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。

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）。

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。

公开(公告)号：KR1020090022070A

公开(公告)日：2009-03-04

申请号：KR1020070087122

申请日：2007-08-29

Applicant: 한국화학연구원

Inventor： 공영대 ,  전문국 ,  이태호 ,  황순희 ,  이상한 ,  허진철

IPC: C07D311/04 ,  A61K31/353

Abstract: A pharmaceutical composition for inhibiting oxidative stress is provided to treat Alzheimer's diseases and cerebral apoplexy by using a 2-methyl-2'-hydroxymethyl-6-amidobenzopyran derivative and its salts. A pharmaceutical composition for inhibiting oxidative stress comprises a 2-methyl-2'-hydroxymethyl-6-amidobenzopyran derivative represented by the formula 1. A method for manufacturing the 2-methyl-2'-hydroxymethyl-6-amidobenzopyran derivative consists of the following steps of manufacturing a 6-amino benzopyran derivative represented by the formula 3 by reducing a 6-nitrobenzopyran derivative represented by the formula 2 with 1.0-3.0 mole equivalent of reductant.

Abstract translation: 提供一种用于抑制氧化应激的药物组合物，通过使用2-甲基-2'-羟甲基-6-氨基苯并吡喃衍生物及其盐来治疗阿尔茨海默病和脑中风。 用于抑制氧化应激的药物组合物包含由式1表示的2-甲基-2'-羟甲基-6-氨基苯并吡喃衍生物。制备2-甲基-2'-羟甲基-6-氨基苯并吡喃衍生物的方法包括以下 通过用1.0-3.0摩尔当量的还原剂还原由式2表示的6-硝基苯并吡喃衍生物制备由式3表示的6-氨基苯并吡喃衍生物的步骤。