NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    4.
    发明公开
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A

    公开(公告)号:EP2970328A1

    公开(公告)日:2016-01-20

    申请号:EP14709320.7

    申请日:2014-03-12

    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: (I). In formula I the variables X
    1 is CH or N, X
    2 is O or S and where R
    1 , R
    2 , R
    3 , R
    4 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。

    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    5.
    发明公开
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    化合物作为磷酸二酯酶10A型抑制剂

    公开(公告)号:EP2922842A2

    公开(公告)日:2015-09-30

    申请号:EP13798625.3

    申请日:2013-11-25

    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 Y
    1 and Y
    2 are adjacent atoms in Het
    1 , which are independently selected from the group consisting of carbon and nitrogen; k is 0, 1, 2 or 3; Het
    1 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-R
    a 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-R
    a as ring members; Het
    2 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-R
    1a 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 Het
    1 and inter alia - halogen, C
    1 -C
    6 -alkyl, C
    2 -C
    6 -alkenyl, C
    2 -C
    6 -alkynyl, C
    1 -C
    6 -alkoxy, C
    1 -C
    6 -fluoroalkyl, C
    1 -C
    6 -fluoroalkoxy, C
    3 -C
    6 -cycloalkyl etc.

    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    7.
    发明公开
    NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    NEUARTIGE INHIBITORVERBINDUNGEN DER PHOSPHODIESTERASE TYP 10A

    公开(公告)号:EP2895489A1

    公开(公告)日:2015-07-22

    申请号:EP13765695.5

    申请日:2013-09-16

    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 X, Y, Q
    1 , Q
    2 have the following meanings: X is C-R
    3 or N; Q
    1 is S or O and Q
    2 is C-R
    4 or N and Q
    2 is connected to X via a double bond while Q
    1 is connected to X via a single bond; or Q
    2 is S or O and Q
    1 is C-R
    4 or N and Q
    1 is connected to X via a double bond while Q
    2 is connected to X via a single bond; Y is C-R
    5 or N; where in formula I the variables R
    1 , R
    2 , R
    3 , R
    4 and R
    5 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.

    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,因此其适用于治疗或控制选自神经障碍和精神障碍的医学病症,用于改善与此类障碍相关的症状并降低此类疾病的风险。

    INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
    10.
    发明公开
    INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A 有权
    抑制剂化合物型磷酸二酯酶10A

    公开(公告)号:EP2885299A1

    公开(公告)日:2015-06-24

    申请号:EP13750071.6

    申请日:2013-08-16

    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 R
    1 , R
    2 , R
    3 , R
    4 and R
    5 are as defined in the claims and where X is C-R
    6 or N,Y is C-R
    7 or N, where R
    6 and R
    7 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.