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1. 发明公开

EP2970258A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：新型的磷酸二酯酶抑制剂化合物10A
公开(公告)号：EP2970258A1
公开(公告)日：2016-01-20
申请号：EP14709693.7
申请日：2014-03-13
申请人： AbbVie Deutschland GmbH & Co KG , AbbVie Inc.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D471/04 , C07D519/00 , A61P25/00 , A61K31/437 , A61K31/4709 , A61K31/5377 , A61K31/541 , A61K31/444 , A61K31/506
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q 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. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof 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）的化合物，其N-氧化物，互变异构体，前药和药学上可接受的盐。在式I中，变量Het，A，X，Y，Z，R 1，R 2，R 3，R 4，R 5和Q如权利要求中所定义。式I化合物，其N-氧化物，互变异构体，前药和药学上可接受的盐是10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，其N-氧化物，互变异构体，前药和药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

2. 发明公开

EP2776418A1 INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译： 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。

3. 发明公开

EP2780324A1 HETEROCYCLIC CARBOXAMIDES USEFUL AS INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：杂环羧酰胺作为抑制剂磷酸二酯酶10A型
公开(公告)号：EP2780324A1
公开(公告)日：2014-09-24
申请号：EP12781349.1
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 , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D217/26 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , A61K31/472 , A61K31/502 , A61K31/4375 , A61P25/00
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.

4. 发明授权

EP2780324B1 HETEROCYCLIC CARBOXAMIDES USEFUL AS INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：杂环化合物羧酰胺抑制剂抑制剂磷酸二酯酶类型10A
公开(公告)号：EP2780324B1
公开(公告)日：2017-05-17
申请号：EP12781349.1
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 , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D217/26 , C07D237/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , A61K31/472 , A61K31/502 , A61K31/4375 , A61P25/00
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.
摘要翻译：本发明涉及作为10A型磷酸二酯酶抑制剂的化合物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，以改善与此类症状相关的症状疾病和降低这种疾病的风险。

5. 发明公开

EP2970328A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 失效
标题翻译： NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A
公开(公告)号：EP2970328A1
公开(公告)日：2016-01-20
申请号：EP14709320.7
申请日：2014-03-12
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： JANTOS, Katja , OCHSE, Michael , GENESTE, Hervé , FROGGETT, Jayne , JAKOB, Clarissa , DRESCHER, Karla , DINGES, Jürgen
IPC分类号： C07D495/04 , A61K31/5025 , A61P25/00
CPC分类号： C07D495/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: (I). In formula I the variables X
1 is CH or N, X
2 is O or S and where R
1 , R
2 , R
3 , R
4 and Q 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. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof 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X1是CH或N，X2是O或S，并且其中R1，R2，R3 R4和Q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10A型磷酸二酯酶的抑制剂。因此，本发明还涉及式I化合物，N-氧化物，互变异构体，前药和其药学上可接受的盐在制备药物中的用途，因此其适用于治疗或控制医学病症选自神经障碍和精神障碍，用于改善与这种障碍相关的症状并降低这种障碍的风险。

6. 发明授权

EP2970258B1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
公开(公告)号：EP2970258B1
公开(公告)日：2018-04-18
申请号：EP14709693.7
申请日：2014-03-13
申请人： AbbVie Deutschland GmbH & Co KG , AbbVie Inc.
发明人： GENESTE, Hervé , OCHSE, Michael , DRESCHER, Karla , BEHL, Berthold , LAPLANCHE, Loic , DINGES, Jürgen , JAKOB, Clarissa
IPC分类号： C07D471/04 , C07D519/00 , A61P25/00 , A61K31/437 , A61K31/4709 , A61K31/5377 , A61K31/541 , A61K31/444 , A61K31/506
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q 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. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof 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.

7. 发明授权

EP2776418B1 INHIBITORS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：作者型磷酸二酯酶抑制剂10A
公开(公告)号：EP2776418B1
公开(公告)日：2017-01-04
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

8. 发明公开

EP3350187A1 SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE 审中-公开
公开(公告)号：EP3350187A1
公开(公告)日：2018-07-25
申请号：EP16763869.1
申请日：2016-09-14
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： DINGES, Jürgen , MOELLER, Achim , OCHSE, Michael , SCHMIDT, Martin , SCHULZ, Michael , TURNER, Sean , VAN DER KAM, Elizabeth Louise , VASUDEVAN, Anil
IPC分类号： C07D498/04 , C07D513/04 , A61K31/4985 , A61P1/04 , A61P25/30
CPC分类号： C07D498/04 , C07D513/04
摘要： and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

9. 发明授权

EP2970146B1 ACYLAMINOCYCLOALKYL COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF DOPAMINE D3 RECEPTOR 有权
标题翻译：适用于治疗应答多巴胺D3受体调节的疾病的酰胺基环酰基化合物
公开(公告)号：EP2970146B1
公开(公告)日：2017-11-01
申请号：EP14710261.0
申请日：2014-03-14
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： HAUPT, Andreas , DINGES, Jürgen , UNGER, Liliane , WICKE, Karsten , VAN WATERSCHOOT, Robert , DRESCHER, Karla , RELO, Ana Lucia
IPC分类号： C07D239/42 , C07D403/04 , A61K31/506 , A61P25/00
CPC分类号： C07D295/155 , A61K31/496 , C07D239/42 , C07D403/04

10. 发明授权

EP2970328B1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 失效
标题翻译：新型的磷酸二酯酶抑制剂化合物10A
公开(公告)号：EP2970328B1
公开(公告)日：2017-04-26
申请号：EP14709320.7
申请日：2014-03-12
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： JANTOS, Katja , OCHSE, Michael , GENESTE, Hervé , FROGGETT, Jayne , JAKOB, Clarissa , DRESCHER, Karla , DINGES, Jürgen
IPC分类号： C07D495/04 , A61K31/5025 , A61P25/00
CPC分类号： C07D495/04

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