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    COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
    62.
    发明申请
    COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS 有权
    化合物治疗CNS病症

    公开(公告)号：US20120115863A1

    公开(公告)日：2012-05-10

    申请号：US13062625

    申请日：2009-09-04

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

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

    IPC分类号： A61K31/519 ,  A61K31/5377 ,  A61P25/00 ,  A61P3/10 ,  A61P25/16 ,  A61P25/18 ,  A61P3/00 ,  A61P3/04 ,  C07D487/04 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein Ā is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. 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. Chemically, the compounds are characterised as pyrazolopyrimidinones with a cycloalkyl-moiety directly bound to the 1 position of the pyrazolopyrimidinone and a second substituent in the 6 position which is bound via an optionally substituted methylene-bridge. Further aspects of the present invention refer to a process for the manufacture of the compounds and their use for producing medicaments.

    摘要翻译： 本发明涉及式（I）的新的环烷基 - 或环烯基取代的吡唑并嘧啶酮，其中Ā选自由C 3 -C 8 - 环烷基或C 4 -C 8 - 环烯基组成的组A1，其中C3- 环烷基选自环丙基，环丁基，环戊基，环己基，环庚烷基和环辛基; 选自环丁烯基，环戊烯基，环己烯基，环庚烯基，环辛烯基，环戊二烯基，环己二烯基，环庚二烯基，环辛二烯基，环庚三烯基，环辛烯基，环辛烯四烯基的C4-C8-环烯基的成员。 新化合物应用于制造药物，特别是用于改善有需要的患者的感知，集中，学习和/或记忆的药物。 在化学上，化合物的特征在于吡唑并嘧啶酮，其中环烷基部分直接键合在吡唑并嘧啶酮的1位上，而6位上的第二个取代基通过任意取代的亚甲基桥结合。 本发明的其它方面是指化合物的制造方法及其制备药物的用途。

    1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS
    63.
    发明申请
    1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS 有权
    1-环己基-1,5-二氢吡喃并[3,4-D]吡啶并[4-a]衍生物及其作为PDE9A调节剂的用途

    公开(公告)号：US20110184000A1

    公开(公告)日：2011-07-28

    申请号：US12935686

    申请日：2009-04-01

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

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

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

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： The invention relates to novel 1,6-disubstituted pyrazolopyrimidinones, Formula (I) with is a mono-, bi- or tri-cyclic heterocyclyl group, the ring members of which are carbon atoms and at least 1, preferably 1, 2 or 3, heteroatom(s), which are selected from the group of nitrogen, oxygen and sulphur, which is in the form of —S(O)r— with r being 0, 1 or 2, and—said heterocyclyl group is or comprises 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member and—said heterocyclyl group is bound to the scaffold by said 1 non-aromatic, saturated, or partly unsaturated monocyclic ring which comprises at least 1 heteroatom as ring member. According to one aspect of the invention the new compounds are for the manufacture of medicaments, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. The new compounds are also for the manufacture of medicaments for the treatment of Alzheimer's disease.

    摘要翻译： 本发明涉及新的1,6-二取代的吡唑并嘧啶酮，式（I）是具有单，双或三环杂环基，其环成员是碳原子，并且至少1个，优选1,2或3个 ，选自氮，氧和硫的杂原子，其为-S（O）r-，其中r为0,1或2，并且所述杂环基为或包含1 包含至少1个杂原子作为环成员的非芳族，饱和或部分不饱和单环，并且所述杂环基通过所述1个非芳族，饱和或部分不饱和的单环与支架结合，所述单芳环包括至少1个杂原子 作为环成员。 根据本发明的一个方面，新化合物用于制造药物，特别是用于治疗有关感知，集中，学习或记忆缺陷的病症的药物。 新化合物也用于制备用于治疗阿尔茨海默氏病的药物。