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
    3.
    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。

    암의 예방 또는 치료를 위한 카지놀 C의 용도
    6.
    发明公开
    암의 예방 또는 치료를 위한 카지놀 C의 용도 有权
    使用KAZINOL C治疗或预防癌症

    公开(公告)号:KR1020160069425A

    公开(公告)日:2016-06-16

    申请号:KR1020140175370

    申请日:2014-12-08

    CPC classification number: A61K31/045 A61K31/05 A61K36/60 Y10S514/908

    Abstract: 본발명은카지놀 C를포함하는암 질환예방및 치료를위한약제학적조성물및 암질환예방및 개선을위한건강기능식품에관한것으로, 보다구체적으로는닥나무에서유래한화학식 1의카지놀 C를유효성분으로포함한다. 상기발명은카지놀 C가세포내에서 AMPK의활성을증가시켜암세포의세포사멸을촉진하고, 세포이동및 비부착성성장을억제하여암 질환을예방및 치료또는개선하는효과를갖는다.

    Abstract translation: 本发明涉及一种用于预防和治疗癌症的药物组合物,其包含kazinol C,以及涉及用于预防和减轻癌症的保健功能性食品,更具体地,涉及包含源自Broussonetia kazinoki的化学式1的kazinol C作为活性成分。 本发明的kazinol C通过增加细胞内的AMPK活性来促进癌细胞的凋亡,并通过抑制非粘性生长和细胞移动来预防,治疗或减轻癌症的作用。

    플라반계 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 갱년기 증후군 또는 골다공증의 예방 및 치료용 약학적 조성물
    8.
    发明公开
    플라반계 화합물 또는 이의 약학적으로 허용가능한 염을 유효성분으로 함유하는 갱년기 증후군 또는 골다공증의 예방 및 치료용 약학적 조성물 有权
    用于预防和治疗包含FLAVAN化合物的男性症状或卵泡病的药物组合物或其作为活性成分的药物可接受的盐

    公开(公告)号:KR1020110133277A

    公开(公告)日:2011-12-12

    申请号:KR1020100052916

    申请日:2010-06-04

    Abstract: PURPOSE: A pharmaceutical composition containing flavan compounds or pharmaceutically acceptable salt thereof is provided to prevent and treat osteoporosis. CONSTITUTION: A pharmaceutical composition for preventing or treating climacteric syndrome or osteoporosis contains flavan compounds of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A health food composition for preventing climacteric syndrome or osteoporosis contains flavan compound of chemical formula 1 as an active ingredient. An isoprenylated flavan compound is denoted by chemical formula 1.

    Abstract translation: 目的:提供含有黄烷化合物或其药学上可接受的盐的药物组合物以预防和治疗骨质疏松症。 构成:用于预防或治疗更年期综合征或骨质疏松症的药物组合物含有化学式1的黄烷化合物或其药学上可接受的盐作为活性成分。 用于预防更年期综合征或骨质疏松症的保健食品组合物含有化学式1的黄烷化合物作为活性成分。 异戊二烯基黄烷化合物由化学式1表示。

    활성화된 대식세포에 의해 유도된 iNOS의 NO 생성 저해활성을 갖는 페닐이소티오우레아 유도체
    9.
    发明公开
    활성화된 대식세포에 의해 유도된 iNOS의 NO 생성 저해활성을 갖는 페닐이소티오우레아 유도체 有权
    作为LPS活化突变体中不产生生物活性物质的苯基衍生物衍生物的合成

    公开(公告)号:KR1020110035195A

    公开(公告)日:2011-04-06

    申请号:KR1020090092811

    申请日:2009-09-30

    Abstract: PURPOSE: A phenylisothiourea derivative is provided to enable use as a material for the development of therapeutic agents for diseases caused by excessive formation of NO. CONSTITUTION: A phenylisothiourea derivative or pharmaceutically is represented by chemical formula 1. In chemical formula 1, R^1 is C1~10 alkyl, aryl, C1~10 alkoxy, hydroxyl, halogen or carbazolylethoxy; R^2 is C1~10 alkyl, benzyl or substituted benzyl; R^3 is H or C1~10 alkyl. A method for synthesizing the phenylisothiourea derivative comprises the steps of: (i) polycondensing p-substituted aniline as a starting material with isocyanate to obtain phenylthiourea; and (ii) introducing alkyl or aryl group to phenylthiourea.

    Abstract translation: 目的:提供苯基异硫脲衍生物,以使其能够用于开发过量形成NO引起的疾病的治疗剂。 构成:苯基异硫脲衍生物或药学上由化学式1表示。在化学式1中,R 1是C 1-10烷基,芳基,C 1-10烷氧基,羟基,卤素或咔唑基聚乙氧基; R 2是C 1-10烷基,苄基或取代的苄基; R 3是H或C 1-10烷基。 合成苯基异硫脲衍生物的方法包括以下步骤:(i)使用异氰酸酯作为起始原料缩聚对取代的苯胺,得到苯基硫脲; 和(ii)将烷基或芳基引入苯基硫脲。

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