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    다불소알킬기를 가진 트리아졸릴쿠마린 유도체, 그 제조방법 및 그의 용도
    55.
    发明公开
    다불소알킬기를 가진 트리아졸릴쿠마린 유도체, 그 제조방법 및 그의 용도 有权
    具有氟烷基的TRIAZOLYLCOUMARIN衍生物及其制备和使用方法

    公开(公告)号：KR1020120100646A

    公开(公告)日：2012-09-12

    申请号：KR1020110019697

    申请日：2011-03-04

    Applicant: 한국화학연구원

    Inventor： 전문국 ,  강명구

    IPC: C07D405/04 ,  G01N33/58 ,  G01N33/52

    CPC classification number: Y02P20/55 ,  C07D405/04 ,  G01N33/582

    Abstract: PURPOSE: A method for preparing triazolylcoumarin derivatives with novel fluorous alkyl groups is provided to enable fixation, fixation monitoring, and organic low molecular compound attachment. CONSTITUTION: A triazolylcoumarin derivative is denoted by chemical formula 1. In chemical formula 1: A, B, and D are alkylene group of 1-6 carbon atoms; a is 5-9 integer; and b is 2-5 integer. A method for preparing the derivative comprises: a step of reacting methyl 7-ethynyl coumarin-4-acetate of chemical formula 2 with azide with the fluorous alkyl group of chemical formula 3 to prepare 7-triazolyl coumarin-4-acetate of chemical formula 4; a step of ester hydrolysis of the compound of chemical formula 4 to prepare a fluorous alkyl group-substituted 7-triazolyl coumarin-4-acetic acid of chemical formula 5; a step of reacting the compound of chemical formula 5 with diamine with a protection group of chemical formula 6 to prepare fluorous alkyl group-substituted 7-triazolyl coumarin-4-acetamide; and a step of deprotecting the compound of chemical formula 7 to prepare triazolylcoumarin of chemical formula 1.

    Abstract translation: 目的：提供一种用新型氟烷基制备三唑基香豆素衍生物的方法，以使固定，固定监测和有机低分子化合物附着。 构成：三唑基香豆素衍生物由化学式1表示。化学式1中，A，B和D为1-6个碳原子的亚烷基; a为5-9整数; b为2-5整数。 制备衍生物的方法包括：使化学式2的7-乙炔基香豆素-4-乙酸甲酯与叠氮化物与化学式3的氟烷基反应以制备化学式4的7-三唑基香豆素-4-乙酸酯的步骤 ; 化学式4的化合物的酯水解步骤以制备化学式5的氟烷基取代的7-三唑基香豆素-4-乙酸; 使化学式5的化合物与二胺与化学式6的保护基反应以制备氟烷基取代的7-三唑基香豆素-4-乙酰胺的步骤; 以及使化学式7的化合物脱保护以制备化学式1的三唑基香豆素的步骤。

    1-(6,7-다이플루오르-3-메톡시퀴녹살린-2-일)-3-［1-(헤테로아릴메틸)피페리딘-4-일］ 우레아 유도체, 그 제조방법 및 그의 용도
    57.
    发明公开
    1-(6,7-다이플루오르-3-메톡시퀴녹살린-2-일)-3-［1-(헤테로아릴메틸)피페리딘-4-일］ 우레아 유도체, 그 제조방법 및 그의 용도 有权
    1-（6,7-二氟-3-甲氧基喹啉-2-基）-3- [1-（异丁基甲基）哌啶-4-基]脲衍生物及其药学上可接受的盐，其制备和使用方法

    公开(公告)号：KR1020110094566A

    公开(公告)日：2011-08-24

    申请号：KR1020100014043

    申请日：2010-02-17

    Applicant: 한국화학연구원

    Inventor： 전문국 ,  이태호 ,  황순희 ,  이지민 ,  유성은 ,  이병호 ,  오광석 ,  공영대 ,  이승호

    IPC: C07D403/12 ,  C07D413/14 ,  A61P3/04

    Abstract: PURPOSE: A 1-(6,7-difluoro-3-methoxyquinoxaline-2-yl)-3-[1-(heteroarylmethyl)piperidine-4-yl]urea derivatives is provided to suppress MCH1R and to prevent and treat obesity without side effects. CONSTITUTION: A 1-(6,7-difluoro-3-methoxyquinoxaline-2-yl)-3-[1-(heteroarylmethyl)piperidine-4-yl]urea derivative is denoted by chemical formula 1. The compound of chemical formula 1 is prepared by reduction alkylation of a compound of chemical formula 5 with heteraryl aldehyde compound of chemical formula 6. A MCH1R inhibitor composition contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient. A pharmaceutical composition for preventing and treating obesity contains the compound of chemical formula 1 or pharmaceutically acceptable salt thereof as an active ingredient.

    Abstract translation: 目的：提供1-（6,7-二氟-3-甲氧基喹喔啉-2-基）-3- [1-（杂芳基甲基）哌啶-4-基]脲衍生物以抑制MCH1R并预防和治疗无侧面肥胖 效果。 构成：化学式1表示1-（6,7-二氟-3-甲氧基喹喔啉-2-基）-3- [1-（杂芳基甲基）哌啶-4-基]脲衍生物。化学式1的化合物 通过用化学式6的杂芳基醛化合物将化学式5的化合物还原烷基化制备.MCH1R抑制剂组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。 用于预防和治疗肥胖症的药物组合物含有化学式1的化合物或其药学上可接受的盐作为活性成分。

    2-메틸-2Ｈ-크로멘-2-카르복사미드 화합물
    58.
    发明公开
    2-메틸-2Ｈ-크로멘-2-카르복사미드 화합물 有权
    2-甲基-2H-色烯-2-羧酰胺化合物

    公开(公告)号：KR1020110012090A

    公开(公告)日：2011-02-09

    申请号：KR1020090069647

    申请日：2009-07-29

    Applicant: 한국화학연구원 ,  에스케이케미칼주식회사

    Inventor： 공영대 ,  조희영 ,  이태호 ,  최길돈 ,  전문국 ,  박우규 ,  공재양 ,  황순희 ,  정대영 ,  이봉용 ,  엄기안 ,  김재선 ,  류근호 ,  류제호 ,  김신애 ,  한혜영 ,  손현주 ,  이현정 ,  김용혁 ,  박성훈

    IPC: C07D311/24 ,  C07D311/16 ,  C07D311/12

    Abstract: PURPOSE: A 2-methyl-2H-chromen-2-carboxamide compound is provided to ensure selective suppression to 11beta-HSD1 enzyme and prevent and treat glucocorticoid regulatory disease. CONSTITUTION: A 2-methyl-2H-chromen-2-carboxamide compound is denoted by chemical formula 1. A pharmaceutical composition contains the 2-methyl-2H-chromen-2-carboxamide compound. The pharmaceutical composition is used for treating and preventing type 1 and 2 diabetes, injured glucose resistance, hyperlipidemia or hypertension. The 2-methyl-2H-chromen-2-carboxamide compound in which an amide is induced is obtained by condensing R1-substituted 2-methyl-2H-chromen-2-carboxy acid compound of chemical formula 2 with amine compound(NHR^2R^3).

    Abstract translation: 目的：提供2-甲基-2H-色烯-2-甲酰胺化合物，以确保对11beta-HSD1酶的选择性抑制，并预防和治疗糖皮质激素调节性疾病。 构成：2-甲基-2H-色烯-2-甲酰胺化合物由化学式1表示。药物组合物含有2-甲基-2H-色烯-2-甲酰胺化合物。 药物组合物用于治疗和预防1型和2型糖尿病，葡萄糖耐量受损，高脂血症或高血压。 通过将化学式2的R1取代的2-甲基-2H-色烯-2-羧酸化合物与胺化合物（NHR 2 R 2） ^ 3）。

    2-(2-아미도메틸)-2-메틸-2Ｈ-벤조피란 화합물
    59.
    发明公开
    2-(2-아미도메틸)-2-메틸-2Ｈ-벤조피란 화합물 有权
    2-（2-氨基甲基）-2-甲基-2H-苯并噻吩化合物

    公开(公告)号：KR1020110012089A

    公开(公告)日：2011-02-09

    申请号：KR1020090069646

    申请日：2009-07-29

    Applicant: 한국화학연구원 ,  에스케이케미칼주식회사

    Inventor： 공영대 ,  조희영 ,  이태호 ,  최길돈 ,  전문국 ,  박우규 ,  공재양 ,  황순희 ,  정대영 ,  이봉용 ,  엄기안 ,  김재선 ,  류근호 ,  류제호 ,  김신애 ,  한혜영 ,  손현주 ,  이현정 ,  김용혁 ,  박성훈

    IPC: C07D311/58 ,  C07D311/04 ,  C07D311/02

    Abstract: PURPOSE: A 2-(2-amido methyl)-2-methyl-2H-benzypyrane compound is provided to ensure selective suppression to 11 beta-HSD 1 enzyme and to prevent and treat clucocorticoid regulatory diseases. CONSTITUTION: A 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is denoted by chemical formula 1. The 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound is 3-methoxy-N-methyl-N-[(2-methyl-8-nitro-2H-chromen-2-yl)methyl]benzamide or 3-chloro-N-[(2,6-dimethyl-2H-chromen-2-yl)methyl]-N-methylbenzamide. A pharmaceutical composition contains the 2-(2-amido methyl)-2-methyl-2H-benzopyrane compound and prevents and treats impaired glucose tolerance(IGT), type 1 and 2 diabetes, insulin resistance, dyslipidemia or hypertension.

    Abstract translation: 目的：提供2-（2-氨基甲基）-2-甲基-2H-苯并吡喃化合物，以确保对11β-HSD 1酶的选择性抑制，并预防和治疗类皮质激素调节性疾病。 构成：2-（2-氨基甲基）-2-甲基-2H-苯并吡喃化合物由化学式1表示。2-（2-酰氨基甲基）-2-甲基-2H-苯并吡喃化合物是3-甲氧基 - N-甲基-N - [（2-甲基-8-硝基-2H-色烯-2-基）甲基]苯甲酰胺或3-氯-N - [（2,6-二甲基-2H-色烯-2-基） 甲基] -N-甲基苯甲酰胺。 药物组合物含有2-（2-酰氨基甲基）-2-甲基-2H-苯并吡喃化合物，并预防和治疗葡萄糖耐量异常（IGT），1型和2型糖尿病，胰岛素抵抗，血脂异常或高血压。

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