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1. 发明申请

US20160318871A1 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.

2. 发明授权

US10308610B2 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.

3. 发明授权

US09856220B2 Inhibitor compounds of phosphodiesterase type 10A 有权
公开(公告)号：US09856220B2
公开(公告)日：2018-01-02
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 , A61K31/47 , C07D401/06 , C07D413/06 , C07D401/14 , C07D237/32 , C07D417/06 , C07D409/08 , C07D471/04 , C07D217/24 , C07D401/12 , C07D417/12 , C07D409/12
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.

4. 发明授权

US09388148B2 Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine D3 receptor 有权
公开(公告)号：US09388148B2
公开(公告)日：2016-07-12
申请号：US14213169
申请日：2014-03-14
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Andreas Haupt , Jürgen Dinges , Liliane Unger , Karsten Wicke , Robert Van Waterschoot , Karla Drescher , Ana Relo
IPC分类号： C07D403/04 , A61K31/496 , C07D295/155 , C07D239/42
CPC分类号： C07D295/155 , A61K31/496 , C07D239/42 , C07D403/04
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor. In formula I, the variables have the following meanings: m is 1 or 2, n is 1 or 2, A is selected from the group consisting of CH2, CH2CH2, CHFCH2 and CF2CH2, R1 is an oxygen containing cyclic radical selected such as C3-C6 cycloalkyl, which carries one or two oxygen containing radicals selected from the group consisting of OH, C1-C2-alkoxy, fluorinated C1-C2-alkoxy, and a carbonyl oxygen, R2 is selected from the group consisting of hydrogen, OH and fluorine, R3a is selected from the group consisting of hydrogen and methyl, R3b is selected from the group consisting of hydrogen and methyl, R4 is branched C4-C6 alkyl or branched fluorinated C4-C6 alkyl, and R5 is inter alia C1-C6 alkyl, fluorinated C1-C3 alkyl, C1-C2-alkoxy-C1-C4-alkyl, fluorinated C1-C2-alkoxy-C1-C4-alkyl, hydroxy-C1-C4-alkyl, fluorinated hydroxy-C1-C4-alkyl, oxetanyl, fluorinated oxetanyl, oxolanyl, fluorinated oxolanyl, C3-C5 cycloalkyl, fluorinated C3-C5 cycloalkyl, etc.

5. 发明授权

US09376396B2 Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作用的疾病的酰氨基环烷基化合物
公开(公告)号：US09376396B2
公开(公告)日：2016-06-28
申请号：US14051626
申请日：2013-10-11
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Andreas Haupt , Jürgen Dinges , Liliane Unger , Karsten Wicke , Robert van Waterschoot , Scott Mittelstadt , Karla Drescher , Ana Relo
IPC分类号： A61K31/496 , C07D239/42 , C07D403/04 , C07D405/14 , C07D239/26 , C07D405/04
CPC分类号： C07D239/26 , C07D239/42 , C07D403/04 , C07D405/04 , C07D405/14
摘要： The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
摘要翻译：本发明涉及新的酰氨基环烷基化合物，特别是涉及本文所述的式I化合物及其盐和N-氧化物。该化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。

6. 发明授权

US09163019B2 Inhibitor compounds of phosphodiesterase type 10A 有权
标题翻译：磷酸二酯酶10A型抑制剂化合物
公开(公告)号：US09163019B2
公开(公告)日：2015-10-20
申请号：US14208067
申请日：2014-03-13
申请人： AbbVie Deutschland GmbH & Co. KG , AbbVie Inc.
发明人： Hervë Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob
IPC分类号： A61K31/54 , C07D471/02 , 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。

7. 发明授权

US10556914B2 Substituted isoxazolopyridazinones and isothiazolopyridazinones and methods of use 有权
公开(公告)号：US10556914B2
公开(公告)日：2020-02-11
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 , C07D513/04 , A61K31/4985
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.

8. 发明申请

US20180222905A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
公开(公告)号：US20180222905A1
公开(公告)日：2018-08-09
申请号：US15948299
申请日：2018-04-09
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 , Katja Jantos
IPC分类号： C07D471/04 , C07D413/14 , C07D403/14 , C07D405/14 , C07D409/14
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.

9. 发明申请

US20180099936A1 NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 审中-公开
公开(公告)号：US20180099936A1
公开(公告)日：2018-04-12
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 , C07D471/04 , C07D401/12 , C07D417/06 , C07D237/32 , C07D401/14 , C07D413/06 , C07D401/06 , C07D409/08 , C07D417/12 , C07D409/12 , A61K31/47 , C07D217/24
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.

10. 发明授权

US09657034B2 Substituted furo[3,2-c]pyridines, thieno[3,2-c]pyridines, thieno[2,3-d]pyridazines and pyrido[3,4-d]pyridazines as phosphodiesterase type 10A inhibitors 有权
公开(公告)号：US09657034B2
公开(公告)日：2017-05-23
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 , Katja Jantos
IPC分类号： A61K31/5025 , A61K31/4355 , A61K31/4365 , C07D487/04 , C07D491/048 , C07D495/04 , C07D519/00 , C07D401/14 , C07D401/06 , C07D471/04 , C07D417/14 , C07D413/14 , C07D405/14
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.

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