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    • 2. 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
    • 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
    • US08648085B2
    • 2014-02-11
    • US12744750
    • 2008-11-27
    • Christian EickmeierCornelia Dorner-CiossekDennis FiegenThomas FoxKlaus FuchsRiccardo GiovanniniNiklas HeineMartin HendrixHolger RosenbrockGerhard Schaenzle
    • Christian EickmeierCornelia Dorner-CiossekDennis FiegenThomas FoxKlaus FuchsRiccardo GiovanniniNiklas HeineMartin HendrixHolger RosenbrockGerhard Schaenzle
    • C07D487/04A61K31/519A61P25/28A61P3/04A61P3/10A61P25/16
    • C07D487/04
    • 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.
    • 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。