公开(公告)号：KR1020150049698A

公开(公告)日：2015-05-08

申请号：KR1020130130569

申请日：2013-10-30

Applicant: 동국대학교 산학협력단 ,  한국화학연구원

Inventor： 공영대 ,  양승주 ,  김성환

IPC: C07D271/10 ,  A61K31/4245 ,  A61P35/00

Abstract: 본발명은우수한 Wnt 유전자발현억제활성을가지는하기화학식 1로표시되는신규 2-아미노치환옥사디아졸유도체, 이의약학적으로허용가능한염, 및이의제조방법및 이를유효성분으로포함하는암의예방또는치료용약학적조성물을제공하기위한것이다. [화학식 1]상기식에서, R및 R의정의는명세서에서정의한바와같다.

Abstract translation: 本发明提供：由化学式1表示的新的2-氨基取代的恶二唑衍生物，具有优异的Wnt基因表达控制活性; 其药学上可允许的盐; 其制造方法; 以及包含其作为预防或治疗癌症的活性成分的药物组合物。 [化学式1]在式中，R 1和R 2与说明书中定义相同。

公开(公告)号：KR101097177B1

公开(公告)日：2011-12-22

申请号：KR1020060063214

申请日：2006-07-06

Applicant: 제이더블유중외제약 주식회사 ,  한국화학연구원

Inventor： 이수진 ,  공영대 ,  전문국 ,  문성환 ,  전기호 ,  김종민 ,  이상휘 ,  이상학 ,  강명주

IPC: C07D471/04

CPC classification number: Y02P20/55

Abstract: 상기화학식 1에서, A, Y 및 Z는각각발명의상세한설명에서정의한바와같다.

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：KR100889839B1

公开(公告)日：2009-03-20

申请号：KR1020070096340

申请日：2007-09-21

Applicant: 한국화학연구원 ,  고려대학교 산학협력단

Inventor： 공영대 ,  전문국 ,  황순희 ,  동미숙 ,  이상범 ,  강경호 ,  오칠환

IPC: C07D241/44 ,  C07D401/12 ,  C07D413/12 ,  C07D403/12

Abstract: Provided is a 2-substituted aminoalkylenyloxy-3-substituted phenylethynyl quinoxaline derivative, capable of suppressing expression of a WNT gene and proliferation of a cancer cell. A 2-substituted aminoalkylenyloxy-3-substituted phenylethynyl quinoxaline derivative is represented by the formula 1. In the formula 1, Y and Z is independently a hydrogen atom, halogen atom, C1-C8 alkyl group, or a C1-C8 alkoxy group; and R shows -X-Het. or -X-NR1R2, in which X is a C1-C8 alkylene group or a C2-C8 alkylene oxyalkylene group, and R1 and R2 is independently a hydrogen atom, C1-C8 alkyl group, or a pentagon or heptagon hetero group in which a hetero atom selected from another nitrogen atom or an oxygen atom with the nitrogen boned to the R1 and R2 is included.

Abstract translation: 提供能够抑制WNT基因表达和癌细胞增殖的2-取代氨基亚烷基氧基-3-取代苯基乙炔基喹喔啉衍生物。 2-取代的氨基亚烷基氧基-3-取代的苯基乙炔基喹喔啉衍生物由式1表示。在式1中，Y和Z独立地为氢原子，卤素原子，C1-C8烷基或C1-C8烷氧基; R表示-X-Het。 或-X-NR 1 R 2，其中X为C 1 -C 8亚烷基或C 2 -C 8亚烷基氧化烯基，R 1和R 2独立地为氢原子，C 1 -C 8烷基或五价或七价杂原子，其中 包括选自另一个氮原子或氧原子的杂原子，其中氮与B和R 2结合。

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。

公开(公告)号：KR100704009B1

公开(公告)日：2007-04-04

申请号：KR1020050080383

申请日：2005-08-30

Applicant: 한국화학연구원

Inventor： 공영대 ,  천혜경 ,  전문국 ,  조영식 ,  황종연 ,  최형섭 ,  전현숙 ,  황순희 ,  송진숙 ,  김지현 ,  유성은

IPC: C07D311/70 ,  C07D409/12 ,  C07D401/12

CPC classification number: C07D311/58 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

Abstract: 본 발명은 신규 6-알킬아미노-2-메틸-2'-(
N- 메틸치환술폰아미도)메틸-2
H- 1-벤조피란 유도체와, 조합화학 합성기술 중 하나인 평형합성법을 이용하여 상기한 신규 화합물을 고효율로 합성하는 방법, 그리고 상기한 신규 화합물이 우수한 5-라이폭시게네이즈(5-LO) 저해효과를 나타내므로 관련 류코트리엔(LTA4, B4, C4, D4)의 활성으로 유발되는 염증질환, 류마티스성 관절염, 대장염(Colitis), 천식, 건선 등의 예방 및 치료제로 사용하는 용도에 관한 것이다.
조합화학 합성, 평형 합성, 5-라이폭시게네이즈, 항염증 질환 치료제, 약리학적 효능, 2'-술폰아미도메틸벤조피란, 유사약물 라이브러리

公开(公告)号：KR1020070024838A

公开(公告)日：2007-03-08

申请号：KR1020050080383

申请日：2005-08-30

Applicant: 한국화학연구원

Inventor： 공영대 ,  천혜경 ,  전문국 ,  조영식 ,  황종연 ,  최형섭 ,  전현숙 ,  황순희 ,  송진숙 ,  김지현 ,  유성은

IPC: C07D311/70 ,  C07D409/12 ,  C07D401/12

CPC classification number: C07D311/58 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14

Abstract: A novel 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative is provided to show excellent 5-lipoxygenase(5-LO) inhibition effect, thereby being used for preventing and treating inflammatory diseases induced by related leukotrien(LTA4, B4, C4, D4), rheumatoid arthritis, colitis, asthma, and psoriasis. The 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative is represented by the formula(1), where R^1 is C1-10 alkyl; phenyl; phenyl substituted by a substituent selected from the group consisting of C1-6 alkyl, C1-6 acyloxy, C1-10 alkoxyalkyl, and C1-10 dialkoxyalkyl; benzyl; benzyl substituted by a substituent selected from the group consisting of halogen, nitro, cyano, hydroxy, C1-6 alkyl and C1-6 alkoxy; phenethyl; pyridyl methyl; thiophene methyl; or thiophene methyl substituted by C1-6 alkyl, each R^2 and R^3 is independently H; or C1-6 alkyl, and R^4 is C1-10 alkyl; phenyl; phenyl substituted by a substituent selected from the group consisting of C1-6 alkyl and C1-6 alkoxy; or thiophene. The anti-inflammatory agent comprises the 6-alkylamino-2-methyl-2-(N-methyl substituted sulfonamido)methyl-2H-1-benzopyran derivative represented by the formula(1).

Abstract translation: 提供新的6-烷基氨基-2-甲基-2-（N-甲基取代亚磺酰氨基）甲基-2H-1-苯并吡喃衍生物，以显示出优异的5-脂氧合酶（5-LO）抑制作用，从而用于预防和治疗 由相关白细胞介素（LTA4，B4，C4，D4），类风湿关节炎，结肠炎，哮喘和牛皮癣引起的炎性疾病。 6-烷基氨基-2-甲基-2-（N-甲基取代亚磺酰氨基）甲基-2H-1-苯并吡喃衍生物由式（1）表示，其中R 1是C 1-10烷基; 苯基; 被选自C 1-6烷基，C 1-6酰氧基，C 1-10烷氧基烷基和C 1-10二烷氧基烷基的取代基取代的苯基; 苄基; 被选自卤素，硝基，氰基，羟基，C 1-6烷基和C 1-6烷氧基的取代基取代的苄基; 苯; 吡啶基甲基; 噻吩甲基; 或被C 1-6烷基取代的噻吩甲基，每个R 2和R 3独立地为H; 或C 1-6烷基，R 4是C 1-10烷基; 苯基; 被选自C 1-6烷基和C 1-6烷氧基的取代基取代的苯基; 或噻吩。 抗炎剂包含式（1）表示的6-烷基氨基-2-甲基-2-（N-甲基取代亚磺酰氨基）甲基-2H-1-苯并吡喃衍生物。

公开(公告)号：KR100666207B1

公开(公告)日：2007-01-09

申请号：KR1020050022826

申请日：2005-03-18

Applicant: 한국화학연구원

Inventor： 공영대 ,  전문국 ,  이일영 ,  황종연 ,  조희영 ,  공재양

IPC: C07D311/70 ,  C07D409/12

Abstract: 본 발명은 RTK(Receptor Tyrosine Kinase; 수용체 티로신 효소) 저해활성이 우수한 다음 화학식 1로 표시되는 6-알킬아미노-2,2'-이중치환-벤조피란 유도체와 이의 이성질체, 및 약제학적으로 허용 가능한 이의 염을 항암제로서 사용하는 용도에 관한 것이다.

상기 화학식 1에서, R
1 , R
2 , R
3 , R
4 , n은 각각 발명의 상세한 설명에서 정의한 바와 같다.
아미노벤조피란, 수용체 티로신 효소, 상피세포, 항암제, RTK