PPARα/γ/δ 효능제로 작용하는 알콕시 인돌-3-아세트산 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
    1.
    发明授权
    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激动剂的烷氧基吲哚-3-乙酸衍生物,其药学上可接受的盐,含有与活性成分相同的

    公开(公告)号:KR101275770B1

    公开(公告)日:2013-06-14

    申请号:KR1020100015380

    申请日:2010-02-19

    Abstract: 본발명은하기화학식 1로표시되는알콕시인돌-3-아세트산유도체, 이의제조방법및 이를유효성분으로함유하는약학적조성물에관한것으로, 본발명에따른알콕시인돌-3-아세트산유도체는 PPARα/γ/δ에대하여우수한활성을나타내므로, 비만, 당뇨, 고지혈증, 고혈압, 동맥경화증, 심혈관계질환, 대사성질환, 암, 염증등의질환을예방또는치료할수 있는 PPAR 효능제로유용하게사용될수 있다.[화학식 1](상기화학식 1에서, 상기 R, R, R및 m은본 명세서내에정의한바와같다.)

    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。

    PPARα/γ/δ 효능제로 작용하는 알콕시 인돌-3-아세트산 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 약학적 조성물
    2.
    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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