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2. 发明公开

EP2726479A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
标题翻译： NEU抑制剂DEN磷酸二酯酶类型10A
公开(公告)号：EP2726479A1
公开(公告)日：2014-05-07
申请号：EP12731416.9
申请日：2012-06-28
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 , JANTOS, Katja
IPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling 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：本发明涉及新的羧酰胺化合物，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗性质，并且特别适用于治疗或控制选自神经障碍和精神疾病的医学病症，用于改善与此类疾病相关的症状并降低此类疾病的风险。

3. 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。

4. 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。

5. 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.

6. 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

7. 发明公开

EP2707358A1 BENZAZEPINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 审中-公开
标题翻译：苯并氮杂衍生物含药物组合物，及其治疗用途。
公开(公告)号：EP2707358A1
公开(公告)日：2014-03-19
申请号：EP12723134.8
申请日：2012-05-11
申请人： Abbvie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： AMBERG, Wilhelm , LANGE, Udo , OCHSE, Michael , POHLKI, Frauke , BEHL, Berthold , MEZLER, Mario , HORNBERGER, Wilfried , HUTCHINS, Charles W.
IPC分类号： C07D223/16 , C07D267/14 , C07D403/12 , C07D413/12 , A61K31/55 , A61K31/553 , A61P25/24
CPC分类号： C07D223/16 , C07D267/14 , C07D403/12 , C07D413/12
摘要： The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.

8. 发明公开

EP2970229A1 OXINDOLE DERIVATIVES CARRYING AN OXETANE SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSINE-RELATED DISEASES 有权
标题翻译： WITH A OXETANSUBSTITUENTEN及其用于疾病介导加压素治疗的羟吲哚衍生物
公开(公告)号：EP2970229A1
公开(公告)日：2016-01-20
申请号：EP14709694.5
申请日：2014-03-13
申请人： AbbVie Deutschland GmbH & Co. KG
发明人： JANTOS, Katja , BRAJE, Wilfried , GENESTE, Hervé , KLING, Andreas , UNGER, Liliane , BEHL, Berthold , VAN GAALEN, Marcel , HORNBERGER, Wilfried , LAPLANCHE, Loic , WEBER, Silke
IPC分类号： C07D405/14 , A61K31/4545 , A61P3/00 , A61P9/00 , A61P25/00 , A61P7/00
CPC分类号： C07D405/14 , C07D487/08
摘要： The present invention relates to novel substituted oxindole derivatives, pharmaceutical compositions comprising them, and their use for the treatment of vasopressin-related disorders.
摘要翻译：本发明涉及新的羟吲哚substituiertem衍生物，药物组合物包含它们，及对加压素相关的疾病的治疗用途。

9. 发明授权

EP2970229B1 OXINDOLE DERIVATIVES CARRYING AN OXETANE SUBSTITUENT AND USE THEREOF FOR TREATING VASOPRESSINE-RELATED DISEASES 有权
标题翻译： WITH A OXETANSUBSTITUENTEN及其用于疾病介导加压素治疗的羟吲哚衍生物
公开(公告)号：EP2970229B1
公开(公告)日：2017-02-08
申请号：EP14709694.5
申请日：2014-03-13
申请人： AbbVie Deutschland GmbH & Co. KG
发明人： JANTOS, Katja , BRAJE, Wilfried , GENESTE, Hervé , KLING, Andreas , UNGER, Liliane , BEHL, Berthold , VAN GAALEN, Marcel , HORNBERGER, Wilfried , LAPLANCHE, Loic , WEBER, Silke
IPC分类号： C07D405/14 , A61K31/4545 , A61P3/00 , A61P9/00 , A61P25/00 , A61P7/00
CPC分类号： C07D405/14 , C07D487/08

10. 发明公开

EP2603487A1 PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 审中-公开
标题翻译：表鬼臼毒胺衍生物，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：EP2603487A1
公开(公告)日：2013-06-19
申请号：EP11748621.7
申请日：2011-08-12
申请人： Abbott GmbH & Co. KG , AbbVie Inc.
发明人： AMBERG, Wilhelm , OCHSE, Michael , LANGE, Udo , BEHL, Berthold , HORNBERGER, Wilfried , MEZLER, Mario , POHLKI, Frauke , TURNER, Sean , HUTCHINS, Charles
IPC分类号： C07C311/04 , C07C311/05 , C07C311/10 , C07D205/04 , C07D207/08 , C07D211/22 , C07D231/18 , C07D233/84 , C07D207/267 , C07D295/03 , A61K31/18 , A61K31/415 , A61K31/4164 , A61P25/28 , A61P25/18
CPC分类号： C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的苯烷基胺衍生物或其生理学耐受的盐。本发明涉及包含这种苯烷基胺衍生物的药物组合物，以及这种苯烷基胺衍生物用于治疗目的的用途。苯烷基胺衍生物是GlyT1抑制剂。

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