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    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    3.
    发明公开
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    化合物作为磷酸二酯酶10A型抑制剂

    公开(公告)号：EP2922842A2

    公开(公告)日：2015-09-30

    申请号：EP13798625.3

    申请日：2013-11-25

    申请人： AbbVie Inc. ,  AbbVie Deutschland GmbH & Co KG

    发明人： GENESTE, Hervé ,  TURNER, Sean ,  OCHSE, Michael ,  DRESCHER, Karla ,  BLACK, Lawrence A. ,  JANTOS, Katja ,  JAKOB, Clarissa

    IPC分类号： C07D401/14 ,  A61K31/4353 ,  A61K31/4427 ,  C07D401/04 ,  C07D401/10 ,  C07D471/04 ,  C07D487/04 ,  A61P25/00

    CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D401/10 ,  C07D471/04 ,  C07D487/04

    摘要： The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders wherein Y
    1 and Y
    2 are adjacent atoms in Het
    1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het
    1 is a bivalent monocyclic 5- or 6-membered heteroaromatic radical, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R
    a as ring members, or a bivalent fused bicyclic 8-, 9- or 10-membered heteroaromatic radical, having 1, 2, 3 or 4 heteroatoms or heteroatom moieties selected from O, S, N and N-R
    a as ring members; Het
    2 is inter alia monocyclic 5- or 6-membered hetaryl, having 1, 2 or 3 heteroatoms or heteroatom moieties selected from O, S, N and N-R
    1a as ring members, Cyc is inter alia optionally substituted monocyclic 5- or 6-membered hetaryl or optionally substituted fused 8-, 9- or 10-membered bicyclic hetaryl; Ar is optionally substituted phenylene or optionally substituted bivalent 6-membered hetaryl; R is attached to a carbon atom of Het
    1 and inter alia - halogen, C
    1 -C
    6 -alkyl, C
    2 -C
    6 -alkenyl, C
    2 -C
    6 -alkynyl, C
    1 -C
    6 -alkoxy, C
    1 -C
    6 -fluoroalkyl, C
    1 -C
    6 -fluoroalkoxy, C
    3 -C
    6 -cycloalkyl etc.

    INHIBITORS OF PHOSPHODIESTERASE TYPE 10A
    5.
    发明公开
    INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
    HEMMER DER PHOSPHODIESTERASE TYP 10A

    公开(公告)号：EP2776418A1

    公开(公告)日：2014-09-17

    申请号：EP12784578.2

    申请日：2012-11-08

    申请人： AbbVie Deutschland GmbH & Co KG ,  AbbVie Inc.

    发明人： GENESTE, Hervé ,  OCHSE, Michael ,  DRESCHER, Karla ,  TURNER, Sean ,  BEHL, Berthold ,  LAPLANCHE, Loic ,  DINGES, Jürgen ,  JAKOB, Clarissa ,  BLACK, Lawrence A. ,  JANTOS, Katja.

    IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04 ,  C07D519/00 ,  A61K31/519 ,  A61P25/00

    CPC分类号： C07D519/00 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/048 ,  C07D495/04

    摘要： The present invention relates to novel compounds of the formula (I) which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X
    1 is N or CH, X
    2 is N or C-R
    7 ; X
    3 is O, S, -X
    4 =C(R
    8 )-, where C(R
    8 ) is bound to the carbon atom which carries R
    2 , or -X
    5 =C(R
    9 )-, where X
    5 is bound to the carbon atom which carries R
    2 ; X
    4 is N or C-R
    9 ; X
    5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R
    1 is selected inter alia from hydrogen, halogen, OH, C
    1 -C
    4 -alkyl, trimethylsilyl, C
    1 -C
    4 -alkylsulfanyl, C
    1 -C
    4 -alkoxy-C
    1 -C
    4 -alkyl, C
    1 -C
    4 - alkoxy, C
    1 -C
    4 -alkoxy-C
    1 -C
    4 -alkoxy, the moiety Y
    1 -Cyc
    1 ; R
    2 is selected inter alia from hydrogen, halogen, OH, C
    1 -C
    4 -alkyl, trimethylsilyl, C
    1 -C
    4 -alkoxy-C
    1 -C
    4 -alkyl, C
    1 -C
    4 -alkoxy, C
    1 -C
    4 - alkoxy-C
    1 -C
    4 -alkoxy, C
    2 -C
    4 -alkenyloxy, etc; A represents one of the following groups A
    1 , A
    2 , A
    3 , A
    4 or A
    5 : where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R
    3 to R
    9 , R
    3e , R
    3f , A', Y
    1 and Cyc
    1 are defined in the claims.

    摘要翻译： 本发明涉及式I的新型化合物，其为10A型磷酸二酯酶的抑制剂及其用于制备药物的用途，因此其适用于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善 与这些疾病相关的症状和降低这种疾病的风险。 其中Q是O或S，X 1是N或CH，X 2是N或C-R 7; X3是O，S-X4 = C（R8） - ，其中C（R8）与携带R2的碳原子结合，或-X5 = C（R9） - ，其中X5与携带R2的碳原子结合 ; X4是N或C-R9; X5是N; Het选自任选取代的苯基，单环杂芳基和稠合双环杂芳基; R1特别是选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4烷基硫烷基，C 1 -C 4 - 烷氧基-C 1 -C 4烷基，C 1 -C 4 - 烷氧基，C 1 -C 4烷氧基 - C1-C4-烷氧基，Y1-Cyc1部分; R2特别是选自氢，卤素，OH，C 1 -C 4 - 烷基，三甲基甲硅烷基，C 1 -C 4 - 烷氧基-C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷氧基-C 1 -C 4烷氧基， C2-C4-烯氧基等; A代表以下组A1，A2，A3，A4或A5：其中*表示分别与Het和氮原子相连的点; 并且在权利要求中定义R3至R9，R3e，R3f，A'，Y1和Cyc1。