Inhibitor compounds of phosphodiesterase type 10A
    11.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    磷酸二酯酶10A型抑制剂化合物

    公开(公告)号:US09475808B2

    公开(公告)日:2016-10-25

    申请号:US14854835

    申请日:2015-09-15

    CPC classification number: C07D471/04 C07D519/00

    Abstract: 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.

    Abstract translation: 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。

    Inhibitor compounds of phosphodiesterase type 10A
    12.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    磷酸二酯酶10A型抑制剂化合物

    公开(公告)号:US09464085B2

    公开(公告)日:2016-10-11

    申请号:US13968242

    申请日:2013-08-15

    CPC classification number: C07D471/14 C07D471/04 C07D487/04

    Abstract: 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.

    Abstract translation: 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。

    Inhibitor compounds of phosphodiesterase type 10A
    13.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    磷酸二酯酶10A型抑制剂化合物

    公开(公告)号:US09388180B2

    公开(公告)日:2016-07-12

    申请号:US14029142

    申请日:2013-09-17

    Abstract: 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 X, Y, Q1, Q2 have the following meanings: X is C—R3 or N; Q1 is S or O and Q2 is C—R4 or N and Q2 is connected to X via a double bond while Q1 is connected to X via a single bond; or Q2 is S or O and Q1 is C—R4 or N and Q1 is connected to X via a double bond while Q2 is connected to X via a single bond; Y is C—R5 or N; where in formula I the variables R1, R2, R3, R4 and R5 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 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.

    Abstract translation: 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X,Y,Q1,Q2具有以下含义:X为C-R3或N; Q1是S或O,Q2是C-R4或N,Q2通过双键连接到X,而Q1通过单键连接到X; 或Q2是S或O,Q1是C-R4或N,并且Q1通过双键连接到X,而Q2通过单键连接到X; Y为C-R5或N; 在式I中,变量R1,R2,R3,R4和R5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磷酸二酯酶10A型和 用于制造药物并因此适合于治疗或控制选自神经系统疾病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。

    Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine D3 receptor
    14.
    发明授权
    Acylaminocycloalkyl compounds suitable for treating disorders that respond to modulation of dopamine D3 receptor 有权
    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:US09388141B2

    公开(公告)日:2016-07-12

    申请号:US14213720

    申请日:2014-03-14

    CPC classification number: C07D239/42 A61K31/506 C07D403/04

    Abstract: 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.

    Abstract translation: 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。 在式I中,变量具有以下含义:m为1或2,n为1或2,A选自CH 2,CH 2 CH 2,CHFCH 2和CF 2 CH 2,R 1为选自氧的环状基团,例如C 3 -C 6环烷基,其携带一个或两个选自OH,C 1 -C 2烷氧基,氟化C 1 -C 2烷氧基和羰基氧的含氧基团,R 2选自氢,OH和 氟,R 3a选自氢和甲基,R 3b选自氢和甲基,R 4是支链C 4 -C 6烷基或支链氟化C 4 -C 6烷基,R 5尤其是C 1 -C 6烷基 氟化C 1 -C 3烷基,C 1 -C 2烷氧基-C 1 -C 4烷基,氟化C 1 -C 2烷氧基-C 1 -C 4 - 烷基,羟基-C 1 -C 4 - 烷基,氟化羟基-C 1 -C 4烷基,氧杂环丁烷基 ,氟化氧杂环丁烷基,氧杂环戊烷基,氟代氧杂环戊烷基,C3-C5环烷基,氟化C3-C5环烷基等

    Inhibitor compounds of phosphodiesterase type 10A
    15.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    磷酸二酯酶10A型抑制剂化合物

    公开(公告)号:US09200005B2

    公开(公告)日:2015-12-01

    申请号:US14189961

    申请日:2014-02-25

    CPC classification number: C07D495/04

    Abstract: 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.

    Abstract translation: 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。

    Inhibitor compounds of phosphodiesterase type 10A
    18.
    发明授权
    Inhibitor compounds of phosphodiesterase type 10A 有权
    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

    CPC classification number: C07D471/04 C07D519/00

    Abstract: 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.

    Abstract translation: 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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