摘要:
The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; R1 is hydrogen, halogen, CN or (1C-4C)alkyl; R2 is hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; R3 and R5 are independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; R4 is hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; R6 is hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or R6 is optionally halogenated (1C-4C)alkyl; each R7 independently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.
摘要翻译:本发明提供具有式I结构的化合物,其中:X是碳原子或氮原子; Ar是苯基或杂芳环; R 1是氢,卤素,CN或(1C-4C)烷基; R 2是氢,卤素或任选氟化的(1C-3C)烷氧基; 卤代(1C-4C)烷氧基,任选卤代(1C-4C)烷氧基,任意卤代的芳基(1C-4C)烷氧基 ,任选卤代(1C-4C)烯基或羟甲基; R 4是氢,卤素,任选卤代的(1C-4C)烷氧基或任选的卤代芳基(1C-4C)烷氧基; R 6是氢,任选被一个或多个卤素或(1C-4C)烷基取代的苄基,或任选被卤代(C 1 -C 4)烷基取代; 每个R 7独立地是氢,卤素,任选卤代(1C-4C)烷基或任选卤代(1C-4C)烷氧基及其药学上合适的酸加成盐,用作糖皮质激素受体调节剂,特别是 治疗中枢神经系统疾病。
摘要:
This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The 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.