公开(公告)号：KR1020110028202A

公开(公告)日：2011-03-17

申请号：KR1020100015380

申请日：2010-02-19

Applicant: 숙명여자대학교산학협력단

Inventor： 전라옥 ,  류재하 ,  김효진 ,  강보미 ,  장희련 ,  이다연

IPC: C07D209/04 ,  C07D209/02 ,  A61K31/40 ,  A61P3/10

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。

公开(公告)号：KR101095734B1

公开(公告)日：2011-12-21

申请号：KR1020090006090

申请日：2009-01-23

Applicant: 숙명여자대학교산학협력단

Inventor： 윤석준 ,  양영 ,  전라옥 ,  최지원 ,  김성화 ,  강보미 ,  박연선 ,  고윤애

IPC: C07D277/36 ,  C07D277/32 ,  A61P3/10 ,  A61P9/12

Abstract: 본 발명은 사람 퍼옥시좀 증식제 활성화 수용체인 PPARγ를 활성화시키는 신규한 로다닌 유도체 화합물에 관한 것이다. 본 발명에서는 PPARγ 활성제로 작용하는 베타-카복시에틸-로다닌 유도체 또는 약학적으로 허용되는 이의 염이 제공된다. 본 발명에 따른 베타-카복시에틸-로다닌 유도체는 PPARγ를 조절하는 작용을 가짐으로써 PPAR에 의해 매개되는 당뇨병, 고혈압, 동맥경화증, 심혈관계 질환, 대사성질환 등에 대하여 예방, 개선 및 치료효과를 나타낼 수 있다.
PPARγ, PPARγ활성제, 로다닌 유도체, 베타-카복시에틸-로다닌 유도체, PPARγ 매개 질환, 당뇨병, 대사성질환

公开(公告)号：KR101275770B1

公开(公告)日：2013-06-14

申请号：KR1020100015380

申请日：2010-02-19

Applicant: 숙명여자대학교산학협력단

Inventor： 전라옥 ,  류재하 ,  김효진 ,  강보미 ,  장희련 ,  이다연

IPC: C07D209/04 ,  C07D209/02 ,  A61K31/40 ,  A61P3/10

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。

公开(公告)号：KR1020100086713A

公开(公告)日：2010-08-02

申请号：KR1020090006090

申请日：2009-01-23

Applicant: 숙명여자대학교산학협력단

Inventor： 윤석준 ,  양영 ,  전라옥 ,  최지원 ,  김성화 ,  강보미 ,  박연선 ,  고윤애

IPC: C07D277/36 ,  C07D277/32 ,  A61P3/10 ,  A61P9/12

Abstract: PURPOSE: A novel rhodanine derivative which activates PPAR gamma is provided to prevent or treat PPAR-mediated diseases. CONSTITUTION: A beta-rhodanine derivative is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating PPAR gamma-mediated diseases contains beta-carboxyethyl-rhodanine derivative or pharmaceutically acceptable salt as an active ingredient. The PPAR gamma-mediated diseases are diabetes, hypertension, artery scleroma, cardiovascular disease or metabolic disorder.

Abstract translation: 目的：提供激活PPARγ的新型罗丹明衍生物，以预防或治疗PPAR介导的疾病。 构成：β-绕丹宁衍生物由化学式1表示。用于预防和治疗PPARγ介导的疾病的药物组合物含有β-羧乙基 - 绕丹宁衍生物或药学上可接受的盐作为活性成分。 PPARγ介导的疾病是糖尿病，高血压，动脉硬化，心血管疾病或代谢紊乱。