氧基至少被二卤代化为全卤代。 优选具有2至6个卤素取代基，并且卤素原子选自氟，氯和溴，优选氟; R 2是苯基或杂芳基，其中苯基被1至3个基团取代，杂芳基任选被1至3个基团取代，各自独立地选自C1-C6-烷基，C1-C6-烷氧基，羟基羰基 氰基，三氟甲基，氨基，硝基，羟基，C 1 -C 6烷基氨基，卤素，C 6 -C 10 - 芳基羰基氨基，C 1 -C 6烷基羰基氨基，C 1 -C 6烷基氨基羰基。 C 1 -C 6 - 烷氧基羰基，C 6 -C 10 - 芳基氨基羰基，杂芳基氨基羰基。 杂芳基羰基氨基，C 1 -C 6烷基磺酰基 - 氨基，C 1 -C 6 - 烷基磺酰基和C 1 -C 6烷硫基; 新化合物应用于制造药物，特别是用于改善，感知，集中，学习和/或记忆有需要的患者的药物。

    1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders
    8.
    发明授权
    1, 5-dihydro-pyrazolo (3, 4-D) pyrimidin-4-one derivatives and their use as PDE9A mudulators for the treatment of CNS disorders 有权
    1,5-二氢 - 吡唑并（3,4-D）嘧啶-4-酮衍生物及其用作治疗CNS紊乱的PDE9A混悬剂

    公开(公告)号：US08648085B2

    公开(公告)日：2014-02-11

    申请号：US12744750

    申请日：2008-11-27

    申请人： Christian Eickmeier ,  Cornelia Dorner-Ciossek ,  Dennis Fiegen ,  Thomas Fox ,  Klaus Fuchs ,  Riccardo Giovannini ,  Niklas Heine ,  Martin Hendrix ,  Holger Rosenbrock ,  Gerhard Schaenzle

    发明人： Christian Eickmeier ,  Cornelia Dorner-Ciossek ,  Dennis Fiegen ,  Thomas Fox ,  Klaus Fuchs ,  Riccardo Giovannini ,  Niklas Heine ,  Martin Hendrix ,  Holger Rosenbrock ,  Gerhard Schaenzle

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P3/04 ,  A61P3/10 ,  A61P25/16

    CPC分类号： C07D487/04

    摘要： The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterized by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl. heteroarylcarbonylamino, C1-C6-alkylsulphonyl-amino, C1-C6-alkylsulphonyl and C1-C6-alkylthio; The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving, perception, concentration, learning and/or memory in patients in need thereof.

    摘要翻译： 本发明涉及新的取代吡唑并嘧啶。 在化学上，化合物的特征在于通式（I）：其中R 1为苯基或吡啶基，其中任何一个被1至4个，优选1至3个取代基X取代; X独立地选自C 2 -C 6 - 烷基或C 1 -C 6 - 烷氧基，其中C 2 -C 6 - 烷基和C 1 -C 6 - 烷氧基至少被二卤代化为全卤代。 优选具有2至6个卤素取代基，并且卤素原子选自氟，氯和溴，优选氟; R 2是苯基或杂芳基，其中苯基被1至3个基团取代，杂芳基任选被1至3个基团取代，各自独立地选自C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，羟基羰基 氰基，三氟甲基，氨基，硝基，羟基，C 1 -C 6烷基氨基，卤素，C 6 -C 10 - 芳基羰基氨基，C 1 -C 6烷基羰基氨基，C 1 -C 6烷基氨基羰基。 C 1 -C 6 - 烷氧基羰基，C 6 -C 10 - 芳基氨基羰基，杂芳基氨基羰基。 杂芳基羰基氨基，C 1 -C 6烷基磺酰基 - 氨基，C 1 -C 6 - 烷基磺酰基和C 1 -C 6烷硫基; 新化合物应用于制造药物，特别是用于改善，感知，集中，学习和/或记忆有需要的患者的药物。