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