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    • 4. 发明公开
    • 베타 아밀로이드 피브릴 형성 억제 화합물, 이의 제조 방법 및 이를 포함하는 약학 조성물
    • 用于BETA淀粉样纤维形成的抑制化合物及其制备方法和包含其的药物组合物
    • KR1020080022988A
    • 2008-03-12
    • KR1020060086900
    • 2006-09-08
    • 한국과학기술연구원한미사이언스 주식회사
    • 김동찬김동진유경호신계정변성림이관순김맹섭안영길묵인희
    • C07D213/34C07D213/26C07D213/30
    • C07D213/38C07D213/30
    • An inhibitory compound for formation of beta-amyloid fibril is provided to inhibit formation of senile plaque caused by beta-amyloid by specifically recognizing beta-amyloid without cytotoxicity and improve brain blood barrier(BBB) permeability, so that the compound is useful for treatment of degenerative brain disease containing dementia. A compound for inhibiting formation of beta-amyloid fibril represented by the formula(1) is prepared by performing Honer-Emmons reaction of compounds represented by the formula(2) with aldehyde compounds represented by the formula(3) and base such as metal hydrogen compound, metal alkoxide, alkyl alkali metal compound or amide type alkali metal compound in an organic solvent, wherein X is N or C; R^1 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy or C1-C3 alkylamino group; and R^2 and R^3 are each independently OH, p-methoxybenzyloxy(OPMB), C1-C3 alkoxy, NO2, NH2, C1-C3 alkyl amino or di C1-C3 alkyl amino. Further, the organic solvent is an ether typed organic solvent.
    • 提供用于形成β-淀粉样蛋白原纤维的抑制化合物,以通过特异性识别β-淀粉样蛋白而不具有细胞毒性并改善脑血管屏障(BBB)通透性,从而抑制由β-淀粉样蛋白引起的老年斑的形成,使得该化合物可用于治疗 退行性脑病包含痴呆症。 由式(1)表示的抑制β-淀粉样蛋白原纤维形成的化合物通过由式(2)表示的化合物与由式(3)表示的醛化合物和碱例如金属氢进行Hon-Emmons反应来制备 化合物,金属醇盐,烷基碱金属化合物或酰胺型碱金属化合物在有机溶剂中,其中X是N或C; R 1是H,卤素,C 1 -C 3烷基,C 1 -C 3烷氧基或C 1 -C 3烷基氨基; R 2和R 3各自独立地为OH,对甲氧基苄氧基(OPMB),C1-C3烷氧基,NO2,NH2,C1-C3烷基氨基或二C1-C3烷基氨基。 此外,有机溶剂是醚类有机溶剂。