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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
    1.
    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
    3.
    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。

    COMPOUNDS FOR THE TREATMENT OF CNS DISORDERS
    4.
    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
    7.
    发明授权
    1-heterocyclyl-1,5-dihydro-pyrazolo[3,4-D] pyrimidin-4-one derivates and their use as PDE9A modulators 有权
    1-杂环基-1,5-二氢 - 吡唑并[3,4-D]嘧啶-4-酮衍生物及其作为PDE9A调节剂的用途

    公开(公告)号：US08623879B2

    公开(公告)日：2014-01-07

    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： C07D487/04 ,  A61K31/519 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16

    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。

    1-HETEROCYCLYL-1,5-DIHYDRO-PYRAZOLO[3,4-D] PYRIMIDIN-4-ONE DERIVATES AND THEIR USE AS PDE9A MODULATORS
    8.
    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。

    6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders
    10.
    发明授权
    6-cycloalkyl-pyrazolopyrimidinones for the treatment of CNS disorders 有权
    6-环烷基 - 吡唑并嘧啶酮用于治疗CNS疾病

    公开(公告)号：US09328120B2

    公开(公告)日：2016-05-03

    申请号：US14511238

    申请日：2014-10-10

    申请人： Niklas Heine ,  Christian Eickmeier ,  Marco Ferrera ,  Riccardo Giovannini ,  Holger Rosenbrock ,  Gerhard Schaenzle

    发明人： Niklas Heine ,  Christian Eickmeier ,  Marco Ferrera ,  Riccardo Giovannini ,  Holger Rosenbrock ,  Gerhard Schaenzle

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61K45/06 ,  A61P25/28 ,  A61P25/18

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

    摘要： The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 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 are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.

    摘要翻译： 本发明涉及式（I）的新型6-环烷基 - 吡唑并嘧啶酮。 其中R1是5或6元芳族杂芳基，R2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是0 ，1或2.新化合物分别用作药物的活性成分或用于制造药物，特别是用于治疗感知，集中，学习或记忆缺陷的病症的药物。 这种情况可能例如与阿尔茨海默病，精神分裂症和其他疾病相关。 新化合物还例如用于制备药物和/或用于治疗这些疾病，特别是与这种疾病相关的认知障碍。 本发明化合物显示PDE9抑制性质。