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    SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES
    18.
    发明申请
    SUBSTITUTED NAPHTHYRIDINES AND USE THEREOF AS MEDICINES 审中-公开
    取代的萘啶酮及其作为药物的用途

    公开(公告)号：US20110201608A1

    公开(公告)日：2011-08-18

    申请号：US13057288

    申请日：2009-07-23

    申请人： Matthias Hoffmann ,  Thierry Bouyssou ,  Georg Dahamnn ,  Harald Engelhardt ,  Dennis Fiegen ,  Sandra Handschum ,  Silke Hobbie ,  Takeshi Kono ,  Ulrich Reiser ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    发明人： Matthias Hoffmann ,  Thierry Bouyssou ,  Georg Dahamnn ,  Harald Engelhardt ,  Dennis Fiegen ,  Sandra Handschum ,  Silke Hobbie ,  Takeshi Kono ,  Ulrich Reiser ,  Yayoi Sato ,  Andreas Schnapp ,  Annette Schuler-Metz

    IPC分类号： A61K31/5377 ,  C07D471/04 ,  A61K31/496 ,  A61P11/06 ,  A61P19/02 ,  A61P1/04 ,  A61P17/06 ,  A61P35/00 ,  A61P17/00 ,  A61P11/00

    CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04

    摘要： The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 denotes a group A selected from among —O—R3, —NR3R4, —CR3R4R5, -(ethyne)-R3, —S—R3, —SO—R3 and SO2—R3 or R1 denotes a group B selected from among C6-10-aryl, five- to ten-membered, mono- or bicyclic heteroaryl with 1-3 heteroatoms selected independently of one another from among N, O and S; while this heteroaryl is linked to the structure according to formula 1 via either a C atom or an N atom, three- to ten-membered, mono- or bicyclic, saturated or partially saturated heterocyclic group with 1-3 heteroatoms selected independently of one another from among N, O and S, while this heterocyclic group is linked to the structure according to formula 1 via either a C atom or an N atom, and 5- to 11-membered spiro group which may optionally contain 1, 2 or 3 heteroatoms selected independently of one another from among N, O and S, while this spiro group is linked to the structure according to formula 1 via either a C atom or an N atom, while this group B may optionally be substituted as described in claim 1 and wherein R2 is and R3, R4, R5, R6, R6′, R7, R8, R9, R10, V, n and m may have the meanings given in claim 1, as well as pharmaceutical compositions containing these compounds.

    摘要翻译： 本发明涉及式1的新取代的萘啶，以及其药学上可接受的盐，非对映异构体，对映异构体，外消旋体，水合物或溶剂化物，其中R1表示选自-O-R3，-NR3R4，-CR3R4R5， （乙炔）-R 3，-S-R 3，-SO-R 3和SO 2 -R 3或R 1表示选自C 6-10 - 芳基，5至10元，单 - 或双环杂芳基和1-3 从N，O和S中彼此独立地选择的杂原子; 而该杂芳基通过C原子或N原子连接到根据式1的结构，具有1-3个互相独立选择的杂原子的三至十元，单环或二环，饱和或部分饱和的杂环基 N，O和S中的至少一个，而该杂环基通过C原子或N原子与根据式1的结构连接，并且可以任选地含有1,2或3个杂原子的5至11元螺环 N，O和S彼此独立地选择，而该螺环通过C原子或N原子连接到根据式1的结构，而该基团B可以任选地被如权利要求1和 其中R2是和R3，R4，R5，R6，R6'，R7，R8，R9，R10，V，n和m可以具有权利要求1中给出的含义，以及含有这些化合物的药物组合物。

    1, 5-DIHYDRO-PYRAZOLO (3, 4-D) PYRIMIDIN-4-ONE DERIVATIVES AND THEIR USE AS PDE9A MUDULATORS FOR THE TREATMENT OF CNS DISORDERS
    19.
    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。