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Imidazole derivatives having a positive allosteric GABAB receptor modulator effect and methods of use

机译:具有正变构型GABA B 受体调节剂作用的咪唑衍生物及其使用方法

摘要

The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R1, R2, R3 and R4 are as defined in the description. For example, R1 may be phenyl, R2 may be dimethylamino pyrrolidin-1-yl, R3 may be alkoxy and R4 may be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.
机译:本发明涉及具有正变构GABA B 受体(GBR)调节剂作用的新型咪唑衍生物,所述化合物的制备方法及其用途,任选地与GABA B结合使用激动剂,用于抑制短暂的食管下括约肌松弛,用于治疗胃食管反流疾病,以及用于治疗功能性胃肠道疾病和肠易激综合症(IBS)。这些化合物由通式(I)表示,其中R 1 ,R 2 ,R 3 和R 4 如描述中所定义。例如,R 1 可以是苯基,R 2 可以是二甲基氨基吡咯烷-1-基,R 3 可以是烷氧基,R 4 可以是烷基,芳烷基,芳氧基烷基,芳氧基或杂环基烷基。

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