닥나무로부터 추출된 폴리페놀을 유효성분으로 함유하는 제1형 당뇨병 예방 및 치료용 약학적 조성물
    26.
    发明授权
    닥나무로부터 추출된 폴리페놀을 유효성분으로 함유하는 제1형 당뇨병 예방 및 치료용 약학적 조성물 有权
    用于预防和治疗包含从作为活性成分的双歧杆菌KAZINOKI提取的多酚的1型糖尿病的药物组合物

    公开(公告)号:KR101620022B1

    公开(公告)日:2016-05-12

    申请号:KR1020140163589

    申请日:2014-11-21

    CPC classification number: A61K31/05 A61K31/045 A61K36/60 Y10S514/937

    Abstract: 본발명은닥나무()로부터추출된페놀성분인카지놀 C(kazinol C; 5-(3-(2,4-dihydroxy-5-(2-methylbut-3-en-2-yl)phenyl)prophyl)-3,4-bis(3-methylbut-2-enyl)benzene-1,2-diol) 및이소카지놀 D(isokazinol D; 4-(3-(8-hydroxy-2,2-dimethyl-5-(3-methylbut-2-enyl)chroman-6-yl)propyl)-6-(3-methylbut-3-en-2-yl)benzene-1,3-diol)을유효성분으로함유하는제1형당뇨병예방및 치료용약학적조성물에관한것으로, 상기화합물은 RINm5F 세포또는췌도에서사이토카인으로유도된세포사멸, NO 생성및 iNOS 발현을억제하고포도당자극에따라인슐린을분비하였으며 NF-κB DNA 결합, NF-κB 소단위의핵 이동, 및세포질 IκBα분해를억제하였다. 또한, MLDS-매개된당뇨병마우스의혈장인슐린수준을회복하여당뇨병에대하여보호효과를나타냄을확인함으로써, 제1형당뇨병예방및 치료용약학적조성물의유효성분으로유용하게사용될수 있다.

    Abstract translation: 本发明涉及含有吗啉酮C(5-(3-(2,4-二羟基-5-(2-甲基丁-3-烯-2-基)苯基))预防和治疗1型糖尿病的药物组合物 )-3,4-二(3-甲基丁-2-烯基)苯-1,2-二醇)和异喹啉醇D(4-(3-(8-羟基-2,2-二甲基-5-(3-甲基丁基) -2-烯基)苯并二氢吡喃-6-基)丙基)-6-(3-甲基丁-3-烯-2-基)苯-1,3-二醇),它们是从布鲁氏菌(Broussonetia kazinoki)提取的酚类作为活性成分。 复合物抑制细胞因子诱导的凋亡,NO生成和iNOS在RINm5F细胞或朗格汉斯胰岛中的表达,诱导葡萄糖刺激的胰岛素分泌,并抑制NF-κB与DNA的结合,NF-κB亚基的核易位和降解 细胞质IκBα。 此外,通过在MLDS诱导的糖尿病小鼠中回收血浆胰岛素水平,复合物显示出对糖尿病的保护作用,从而能够有效地用作预防和治疗1型糖尿病的药物组合物的活性成分。

    PPARα/γ/δ 효능제로 작용하는 알콕시 인돌-3-아세트산 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
    28.
    发明公开
    PPARα/γ/δ 효능제로 작용하는 알콕시 인돌-3-아세트산 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물 有权
    作为PPARα/γ/δ激动剂的烷基-3-乙酸衍生物,其药学上可接受的盐,含有活性成分

    公开(公告)号:KR1020110028202A

    公开(公告)日:2011-03-17

    申请号:KR1020100015380

    申请日:2010-02-19

    Abstract: PURPOSE: A pharmaceutical composition containing an alkoxy indole-3-acetic acid derivative is provided to prevent or treat obesity, diabetes, hyperlipidemia, hypertension, vascular diseases, cancer, and inflammatory diseases. CONSTITUTION: An alkoxy indole-3-acetic acid derivative is denoted by chemical formula 1. A compound of chemical formula 1a or 1b is prepared by coupling reaction of R3-(CH2)m-OH and a hydroxy idole compound of chemical formula 2a or 2b. A method for preparing 6-hydroxy indole compound of chemical formula 2a which is a starting material comprises; a step of substituting amine of 4-amino-3-nitro phenol of chemical formula 3 with iodine; a step of protecting hydroxy group of a compound of chemical formula 4 with benzyl group; a step of introducing methacrylate to a compound of chemical formula 5; a step of reducing a nitro group of a compound of chemical formula 6 with amine; a step of reacting a compound of chemical formula 7 with formyl acetate(AcOCHO) to obtain a compound of chemical formula 8; a step of reacting the compound of chemical formula 8 with triphosgen to obtain an isonitrile compound of chemical formula 9; a step of performing radical reaction of the compound of chemical formula 9 to obtain an indole compound of chemical formula 10; and a step of removing a benzyl group of the compound of chemical formula 10.

    Abstract translation: 目的:提供含有烷氧基吲哚-3-乙酸衍生物的药物组合物,用于预防或治疗肥胖,糖尿病,高脂血症,高血压,血管疾病,癌症和炎性疾病。 组分:烷氧基吲哚-3-乙酸衍生物由化学式1表示。化学式1a或1b的化合物通过R3-(CH2)m-OH和化学式2a的羟基偶氮化合物的偶联反应或 2B。 作为原料的化学式2a的6-羟基吲哚化合物的制备方法包括: 用碘取代化学式3的4-氨基-3-硝基苯胺的步骤; 用苄基保护化学式4化合物的羟基的步骤; 将甲基丙烯酸酯引入化学式5的化合物的步骤; 用胺还原化学式6的化合物的硝基的步骤; 使化学式7的化合物与乙酸甲酰酯(AcOCHO)反应得到化学式8的化合物的步骤; 使化学式8的化合物与三磷酸反应以获得化学式9的异腈化合物的步骤; 进行化学式9的化合物的自由基反应以获得化学式10的吲哚化合物的步骤; 以及除去化学式10的化合物的苄基的步骤。

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