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    • 11. 发明公开
    • 봄베신 수용체 아형-3 조절제로서의 파이퍼 아미드 계열 화합물
    • 作为BOMBESIN受体亚型-3调节剂的主要胺衍生物
    • KR1020140109273A
    • 2014-09-15
    • KR1020140022221
    • 2014-02-25
    • 서울대학교산학협력단
    • 김상희강건욱임채민김수민
    • C07D307/52C07D307/36C07C233/11A61K31/341A61P3/04
    • C07C233/22C07C233/09C07C233/11C07C235/34C07D295/192C07D307/54C07D317/60C07D319/18
    • The present invention relates to a novel α,β-unsaturated amide compound expressed by following Chemical Formula 1, a method for preparing a composition for preventing or treating obesity; and a composition for preventing or treating obesity including the α,β-unsaturated amide compound, the method being characterized by comprising: screening a compound exhibiting the effect of treating or preventing obesity from a compound library including one or more of α,β-unsatruated amide compound(s); and preparing a composition for treating or preventing obesity containing the selected compound. [Chemical Formula 1]. Since the α,β-unsatruated amide compound of the present invention is a compound having a scaffold which mimics a natural substance, piper amide, showing various activity, the α,β-unsatruated amide compound would exhibit various pharmacological activities. Also, as an intermediate, soluble by-products are produced by using β-phosphono-N-hydroxysuccinimidyl ester, and thus a pure compound is obtainable without a need for performing the typically used purification process through column chromatography. Furthermore, pharmacological activity is tested from a chemical library thus synthesized to screen a compound which serves as an agonist against BRS-3a and thus this compound can be useful as a composition for treating or preventing obesity.
    • 本发明涉及以下化学式1表示的新型α,β-不饱和酰胺化合物,用于预防或治疗肥胖症的组合物的制备方法。 以及用于预防或治疗包括α,β-不饱和酰胺化合物的肥胖症的组合物,所述方法的特征在于包括:从包含α,β-不饱和酰胺化合物中的一种或多种的化合物文库筛选显示出治疗或预防肥胖的作用的化合物 酰胺化合物; 以及制备用于治疗或预防含有所选化合物的肥胖症的组合物。 [化学式1]。 由于本发明的α,β-不饱和酰胺化合物是具有模仿具有各种活性的天然物质,哌啶酰胺的支架的化合物,所以α,β-不饱和酰胺化合物具有各种药理活性。 此外,作为中间体,通过使用β-膦酰基-N-羟基琥珀酰亚胺酯制备可溶性副产物,因此可以获得纯化合物,而不需要通过柱色谱法进行通常使用的纯化方法。 此外,从如此合成的化学文库中测试药理活性,筛选作为针对BRS-3a的激动剂的化合物,因此该化合物可用作治疗或预防肥胖症的组合物。