公开(公告)号：US09273068B2

公开(公告)日：2016-03-01

申请号：US13663008

申请日：2012-10-29

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： A61K31/4725 ,  A61K31/502 ,  C07D217/24 ,  C07D237/32 ,  C07D519/00 ,  C07D495/04 ,  C07D401/14 ,  C07D401/06 ,  C07D471/04 ,  C07D417/14 ,  C07D491/048 ,  C07D413/14

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), wherein Het, A, Q, X1, X2, X3, R1 and R2 are defined in the specification, 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.

摘要翻译： 本发明涉及式（I）的新型化合物，其中Het，A，Q，X 1，X 2，X 3，R 1和R 2在本说明书中定义，其为10A型磷酸二酯酶的抑制剂及其在制备中的用途 因此适合于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

公开(公告)号：US09138494B2

公开(公告)日：2015-09-22

申请号：US13723406

申请日：2012-12-21

申请人： AbbVie Inc.

发明人： Lawrence A. Black ,  Berthold Behl ,  Jill Wetter

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  C07D471/04 ,  C07D413/14 ,  C07D401/14 ,  C07D417/14 ,  C07B59/00

CPC分类号： A61K51/0455 ,  A61K51/0459 ,  A61K51/0465 ,  C07B59/002 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

摘要翻译： 公开了式（I）的化合物式（I）的化合物可用于治疗由PDE10A配体预防或改善的病症和病症。 式（I）的放射性标记化合物也可用作PDE10A正电子发射断层摄影配体的诊断工具。 还公开了包含式（I）化合物，使用这些化合物和组合物的方法以及制备式（I）范围内的化合物的方法的药物组合物。

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。