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    • 10. 发明申请
    • 2-PYRIDIN-2-YL-QUINAZOLINE DERIVATIVES AS POTASSIUM CHANNEL MODULATING AGENTS FOR THE TREATMENT OF RESPIRATORY DISEASES
    • 作为用于治疗呼吸道疾病的钾通道调节剂的2-吡啶-2-基 - 喹喔啉衍生物
    • WO2007071632A3
    • 2007-08-30
    • PCT/EP2006069795
    • 2006-12-18
    • NEUROSEARCH ASERIKSEN BIRGITTE LSOERENSEN ULRIK SVANETEUBER LENEPETERS DANHOUGAARD CHARLOTTEJOHANSEN TINA HOLMCHRISTOPHERSEN PALLE
    • ERIKSEN BIRGITTE LSOERENSEN ULRIK SVANETEUBER LENEPETERS DANHOUGAARD CHARLOTTEJOHANSEN TINA HOLMCHRISTOPHERSEN PALLE
    • C07D401/04A61K31/517A61P11/06
    • C07D401/04
    • 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 R 1 , R 2 , R 3 and R 4 , 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 R 1 and R 2 , or R 2 and R 3 , or R 3 and R 4 , 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 R 1 , R 2 , R 3 and R 4 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, alkenyl, halo, haloalkyl, hydroxy, alkoxy, haloalkoxy. alkoxy-carbonyl, cyano, nitro, amino, phenyl or benzoyl.
    • 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,本发明涉及可用于治疗或缓解与钾通道活性相关的疾病或病症的药物组合物。 n为0,1,2或3; X表示O,S或NR'; 其中R'表示氢,烷基I,环烷基或环烷基 - 烷基; 或者当n为0且X为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,该苯基任选被取代基取代一次或多次,所述取代基选自烷基,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; 或当n为O时,Y与R'一起并与它们所连接的氮一起形成杂环,该杂环可任选被苯基的烷基取代; 和R 1,R 2,R 3和R 4彼此独立地表示氢,烷基 氰基,硝基,氨基,苯基或苯甲酰基; 或R 1和R 2,或R 2和R 3或R 3, SUP和R 4分别一起形成苯并稠合的碳环,任选地被烷基,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,烷氧羰基 ,氰基,硝基,氨基,苯基或苯甲酰基; 而R 1,R 2,R 3和R 4的剩余部分代表氢,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。 烷氧羰基,氰基,硝基,氨基,苯基或苯甲酰基。