公开(公告)号：KR1020130016041A

公开(公告)日：2013-02-14

申请号：KR1020120041622

申请日：2012-04-20

Applicant: 재단법인 의약바이오컨버젼스연구단

Inventor： 김성훈 ,  권남훈 ,  이희숙 ,  오영선 ,  김대규

IPC: C07C233/65 ,  C07C229/38 ,  A61K31/166 ,  A61P35/00

CPC classification number: C07C235/74 ,  A61K31/167 ,  A61P35/00 ,  C07C233/04 ,  C07C233/07 ,  C07C233/09 ,  C07C233/15 ,  C07C233/25 ,  C07C233/27 ,  C07C235/76 ,  C07C2603/24

Abstract: PURPOSE: An aniline derivative is provided to be effective for preventing and treating cancer by effectively deriving the death of a cancer cell through decreasing the activity of AIMP2-DX2. CONSTITUTION: An aniline derivative and a pharmaceutically acceptable salt is represented by chemical formula 1. In chemical formula 1, Each of R1-R5 is selected from hydrogen, a C1-4 linear, branched, or cyclic alkyl, halogen, alkoxy, and hydroxy; R6 is -C(=O)-CH=CH-C(=O)R7 or -C(=O)-CHR9-C(=O)R8; R7 is a hydroxy or a functional group indicated in chemical formula 1-A; R8 is a C1-6 alkoxy or a functional group indicated in chemical formula 1-B; R9 is a hydrogen or C1-6 alkyl; and each of R10-R14 is selected from hydrogen, methyl, halogen, and methoxy.

Abstract translation: 目的：提供苯胺衍生物，通过降低AIMP2-DX2的活性，有效地导致癌细胞的死亡，从而有效预防和治疗癌症。 构成：苯胺衍生物和药学上可接受的盐由化学式1表示。在化学式1中，R 1 -R 5各自选自氢，C 1-4直链，支链或环状的烷基，卤素，烷氧基和羟基 ; R6是-C（= O）-CH = CH-C（= O）R7或-C（= O）-CHR9-C（= O）R8; R7是化学式1-A表示的羟基或官能团; R8是C1-6烷氧基或化学式1-B所示的官能团; R9是氢或C1-6烷基; R 10 -R 14选自氢，甲基，卤素和甲氧基。

公开(公告)号：KR1020130118612A

公开(公告)日：2013-10-30

申请号：KR1020120041623

申请日：2012-04-20

Applicant: 재단법인 의약바이오컨버젼스연구단

Inventor： 김성훈 ,  권남훈 ,  이희숙 ,  오영선 ,  김대규

IPC: C07D213/75 ,  C07D215/38 ,  A61K31/435 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4706

CPC classification number: C07D215/38 ,  A61K31/435 ,  C07D213/75 ,  A61K31/44 ,  A61K31/47 ,  A61K31/4706

Abstract: PURPOSE: A novel aminopyridine derivative is provided to suppress the activity of AIMP2-DX2 which is a new target of an anticancer agent and to effectively induce apoptosis of cancer cells, thereby effectively preventing and treating cancer. CONSTITUTION: An aminopyridine derivative of chemical formula 1 or a pharmaceutically acceptable salt thereof is provided. A pharmaceutical composition for preventing or treating cancer contains the aminopyridine derivative of chemical formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient. The derivative is selected among ethyl 3-[(5-chloropyridine-2-yl)amino]-2-methyl-3-oxopropanoate, ethyl 3-[(6-methylpyridine-2-yl)amino]-3-oxopropanoate, ethyl 3-oxo-3-(quinoline-3-ylamino) propanoate, ethyl 3-[(3,6-dimethylpyridine-2-yl)amino]-3-oxopropanoate, ethyl 3-[(4-hydroxypyridine-2-yl)amino]-3-oxopropanoate, ethyl 2-methyl-3-oxo-3-(quinoline-3-ylamino) propanoate, ethyl 2-methyl-3-[(6-methylpyridine-2-yl)amino]-3-oxopropanoate, and ethyl 3-[(5-chloropyridine-2-yl)amino]-3-oxopropanoate.

Abstract translation: 目的：提供一种新的氨基吡啶衍生物，以抑制作为抗癌剂新靶标的AIMP2-DX2的活性，有效诱导癌细胞凋亡，从而有效预防和治疗癌症。 构成：提供化学式1的氨基吡啶衍生物或其药学上可接受的盐。 用于预防或治疗癌症的药物组合物含有化学式1的氨基吡啶衍生物或其药学上可接受的盐作为活性成分。 该衍生物选自3 - [（5-氯吡啶-2-基）氨基] -2-甲基-3-氧代丙酸乙酯，3 - [（6-甲基吡啶-2-基）氨基] -3-氧代丙酸乙酯，乙基 3-（3-喹啉-3-基氨基）丙酸乙酯，3 - [（3,6-二甲基吡啶-2-基）氨基] -3-氧代丙酸乙酯，3 - [（4-羟基吡啶-2-基） 氨基] -3-氧代丙酸乙酯，2-甲基-3-氧代-3-（喹啉-3-基氨基）丙酸乙酯，2-甲基-3 - [（6-甲基吡啶-2-基）氨基] -3-氧代丙酸乙酯 ，和3 - [（5-氯吡啶-2-基）氨基] -3-氧代丙酸乙酯。

公开(公告)号：KR1020130016134A

公开(公告)日：2013-02-14

申请号：KR1020120085685

申请日：2012-08-06

Applicant: 재단법인 의약바이오컨버젼스연구단

Inventor： 김성훈 ,  이희숙 ,  오영선 ,  김대규

IPC: C07C233/07 ,  C07C233/09 ,  C07C233/15 ,  C07C233/25 ,  C07C233/27 ,  A61K31/167

CPC classification number: C07C235/74 ,  A61K31/167 ,  A61P35/00 ,  C07C233/04 ,  C07C233/07 ,  C07C233/09 ,  C07C233/15 ,  C07C233/25 ,  C07C233/27 ,  C07C235/76 ,  C07C2603/24

Abstract: PURPOSE: An aniline derivative is provided to effectively derive the death of cancer cells by reducing the activity of AIMP2-DX2 which is a target for a new anticancer drug. CONSTITUTION: An aniline derivative is indicated in chemical formula 1. In the chemical formula 1: each of R1-R5 is selected from hydrogen, C1-C4 linear, branched or cyclic alkyl, halogen, alkoxy, and hydroxy; R6 is -CO-CH=CH-COR7 or -CO-CHR9-COR8; R7 is a hydroxy or a functional group indicated in chemical formula 1-a; R8 is a C1-6 alkoxy or a functional group indicated in chemical formula 1-b; R9 is hydrogen or a C1-6 alkyl; and each of R10-R14 is selected from hydrogen, methyl, halogen, and methoxy.

Abstract translation: 目的：提供苯胺衍生物，通过降低作为新抗癌药物靶标的AIMP2-DX2的活性来有效地导致癌细胞的死亡。 化学式1表示苯胺衍生物：化学式1：R1-R5各自选自氢，C1-C4直链，支链或环状烷基，卤素，烷氧基和羟基; R6是-CO-CH = CH-COR7或-CO-CHR9-COR8; R7是化学式1-a所示的羟基或官能团; R8是C1-6烷氧基或化学式1-b表示的官能团; R9为氢或C1-6烷基; R 10 -R 14选自氢，甲基，卤素和甲氧基。