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1. 发明申请

US20190367531A1 SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE 审中-公开
公开(公告)号：US20190367531A1
公开(公告)日：2019-12-05
申请号：US16409323
申请日：2019-05-10
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Jürgen DINGES , Achim MOELLER , Michael OCHSE , Martin SCHMIDT , Michael SCHULZ , Sean TURNER , Elizabeth Louise VAN DER KAM , Anil VASUDEVAN
IPC分类号： C07D498/04 , A61K31/4985 , C07D513/04
摘要： Compounds of formula (I) 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.

2. 发明申请

US20140275069A1 Novel inhibitor compounds of phosphodiesterase type 10A 有权
标题翻译：新型磷酸二酯酶10A抑制剂化合物
公开(公告)号：US20140275069A1
公开(公告)日：2014-09-18
申请号：US14189961
申请日：2014-02-25
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Katja JANTOS , Michael OCHSE , Hervé GENESTE , Jayne FROGGETT , Clarissa JAKOB , Karla DRESCHER , Jürgen DINGES
IPC分类号： C07D495/04
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: In formula I the variables X1 is CH or N, X2 is O or S and where R1, R2, R3, R4 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，其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。

3. 发明申请

US20160304527A1 SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE 有权
标题翻译：取代的吡唑并嘧啶及其使用方法
公开(公告)号：US20160304527A1
公开(公告)日：2016-10-20
申请号：US15133851
申请日：2016-04-20
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Ramin FAGHIH , Achim MOELLER , Michael OCHSE , Frauke POHLKI , Martin SCHMIDT , Michael SCHULZ , Kevin SIPPY , Sean TURNER , Elizabeth Louise VAN DER KAM
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/519 , C07D519/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 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.
摘要翻译：其中R 1，R 2，R 3，R 4，L 1和G 1如说明书中所定义，可用于治疗通过γ-氨基丁酸B（GABA）的正性变构调节来预防或改善的病症或病症， B）受体。描述了制备化合物的方法。还描述了式（I）化合物的药物组合物，以及使用这些化合物和组合物的方法。

4. 发明申请

US20140303153A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20140303153A1
公开(公告)日：2014-10-09
申请号：US14208067
申请日：2014-03-13
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB
IPC分类号： C07D471/04
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Het，A，X，Y，Z，R1，R2，R3，R4， R5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。

5. 发明申请

US20140051695A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20140051695A1
公开(公告)日：2014-02-20
申请号：US13968242
申请日：2013-08-15
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Clarissa JAKOB
IPC分类号： C07D471/14 , C07D487/04
CPC分类号： C07D471/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. 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，其N-氧化物，互变异构体，前体药物及其药学上可接受的盐，其中在式I中，变量R1，R2，R3，R4和R5如权利要求中所定义，其中X 是C-R6或N，Y是C-R7或N，其中R6和R7尤其是氢，卤素，烷氧基，卤代烷氧基等。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及其用于制备药物的用途，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. 发明申请

US20180105530A1 SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE 审中-公开
公开(公告)号：US20180105530A1
公开(公告)日：2018-04-19
申请号：US15793711
申请日：2017-10-25
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Ramin FAGHIH , Achim MOELLER , Michael OCHSE , Frauke POHLKI , Martin SCHMIDT , Kevin SIPPY , Sean TURNER , Elizabeth Louise VAN DER KAM
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/519 , C07D519/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 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.

7. 发明申请

US20180030033A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
公开(公告)号：US20180030033A1
公开(公告)日：2018-02-01
申请号：US15724410
申请日：2017-10-04
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Hervé GENESTE , Sean Colm TURNER , Michael OCHSE , Karla DRESCHER , Lawrence A. BLACK , Katja JANTOS
IPC分类号： C07D401/14 , C07D471/04 , C07D401/04 , C07D401/10 , C07D487/04
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 Y1 and Y2 are adjacent atoms in Het1, which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het1 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—Ra 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—Ra as ring members; Het2 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—R1a 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 Het1 and inter alia—halogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-fluoroalkyl, C1-C6-fluoroalkoxy, C3-C6-cycloalkyl etc.

8. 发明申请

US20160137668A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20160137668A1
公开(公告)日：2016-05-19
申请号：US14997997
申请日：2016-01-18
申请人： AbbVie Deutschland 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： C07D519/00 , C07D401/14 , C07D491/048 , C07D405/14 , C07D471/04 , C07D495/04 , C07D401/06
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。

9. 发明申请

US20170073353A1 SUBSTITUTED ISOXAZOLOPYRIDAZINONES AND ISOTHIAZOLOPYRIDAZINONES AND METHODS OF USE 审中-公开
标题翻译：取代的异丙嗪酰胺和异亮氨酸亚胺碱及其使用方法
公开(公告)号：US20170073353A1
公开(公告)日：2017-03-16
申请号：US15266473
申请日：2016-09-15
申请人： AbbVie Inc. , AbbVie Deutschland GmbH & Co. KG
发明人： Jürgen DINGES , Achim MOELLER , Michael OCHSE , Martin SCHMIDT , Michael SCHULZ , Sean TURNER , Elizabeth Louise VAN DER KAM , Anil VASUDEVAN
IPC分类号： C07D498/04
CPC分类号： C07D498/04 , A61K31/4985 , C07D513/04
摘要： Compounds of formula (I) 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.
摘要翻译：和其药学上可接受的盐，其中R 1，R 2和R 3如说明书中所定义，可用于治疗通过γ-氨基丁酸B（GABA-B）受体的正性变构调节而预防或改善的病症或病症。描述了制备化合物的方法。还描述了式（I）化合物的药物组合物，以及使用这些化合物和组合物的方法。

10. 发明申请

US20160002231A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
标题翻译：磷酸二酯酶类型10A的新型抑制剂化合物
公开(公告)号：US20160002231A1
公开(公告)日：2016-01-07
申请号：US14854835
申请日：2015-09-15
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervé GENESTE , Michael OCHSE , Karla DRESCHER , Berthold BEHL , Loic LAPLANCHE , Jürgen DINGES , Clarissa JAKOB
IPC分类号： C07D471/04 , C07D519/00
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Het，A，X，Y，Z，R1，R2，R3，R4， R5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。

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