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    베타-아밀로이드 피브릴 형성 저해 효능을 갖는 아미노스티릴벤조퓨란 화합물 및 이를 함유하는 약학 조성물
    5.
    发明公开
    베타-아밀로이드 피브릴 형성 저해 효능을 갖는 아미노스티릴벤조퓨란 화합물 및 이를 함유하는 약학 조성물 无效
    作为抗β-淀粉样蛋白形成的抑制剂的氨基苯丙酮衍生物和包含其的药物组合物

    公开(公告)号：KR1020130111082A

    公开(公告)日：2013-10-10

    申请号：KR1020120033590

    申请日：2012-03-30

    Applicant: 한국과학기술연구원

    Inventor： 김동진 ,  유경호 ,  김영수 ,  박웅서 ,  강용구 ,  김혜연 ,  김윤경 ,  박기덕 ,  김맹섭 ,  서귀현 ,  안영길

    IPC: C07D413/12 ,  C07D307/86 ,  A61K31/421 ,  A61P25/00

    CPC classification number: C07D413/12 ,  C07D307/81 ,  C07D405/12

    Abstract: PURPOSE: An aminostyrylbenzofuran compound and a pharmaceutical composition containing the same are provided to prevent and treat neurodegenerative diseases caused by beta-amyloid fibrillation. CONSTITUTION: A compound is selected among an aminostyrylbenzofuran compound of chemical formula 1 and a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof. A pharmaceutical composition which suppresses beta-fibrillation contains the compound as an active ingredient. A pharmaceutical composition for preventing or treating neurodegenerative diseases contains the compound as an active ingredient. The neurodegenerative diseases are senile dementia, stroke, Parkinson's disease, Huntington's disease, or bovine spongiform encephalopathy.

    Abstract translation: 目的：提供氨基苯乙烯基苯并呋喃化合物和含有它们的药物组合物，以预防和治疗由β-淀粉样蛋白原纤颤引起的神经变性疾病。 构成：化合物选自化学式1的氨基苯乙烯基苯并呋喃化合物及其药学上可接受的盐，异构体，水合物和溶剂合物。 抑制β-原纤维化的药物组合物含有作为活性成分的化合物。 用于预防或治疗神经变性疾病的药物组合物含有该化合物作为活性成分。 神经变性疾病是老年性痴呆，中风，帕金森病，亨廷顿氏病或牛海绵状脑病。

    베타-아밀로이드 피브릴 형성 저해 효능을 갖는 스티릴벤조퓨란 화합물 및 이의 제조 방법
    8.
    发明公开
    베타-아밀로이드 피브릴 형성 저해 효능을 갖는 스티릴벤조퓨란 화합물 및 이의 제조 방법 失效
    作为抗坏血酸纤维素形成的抑制剂的苯乙烯苯并呋喃衍生物及其制备方法

    公开(公告)号：KR1020090129377A

    公开(公告)日：2009-12-16

    申请号：KR1020090052245

    申请日：2009-06-12

    Applicant: 한국과학기술연구원 ,  한미사이언스 주식회사

    Inventor： 김동진 ,  유경호 ,  변지훈 ,  김영수 ,  김혜연 ,  이관순 ,  김맹섭 ,  안영길 ,  이지훈 ,  이명환 ,  황하나 ,  류지연

    IPC: C07D307/78 ,  C07D307/81 ,  C07D307/77

    CPC classification number: C07D307/81 ,  C07D307/80

    Abstract: PURPOSE: A pharmaceutical composition containing styrylbenzofuran compound is provided to ensure suppression efficiency of beta amyloid fibril formation. CONSTITUTION: A styrylbenzofuran compound is denoted by chemical formula 1. A compound of chemical formula 1 is obtained through Honer-Emmons reaction of a compound of chemical formula 2 with a compound of chemical formula 3 and alkali under the presence of organic solvent. The alkali is hydride of alkali metal, alkyl alkali metal compound, alkoxide compound of alkali metal or alkali metal amide compound. The organic solvent is ether organic solvent. A product thorugh Honer-Emmons reaction is demethylated using boron trichloride, boron trifluoride, boron tribromide or iodotrimethylsilane.

    Abstract translation: 目的：提供含有苯乙烯基苯并呋喃化合物的药物组合物，以确保β-淀粉样蛋白原纤维形成的抑制效率。 组成：苯乙烯基苯并呋喃化合物由化学式1表示。化学式1的化合物通过化学式2的化合物与化学式3的化合物和碱在有机溶剂的存在下的Hon-Emmons反应获得。 碱是碱金属的氢化物，烷基碱金属化合物，碱金属或碱金属酰胺化合物的醇盐化合物。 有机溶剂为醚有机溶剂。 使用三氯化硼，三氟化硼，三溴化硼或碘代三甲基硅烷将Honer-Emmons反应产物脱甲基化。

    베타 아밀로이드 피브릴 형성 억제 화합물, 이의 제조 방법 및 이를 포함하는 약학 조성물
    9.
    发明公开
    베타 아밀로이드 피브릴 형성 억제 화합물, 이의 제조 방법 및 이를 포함하는 약학 조성물 失效
    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

    公开(公告)号：KR1020080022988A

    公开(公告)日：2008-03-12

    申请号：KR1020060086900

    申请日：2006-09-08

    Applicant: 한국과학기술연구원 ,  한미사이언스 주식회사

    Inventor： 김동찬 ,  김동진 ,  유경호 ,  신계정 ,  변성림 ,  이관순 ,  김맹섭 ,  안영길 ,  묵인희

    IPC: C07D213/34 ,  C07D213/26 ,  C07D213/30

    CPC classification number: C07D213/38 ,  C07D213/30

    Abstract: 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.

    Abstract translation: 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。

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