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    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    1.
    发明申请
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
    磷酸二酯酶类型10A的新型抑制剂化合物

    公开(公告)号：US20130116241A1

    公开(公告)日：2013-05-09

    申请号：US13660524

    申请日：2012-10-25

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

    发明人： Hervé Geneste ,  Michael Ochse ,  Karla Drescher ,  Sean Turner ,  Berthold Behl ,  Loic Laplanche ,  Jürgen Dinges ,  Clarissa Jakob ,  Lawrence Black

    IPC分类号： C07D495/04 ,  C07D471/04 ,  C07D417/14

    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, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.

    摘要翻译： 本发明涉及式I的新型化合物，其是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并降低这种疾病的风险。 其中Q为O或S，X1为N或CH，X2为N或C-R7; X3为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。

    Inhibitor compounds of phosphodiesterase type 10A
    4.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    磷酸二酯酶10A型抑制剂化合物

    公开(公告)号：US09388180B2

    公开(公告)日：2016-07-12

    申请号：US14029142

    申请日：2013-09-17

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

    发明人： Hervé Geneste ,  Michael Ochse ,  Karla Drescher ,  Clarissa Jakob ,  Maricel Torrent

    IPC分类号： C07D491/14 ,  C07D495/14 ,  C07D498/14 ,  C07D513/14 ,  A61K31/4985 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P3/04 ,  C07D471/14 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04

    CPC分类号： C07D471/14 ,  A61K31/4985 ,  C07D491/04 ,  C07D491/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D498/14 ,  C07D513/14

    摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. where in formula I the variables X, Y, Q1, Q2 have the following meanings: X is C—R3 or N; Q1 is S or O and Q2 is C—R4 or N and Q2 is connected to X via a double bond while Q1 is connected to X via a single bond; or Q2 is S or O and Q1 is C—R4 or N and Q1 is connected to X via a double bond while Q2 is connected to X via a single bond; Y is C—R5 or N; where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof 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.

    摘要翻译： 本发明涉及式I化合物，N-氧化物，互变异构体，前药及其药学上可接受的盐。 在式I中，变量X，Y，Q1，Q2具有以下含义：X为C-R3或N; Q1是S或O，Q2是C-R4或N，Q2通过双键连接到X，而Q1通过单键连接到X; 或Q2是S或O，Q1是C-R4或N，并且Q1通过双键连接到X，而Q2通过单键连接到X; Y为C-R5或N; 在式I中，变量R1，R2，R3，R4和R5如权利要求中所定义。式I化合物，N-氧化物，互变异构体，其前药和药学上可接受的盐是磷酸二酯酶10A型和 用于制造药物并因此适合于治疗或控制选自神经系统疾病和精神疾病的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

    Inhibitor compounds of phosphodiesterase type 10A
    6.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权

    公开(公告)号：US10308610B2

    公开(公告)日：2019-06-04

    申请号：US15840138

    申请日：2017-12-13

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

    发明人： Hervé Geneste ,  Michael Ochse ,  Karla Drescher ,  Jürgen Dinges ,  Clarissa Jakob

    IPC分类号： C07D217/26 ,  C07D401/06 ,  C07D413/06 ,  C07D401/14 ,  C07D237/32 ,  C07D417/06 ,  C07D409/08 ,  C07D471/04 ,  A61K31/47 ,  C07D217/24 ,  C07D401/12 ,  C07D417/12 ,  C07D409/12

    摘要： The present invention relates to compounds 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 X1 is CH or N, X2 is C—R5 or N, Y is O or S, R1 is inter alia C2-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, C5-C8-cycloalkyl carrying a fused benzene ring, or a moiety Z1—Ar1; R2 is a radical of the formula CR21R22R23 or phenyl or 5- or 6-membered hetaryl having 1, 2 or 3 heteroatoms as ring members which are selected from O, S and N, where phenyl and monocyclic hetaryl are unsubstituted or may carry 1, 2 or 3 identical or different substituents Ra, R3 is inter alia hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, etc, or R2 and R3 together with the nitrogen atom, to which they are bound form an optionally substituted saturated 5- to 7-membered heterocyclic ring which, in addition to the nitrogen atom, may have 1 or 2 further heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SO2; R4 is inter alia C1-C4-alkyl, C1-C4-fluoroalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl or Z4—Ar4; R5 is inter alia hydrogen, halogen, C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-alkoxy, C1-C4-fluoroalkoxy, —Z5—Ar5, —O—Z5—Ar5, etc; where Z1 to Z5, Ar1 to Ar5, Ra, R21, R22 and R23 are as defined in the claims.

    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    9.
    发明申请
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权

    公开(公告)号：US20160318871A1

    公开(公告)日：2016-11-03

    申请号：US15207137

    申请日：2016-07-11

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

    发明人： Hervé Geneste ,  Michael Ochse ,  Karla Drescher ,  Jürgen Dinges ,  Clarissa Jakob

    IPC分类号： C07D217/26 ,  C07D401/14 ,  C07D471/04 ,  C07D401/12 ,  C07D417/12 ,  C07D409/12 ,  C07D401/06 ,  C07D237/32

    CPC分类号： C07D217/26 ,  A61K31/47 ,  C07D217/24 ,  C07D237/32 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D409/08 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04

    摘要： The present invention relates to compounds 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 X1 is CH or N, X2 is C—R5 or N, Y is O or S, R1 is inter alia C2-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, C5-C8-cycloalkyl carrying a fused benzene ring, or a moiety Z1—Ar1; R2 is a radical of the formula CR21R22R23 or phenyl or 5- or 6-membered hetaryl having 1, 2 or 3 heteroatoms as ring members which are selected from O, S and N, where phenyl and monocyclic hetaryl are unsubstituted or may carry 1, 2 or 3 identical or different substituents Ra, R3 is inter alia hydrogen, C1-C8-alkyl, C2-C8-alkenyl, C1-C4-fluoroalkyl, C3-C8-cycloalkyl, etc, or R2 and R3 together with the nitrogen atom, to which they are bound form an optionally substituted saturated 5- to 7-membered heterocyclic ring which, in addition to the nitrogen atom, may have 1 or 2 further heteroatoms or heteroatom containing groups selected from the group of O, N, S, SO and SO2; R4 is inter alia C1-C4-alkyl, C1-C4-fluoroalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl or Z4—Ar4; R5 is inter alia hydrogen, halogen, C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-alkoxy, C1-C4-fluoroalkoxy, —Z5—Ar5, —O—Z5—Ar5, etc; where Z1 to Z5, Ar1 to Ar5, Ra, R21, R22, and R23 are as defined in the claims.