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    PYRIDINYL-QUINAZOLINE DERIVATIVES AND THEIR MEDICAL USE
    3.
    发明公开
    PYRIDINYL-QUINAZOLINE DERIVATIVES AND THEIR MEDICAL USE 有权
    PYRIDINYLCHINAZOLINDERIVATE及其医药用途

    公开(公告)号：EP1966184A2

    公开(公告)日：2008-09-10

    申请号：EP06841392.1

    申请日：2006-12-18

    申请人： NeuroSearch A/S

    发明人： ERIKSEN, Birgitte, L. ,  SØRENSEN, Ulrik, Svane ,  TEUBER, Lene ,  PETERS, Dan ,  HOUGAARD, Charlotte ,  JOHANSEN, Tina, Holm ,  CHRISTOPHERSEN, Palle

    IPC分类号： C07D401/04 ,  A61K31/517 ,  A61P11/06

    CPC分类号： C07D401/04

    摘要： This invention relates to novel pyridinyl-quinazoline derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. n is 0, 1, 2 or 3; X represents O, S or NR'; wherein R' represents hydrogen, alky I, cycloalkyl or cycloalkyl-alkyl; or, when n is 0 and X is NR', R' together with Y and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; Y represents alkyl, cycloalkyl, alkyl-cycloalkyl, alkenyl or phenyl, which phenyl is optionally substituted one or more times with substituents selected from the group consisting of alkyl, amino-alkyl, alkyl-amino, alkyl-amino-alkyl, hydroxy-alkyl, alkoxy-alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, cyano, nitro and amino; or, when n is O, Y together with R' and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; and R1, R2, R3 and R4, independently of each other, represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; or R1 and R2, or R2 and R3, or R3 and R4, respectively, together form a benzo-fused carbocyclic ring, optionally substituted with alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; and the remaining of R1, R2, R3 and R4 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy. alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl.

    PYRIDINYL-QUINAZOLINE DERIVATIVES AND THEIR MEDICAL USE
    8.
    发明授权
    PYRIDINYL-QUINAZOLINE DERIVATIVES AND THEIR MEDICAL USE 有权
    吡啶基 - 喹唑啉衍生物及其医疗用途

    公开(公告)号：EP1966184B1

    公开(公告)日：2010-08-25

    申请号：EP06841392.1

    申请日：2006-12-18

    申请人： NeuroSearch A/S

    发明人： ERIKSEN, Birgitte, L. ,  SØRENSEN, Ulrik, Svane ,  TEUBER, Lene ,  PETERS, Dan ,  HOUGAARD, Charlotte ,  JOHANSEN, Tina, Holm ,  CHRISTOPHERSEN, Palle

    IPC分类号： C07D401/04 ,  A61K31/517 ,  A61P11/06

    CPC分类号： C07D401/04

    摘要： This invention relates to novel pyridinyl-quinazoline derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels. n is 0, 1, 2 or 3; X represents O, S or NR'; wherein R' represents hydrogen, alky I, cycloalkyl or cycloalkyl-alkyl; or, when n is 0 and X is NR', R' together with Y and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; Y represents alkyl, cycloalkyl, alkyl-cycloalkyl, alkenyl or phenyl, which phenyl is optionally substituted one or more times with substituents selected from the group consisting of alkyl, amino-alkyl, alkyl-amino, alkyl-amino-alkyl, hydroxy-alkyl, alkoxy-alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, cyano, nitro and amino; or, when n is O, Y together with R' and together with the nitrogen to which they are attached form a heterocyclic ring, which heterocyclic ring may optionally be substituted with alkyl of phenyl; and R1, R2, R3 and R4, independently of each other, represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; or R1 and R2, or R2 and R3, or R3 and R4, respectively, together form a benzo-fused carbocyclic ring, optionally substituted with alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl; and the remaining of R1, R2, R3 and R4 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy. alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl.

    摘要翻译： 本发明涉及式（I）的新型吡啶基 - 喹唑啉衍生物及其作为钾通道调节剂的用途。 此外，本发明涉及用于治疗或缓解与钾通道活性有关的疾病或病症的药物组合物。 n是0,1,2或3; X代表O，S或NR'; 其中R'代表氢，烷基，环烷基或环烷基 - 烷基; 或者当n是0且X是NR'时，R'与Y一起并与它们所连接的氮一起形成杂环，该杂环可以任选被苯基的烷基取代; Y表示烷基，环烷基，烷基 - 环烷基，烯基或苯基，该苯基任选用选自烷基，氨基 - 烷基，烷基 - 氨基，烷基 - 氨基 - 烷基，羟基 - 烷基 ，烷氧基 - 烷基，环烷基，环烷基 - 烷基，烯基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，氰基，硝基和氨基; 或者当n是0时，Y与R'一起并与它们所连接的氮一起形成杂环，该杂环可以任选地被苯基的烷基取代; 烷基，环烷基，环烷基 - 烷基，烯基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，烷氧基 - 羰基，氰基，硝基，氨基，苯基或苯甲酰基 ; 或者R 1和R 2或R 2和R 3或R 3和R 4一起形成任选被烷基，环烷基，环烷基 - 烷基，烯基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基，烷氧基 氰基，硝基，氨基，苯基或苯甲酰基; 其余的R1，R2，R3和R4代表氢，烷基，环烷基，环烷基 - 烷基，烯基，卤素，卤代烷基，羟基，烷氧基，卤代烷氧基。 烷氧基 - 羰基，氰基，硝基，氨基，苯基或苯甲酰基。