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公开(公告)号：US20160318871A1
公开(公告)日：2016-11-03
申请号：US15207137
申请日：2016-07-11
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.
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公开(公告)号：US10308610B2
公开(公告)日：2019-06-04
申请号：US15840138
申请日：2017-12-13
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.
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公开(公告)号：US09856220B2
公开(公告)日：2018-01-02
申请号：US15207137
申请日：2016-07-11
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.
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公开(公告)号：US09163019B2
公开(公告)日：2015-10-20
申请号：US14208067
申请日：2014-03-13
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。
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公开(公告)号：US20180222905A1
公开(公告)日：2018-08-09
申请号：US15948299
申请日：2018-04-09
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.
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公开(公告)号：US20180099936A1
公开(公告)日：2018-04-12
申请号：US15840138
申请日：2017-12-13
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.
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![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](/abs-image/US/2017/05/23/US09657034B2/abs.jpg.150x150.jpg)
公开(公告)号：US09657034B2
公开(公告)日：2017-05-23
申请号：US14997997
申请日：2016-01-18
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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公开(公告)号：US09475808B2
公开(公告)日：2016-10-25
申请号：US14854835
申请日：2015-09-15
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob
IPC分类号： A61K31/54 , 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： 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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公开(公告)号：US09464085B2
公开(公告)日：2016-10-11
申请号：US13968242
申请日：2013-08-15
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Clarissa Jakob
IPC分类号： C07D471/14 , C07D487/04 , C07D471/04
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： 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。
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公开(公告)号：US09200005B2
公开(公告)日：2015-12-01
申请号：US14189961
申请日：2014-02-25
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。
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