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    6-CYCLOALKYL-1, 5-DIHYDRO-PYRAZOLO [3, 4-D]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A INHIBITORS
    5.
    发明公开
    6-CYCLOALKYL-1, 5-DIHYDRO-PYRAZOLO [3, 4-D]PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A INHIBITORS 审中-公开
    6-环丙基-1,5-二氢吡喃并[3,4-D]吡啶二酮-4-酮在DEREN VERWENDUNG ALS PDE9A-HEMMER

    公开(公告)号：EP3053924A1

    公开(公告)日：2016-08-10

    申请号：EP16152675.1

    申请日：2011-08-09

    申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH

    发明人： HEINE, Niklas ,  EICKMEIER, Christian ,  FERRARA, Marco ,  GIOVANNINI, Riccardo ,  ROSENBROCK, Holger ,  SCHAENZLE, Gerhard

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

    CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

    摘要： Novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I) with PDE9 inhibiting properties,

    wherein R 1 is a 5 or 6 membered aromatic heteroaryl-group, R 2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m= 1 or 2 and n is 0, 1 or 2.
    The new compounds can be used as medicaments, in particular for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds can be used in the treatment of cognitive impairment associated with such diseases.

    摘要翻译： 具有PDE9抑制性质的式（I）的新型6-环烷基 - 吡唑并嘧啶酮，其中R 1是5或6元芳族杂芳基，R 2是任选的取代基，D是任选取代的环戊基，环己基，四氢呋喃基，四氢吡喃基或 2-，3-或4-吡啶基，m = 1或2，n为0,1或2.新化合物可用作药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症 。 这些病症可能与阿尔茨海默病，精神分裂症和其他疾病有关。 新化合物可用于治疗与这些疾病相关的认知障碍。

    1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS FOR THE TEATMENT OF CNS DISORDERS
    8.
    发明公开
    1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MODULATORS FOR THE TEATMENT OF CNS DISORDERS 审中-公开
    1，-1,5-二氢 - 吡唑并（3,4-d）嘧啶-4-酮衍生物及其作为PDE9A调节剂的中枢神经系统疾病的治疗

    公开(公告)号：EP2217602A1

    公开(公告)日：2010-08-18

    申请号：EP08855654.3

    申请日：2008-11-27

    申请人： Boehringer Ingelheim International GmbH

    发明人： EICKMEIER, Christian ,  DORNER-CIOSSEK,Cornelia ,  FIEGEN, Dennis ,  FOX, Thomas ,  FUCHS, Klaus ,  GIOVANNINI, Riccardo ,  HEINE, Niklas ,  HENDRIX, Martin ,  ROSENBROCK, Holger ,  SCHAENZLE, Gerhard

    IPC分类号： C07D487/04 ,  A61K31/519

    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： 本发明涉及一种新颖的吡唑并嘧啶substituiertem。 在化学上，该化合物由通式（I）的特征在于：R1是苯基或吡啶基，其中的任何一个取代有1至4个，优选1至3个取代基X; 海誓山盟Xunabhängig从C2-C6-alky1或C1-C6烷氧基，其中C 2 -C 6烷基和C 1 -C 6烷氧基被至少二卤代至多全卤化的被选择。 优选具有2至6个卤素取代基，卤素原子选自氟，氯和溴，优选氟的被选择; R 2为苯基或杂芳基，其中苯基被1至3个基团和杂芳基取代任选substituiertem通过在每种情况下为1〜3个基团unabhängig彼此的选自C1-C6烷基，C1-C6烷氧基，羟基羰基的选择 基，氰基，三氟甲基，氨基，硝基，羟基，C1-C6烷基氨基，卤素，C 6 -C 10芳基羰基，C1-C6烷基羰基氨基，C1-C6烷基氨基羰基。 C1-C6烷氧羰基，C 6 -C 10芳基氨基羰，heteroarylaminocarbonyl。 杂芳基羰，C1-C6-烷基磺酰基氨基，C1-C6-烷基磺酰基和C1-C6烷硫基; 新化合物应当用于药物的制造中，在用于提高，感知，浓度，在需要其的患者的学习和/或记忆的特殊药剂。