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    • 7. 发明授权
    • 1-phenyl-benzimidazole compounds and their use as GABA-a receptor modulators
    • 1-苯基 - 苯并咪唑化合物及其作为GABA-a受体调节剂的用途
    • US06218547B1
    • 2001-04-17
    • US09269643
    • 1999-03-31
    • Lene TeuberFrank Watjen
    • Lene TeuberFrank Watjen
    • C07D23502
    • C07D235/06C07D401/06C07D401/10C07D401/12C07D401/14C07D405/04C07D413/04
    • The present invention relates to novel benzimidazole compounds, represented by general formula (I) in which o is 0, 1, 2 or 3; R1 represents an alkyl group, a phenyl group, or a monocyclic heterocyclic group, which groups may be substituted one or more times with substituents selected from alkyl, cycloalkyl, cycloalkyl-alkyl, alkoxy, halogen, trifluoromethyl, cyano, amino and nitro; or R1 represents a cyano group or a group of the formula -alkyl-CO2R2, alkenyl-CO2R2, —CO—R2, —CO2(CH2)mR2, or —C(R3)═N—OR2, R11 represents a group of formula —CO2—R9, or R11 represents a group of general formula (II) in which n is 0, 1, 2 or 3; or R11 may represent a group of general formula (III), in which n is 0, 1, 2 or 3; the novel compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, such as for example anxiety, sleep disorders, anaestesia, memory disorders, and epilepsia or other convulsive disorders.
    • 本发明涉及由通式(I)表示的新的苯并咪唑化合物,其中o为0,1,2或3; R1表示烷基,苯基或单环杂环基,该基团可以被选自烷基,环烷基,环烷基 - 烷基,烷氧基,卤素,三氟甲基,氰基,氨基和硝基的取代基取代一次或多次; 或R 1表示氰基或式 - 烷基-CO 2 R 2,烯基-CO 2 R 2,-CO-R 2,-CO 2(CH 2)m R 2或-C(R 3)= N-OR 2的基团,R 11表示式 -CO 2 -R 9或R 11表示其中n为0,1,2或3的通式(II)的基团; 或R 11可以表示通式(III)的基团,其中n为0,1,2或3; 本发明的新化合物可用于治疗对GABA A受体复合物调节有反应的中枢神经系统疾病和病症,例如焦虑症,睡眠障碍,麻醉,记忆障碍和癫痫或其它惊厥性疾病 。