公开(公告)号：WO2018008920A1

公开(公告)日：2018-01-11

申请号：PCT/KR2017/007021

申请日：2017-07-03

Applicant: 한국과학기술연구원

Inventor： 마흐무드가말엘딘 ,  최홍석 ,  유경호 ,  한동근 ,  오창현 ,  무함마드아브델막수드 ,  무함마드아이. 엘가말

IPC: C07D498/04 ,  C07D513/04 ,  C07D417/14 ,  A61K31/424 ,  A61K31/429 ,  A61K31/433 ,  A61K31/506

Abstract: 이미다조옥사졸 유도체 화합물, 용매화물, 입체 이성질체 또는 이들의 약학적으로 허용가능한 염을 유효성분으로 포함하는 종양 예방 및 치료용 약학적 조성물을 제공하여, 이를 종양에 걸리거나 걸릴 위험이 있는 개체에 투여함으로써 종양을 예방 또는 치료할 수 있다.

Abstract translation: 一种用于预防和治疗肿瘤的药物组合物，其包含咪唑并唑衍生物化合物，其溶剂合物，立体异构体或药学可接受的盐作为活性成分， 通过向可能被捕或被捕的人施用，可以预防或治疗肿瘤。

公开(公告)号：KR101948805B1

公开(公告)日：2019-02-15

申请号：KR1020160085062

申请日：2016-07-05

Applicant: 한국과학기술연구원

Inventor： 가말엘딘마흐무드 ,  최홍석 ,  유경호 ,  한동근 ,  오창현 ,  아브델막수드무함마드 ,  엘가말무함마드

IPC: C07D498/04 ,  C07D513/04 ,  C07D417/14 ,  A61K31/424 ,  A61K31/429 ,  A61K31/433 ,  A61K31/506

公开(公告)号：KR1020140029594A

公开(公告)日：2014-03-11

申请号：KR1020120094447

申请日：2012-08-28

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  한동근 ,  유승원

IPC: C07D405/14 ,  A61K31/41 ,  A61K31/4178 ,  A61P9/12

Abstract: The present invention relates to a purification method of olmesartan medoxomil which comprises the following simple steps: dissolving the olmesartan medoxomil in a mixed solvent of halogenated alkane, and low class alcohol or low class ketone; and removing the halogenated alkane before crystalizing. The halogenated alkane is one or more compound selected from chloroform, methylene chloride, chlorodifluoromethane, dichlorofluoromethane, 1,1,2,2-tetrachloroethane, 1,1,1,2-tetrachloroethane, and ethylene chloride.

Abstract translation: 本发明涉及奥美沙坦酯的纯化方法，其包括以下简单步骤：将奥美沙坦酯在卤代烷烃和低级醇或低级酮的混合溶剂中溶解; 并在结晶之前除去卤代烷烃。 卤代烷烃是一种或多种选自氯仿，二氯甲烷，氯二氟甲烷，二氯氟甲烷，1,1,2,2-四氯乙烷，1,1,1,2-四氯乙烷和二氯乙烷的化合物。

公开(公告)号：KR1020120078687A

公开(公告)日：2012-07-10

申请号：KR1020120056983

申请日：2012-05-29

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  조정혁

IPC: C12P35/00 ,  A61K31/545

CPC classification number: C12P35/06 ,  A61K31/545 ,  C07B2200/13 ,  C07D501/16 ,  C12N9/84 ,  C12Y305/01011

Abstract: PURPOSE: A method for preparing a cephalosporin-based antibiotic intermediate is provided to industrially synthesize crystalline hydrate of the intermediate and to develop the antibiotics. CONSTITUTION: A method for preparing a cephalosporin-based antibiotic intermediate of chemical formula 1 comprises: a step of adding cresol and phenol to a compound of chemical formula 2 and stirring for deprotecting protection groups of a carboxyl group; a step of adding syntha CLEC-PA(cross-linked enzyme crystal-penicillin g amidase/acylase) while adjusting pH concentration using alkaline; a step of adjusting pH concentration using inorganic acid. The alkaline is hydrocarbon alkali metal, alkali hydroxide metal, ammonia solution, or trialkyl amine. The hydrocarbon alkali metal is sodium carbonate or potassium carbonate.

Abstract translation: 目的：提供一种制备头孢菌素类抗生素中间体的方法，以工业合成中间体的结晶水合物并开发抗生素。 构成：一种制备化学式1的头孢菌素类抗生素中间体的方法，包括：向化学式2的化合物中加入甲酚和苯酚并搅拌使羧基保护基团脱保护的步骤; 在使用碱性调节pH浓度的同时加入合成CLEC-PA（交联酶结晶 - 青霉素g酰胺酶/酰基转移酶）的步骤; 使用无机酸调节pH浓度的步骤。 碱性为烃类碱金属，碱金属氢氧化物，氨溶液或三烷基胺。 烃类碱金属是碳酸钠或碳酸钾。

公开(公告)号：KR1020120040980A

公开(公告)日：2012-04-30

申请号：KR1020100102522

申请日：2010-10-20

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  정명호 ,  엘가말모하메드 ,  유경호 ,  심태보 ,  최원경 ,  조정혁

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

Abstract: PURPOSE: A pyrrolo[3,2-c]pyridine derivative and a pharmaceutical composition containing the same are provided to ensure anti-proliferatioin activity of melanoma and to prevent or treat melanoma. CONSTITUTION: A pyrrolo[3,2-c]pyridine derivative is denoted by chemical formula I. A method for preparing the pyrrolo[3,2-c]pyridine derivative of chemical formula I' or pharmaceutically acceptable salt thereof comprises: a step of reacting 4-chloro-1-pyrrolo[2,3-b]pyridine of chemical formula II with nitroaniline to prepare a compound of chemical formula III; a step of reacting a compound of chemical formula III with benzoyl chloride to prepare a compound of chemical formula IV; a step of reducing the compound of chemical formula IV to prepare a compound of chemical formula V; and a step of reacting the compound of chemical formula V with a compound of chemical formula VI or formula VII.

Abstract translation: 目的：提供吡咯并[3,2-c]吡啶衍生物和含有它们的药物组合物，以确保黑色素瘤的抗增殖活性并预防或治疗黑素瘤。 构成：化学式I表示吡咯并[3,2-c]吡啶衍生物。制备化学式I'吡咯并[3,2-c]吡啶衍生物或其药学上可接受的盐的方法包括： 使化学式II的4-氯-1-吡咯并[2,3-b]吡啶与硝基苯胺反应制备化学式Ⅲ化合物; 使化学式III的化合物与苯甲酰氯反应以制备化学式IV的化合物的步骤; 降低化学式IV化合物以制备化学式V的化合物的步骤; 以及使化学式V的化合物与化学式VI或式VII的化合物反应的步骤。

公开(公告)号：KR101083421B1

公开(公告)日：2011-11-14

申请号：KR1020090055939

申请日：2009-06-23

Applicant: 한국과학기술연구원

Inventor： 하정미 ,  유경호 ,  심태보 ,  오창현 ,  유하나 ,  김환 ,  정윤경 ,  이정헌

IPC: C07D487/04 ,  C07D487/02 ,  A61K31/4188

Abstract: (상기화학식 1에서, R, R, R, R및 R는본 명세서에서정의된바와같다)

公开(公告)号：KR1020110019584A

公开(公告)日：2011-02-28

申请号：KR1020090077185

申请日：2009-08-20

Applicant: 한국과학기술연구원

Inventor： 심태보 ,  함영진 ,  유경호 ,  오창현 ,  하정미 ,  김환 ,  최환근 ,  이정헌

IPC: C07D209/04 ,  C07D403/04 ,  A61K31/40 ,  A61P29/00

CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

Abstract: PURPOSE: A 1,3,6-substituted indole compound having an activity of suppressing protein kinase is provided to suppress various protein kinases and to prevent and treat abnormal cell growth diseases. CONSTITUTION: A 1,3,6-substituted indole compound is denoted by chemical formula 1. A pharmaceutical composition contains 1,3,6-substituted indole compound of chemical formula 1 as an active ingredient. The pharmaceutical composition prevents and treats abnormal cell growth diseases through protein kinase suppression mechanism selected from Raf, KDR, Fms, Tie2, SAPK2a, Ret, Abl, Abl(T315I), ALK, Aurora A, Bmx, CDK/cyclinE, Kit, Src, EGFR, EphA1, FGFR3, Flt3, Fms, IGF-1R, IKKb, IR, Itk, JAK2, KDR, Met, mTOR, PDGFRa, Plk1, Ret, Syk, Tie2, and TrtB. An agent for preventing and treating tumor contains 1,3,6-substituted indole compound of chemical formula 1.

Abstract translation: 目的：提供具有抑制蛋白激酶活性的1,3,6-取代的吲哚化合物以抑制各种蛋白激酶并预防和治疗异常的细胞生长疾病。 构成：1,3,6-取代的吲哚化合物由化学式1表示。药物组合物含有化学式1的1,3,6-取代的吲哚化合物作为活性成分。 药物组合物通过选自Raf，KDR，Fms，Tie2，SAPK2a，Ret，Abl，Abl（T315I），ALK，Aurora A，Bmx，CDK / cyclinE，Kit，Src的蛋白激酶抑制机制预防和治疗异常细胞生长疾病 ，EGFR，EphA1，FGFR3，Flt3，Fms，IGF-1R，IKKb，IR，Itk，JAK2，KDR，Met，mTOR，PDGFRa，Plk1，Ret，Syk，Tie2和TrtB。 用于预防和治疗肿瘤的药物含有化学式1的1,3,6-取代的吲哚化合物。

公开(公告)号：KR1020100047998A

公开(公告)日：2010-05-11

申请号：KR1020080106962

申请日：2008-10-30

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  유경호 ,  심태보 ,  이소하 ,  하정미 ,  김희진 ,  정명호

IPC: C07D487/04

Abstract: PURPOSE: A novel pyrollo[3,2-b]pyridine derivative and a pharmaceutical composition for preventing or treating melanoma containing the same are provided to ensure high anti-proliferative activity to melanoma cells. CONSTITUTION: A pyrollo(3,2-b)pyridine derivative is denoted by chemical formula 1. A method for preparing the pirrolo(3,2,-b)pyridine derivative comprises: a step of coupling 1-iodine-4-nitrobenze to a compound of chemical formula 2 to obtain a compound of chemical formula 3; a step of reducing the compound of chemical formula 3 to obtain a compound of chemical formula 4; and a step of coupling the compound of chemical formula 4 with a phenylcarboxylic acid or amine derivative which trifluoromethyl, halogen, morpholine, piperazine. A pharmaceutical composition for preventing or treating melanoma contains the pyrollo(3,2-b)pyridine derivative or pharmaceutically acceptable salt as an active ingredient.

Abstract translation: 目的：提供一种新型的吡咯并[3,2-b]吡啶衍生物和用于预防或治疗含有此类黑色素瘤的药物组合物，以确保对黑素瘤细胞的高抗增殖活性。 构成：吡咯（3,2-b）吡啶衍生物由化学式1表示。制备吡罗咯（3,2，-b）吡啶衍生物的方法包括：将1-碘-4-硝基苯偶联到 化学式2的化合物，得到化学式3的化合物; 还原化学式3的化合物以获得化学式4的化合物的步骤; 以及将化学式4的化合物与三氟甲基，卤素，吗啉，哌嗪的苯基羧酸或胺衍生物偶合的步骤。 用于预防或治疗黑素瘤的药物组合物含有吡罗洛（3,2-b）吡啶衍生物或其药学上可接受的盐作为活性成分。

公开(公告)号：KR1020100031837A

公开(公告)日：2010-03-25

申请号：KR1020080090659

申请日：2008-09-16

Applicant: 한국과학기술연구원

Inventor： 오창현 ,  조정혁

IPC: C07D413/10 ,  C07D413/02

CPC classification number: C07D413/10

Abstract: PURPOSE: A novel oxazolidinone derivative having dilfuorophenyl derivative is provided to ensure antibacterial activity to Vancomycin-Resistant Enterococcus including Haemophilus influenza and Coagulase negative staphylococci. CONSTITUTION: A novel oxazolidinone derivative with a dilfuorophenyl derivative is denoted by chemical formula 1. A method for preparing the oxazolidinone derivative comprises: a step of reacting a compound of chemical formula 2 with trifluorenitrobenzene of chemical formula 3 to prepare a compound of chemical formula 4; a step of reducing the compound of chemical formula 4 to prepare a compound of chemical formula 5; a step of introducing carbobenzyloxy(CBZ) group to amine group of the compound of chemical formula 5 to obtain a compound of chemical formula 6; a step of adding n-butyl lithium and (R)-glycidyl butyrate to the compound of chemical formula 6 to prepare a compound of chemical formula 7; a step of performing methylation of hydroxyl group of the compound of chemical formula 7 to obtain a compound of chemical formula 8; a step of reacting the compound of chemical formula 8 with sodium azide to obtain a compound of chemical formula 9; a step of performing reduction and acetylation of the compound of chemical formula 9 to obtain a compound of chemical formula 10; a step of deprotecting the compound of chemical formula 10 to obtain a compound of chemical formula 11; and a step of reducing the compound of chemical formula 11 to obtain a compound of chemical formula 1a.

Abstract translation: 目的：提供一种具有二氟代苯基衍生物的新型恶唑烷酮衍生物，以确保对耐万古霉素肠球菌的抗菌活性，包括流感嗜血杆菌和凝固酶阴性葡萄球菌。 构成：具有二氟苯基衍生物的新型恶唑烷酮衍生物由化学式1表示。制备恶唑烷酮衍生物的方法包括：使化学式2的化合物与化学式3的三氟硝基苯反应以制备化学式4的化合物 ; 还原化学式4的化合物以制备化学式5的化合物的步骤; 将苄氧羰基（CBZ）基团引入到化学式5的化合物的胺基上以获得化学式6的化合物的步骤; 向化学式6化合物中加入正丁基锂和（R） - 缩水甘油基丁酸酯以制备化学式7的化合物的步骤; 进行化学式7的化合物的羟基的甲基化的步骤，得到化学式8的化合物; 使化学式8的化合物与叠氮化钠反应的步骤，得到化学式9的化合物; 进行化学式9的化合物的还原和乙酰化以获得化学式10的化合物的步骤; 使化学式10的化合物脱保护以获得化学式11的化合物的步骤; 以及还原化学式11化合物以获得化学式1a化合物的步骤。

公开(公告)号：KR100378117B1

公开(公告)日：2003-03-29

申请号：KR1020000001329

申请日：2000-01-12

Applicant: 한국과학기술연구원

Inventor： 조정혁 ,  오창현 ,  오창석 ,  이기수

IPC: A01N29/00

Abstract: PURPOSE: A removing method for noxious tide using chlorine dioxide is provided, which can remove noxious tide effectively without secondary pollution by spreading chlorine dioxide solution on a sea area with red tide or green tide. CONSTITUTION: The chlorine dioxide is produced by reacting sodium chlorite with chlorine; 2NaClO2 + Cl2 → 2ClO2 + 2NaCl, which exists as a yellow-green gas at normal temperature, is used in an aqueous solution by dissolving in water to make the concentration at a ratio of 0.1-1ppm, and removes noxious tide with microorganisms(such as Cochlodinium, Chaetoceros, Mesodinium, Gymnodinium, and Gyrodinium) as well as toxic substances produced by them due to strong oxidizing power thereof. But a halogenide is not produced as a by-product, and the chlorine dioxide is easily resolved into oxygen molecule and chlorine ion by sunlight.

Abstract translation: 目的：提供一种利用二氧化氯的有毒潮汐的去除方法，该方法通过在赤潮或绿潮的海域散布二氧化氯溶液来有效去除有害潮汐而无二次污染。 组成：二氧化氯由亚氯酸钠与氯反应产生; 2NaClO 2 + Cl 2＆amp; 在常温下以黄绿色气体形式存在的2ClO 2 + 2NaCl在水溶液中使用，通过溶解在水中使浓度达到0.1-1ppm，并用微生物（如Cochlodinium，Chaetoceros ，中子，（Mesodinium），Gymnodinium和Gyrodinium）以及由于其强氧化能力而产生的有毒物质。 但是，卤化物不作为副产物产生，并且二氧化氯通过日光很容易分解成氧分子和氯离子。