公开(公告)号：KR100688310B1

公开(公告)日：2007-03-02

申请号：KR1020050080366

申请日：2005-08-30

Applicant: 한국과학기술연구원 ,  (주)바이오액츠

Inventor： 김동찬 ,  김동진 ,  박웅서 ,  나종주 ,  고석영 ,  박진우

IPC: C09B45/00 ,  C09B45/38

Abstract: Provided is an azo-based metal complex reactive dye, which has advantages of both azo-based metal complex dyes and reactive dyes, and shows an improved sunlight fastness and a high fixation ratio. The azo-based metal complex reactive dye is represented by a formula of MxAyBz, wherein M represents a metal selected from the group consisting of Cr, Co, Fe, Cu and Ni; each of x and y represents 1 or 2, and z is 1, 2 or 3; A is selected from tridendate ligands represented by formulae 7-13; B represents H2O or is selected from tridendate ligands represented by the formulae 7-13; each of R1 and R2 is selected from the group consisting of -OH, -NH2, -COOH, -NHCOCH2COCH3 and -NH-(C6H5); and at least one of R3-R9 is -NHCOCHBrCH2Br or -NHCOCBr=CH2, and each of the remaining substituents of R3-R9 is selected from the group consisting of -H, -NH2, -SO3H, -OH, -COOH, -CH3, -OCH3, -NH-(C6H5), -NH-(C6H5)CH3, -NHSO2-(C6H5), -NHSO2-(C6H5)Cl, -NHSO2-(C6H5)COOH, -NHCOCH3, -NH2CH3, -SO2NH2, -NHSO2CH3, -N(CH3)2, -N(C2H5)2, -NO2, -NHCONH2, -CONH2, -N(C2H4OH)2 and -OC2H5.

Abstract translation: 本发明提供一种偶氮类金属络合物活性染料，其兼具偶氮类金属络合物染料和活性染料两者的优点，并且显示出改善的日光牢度和高固色率。 偶氮类金属络合物反应性染料由式M x A y B z表示，其中M表示选自Cr，Co，Fe，Cu和Ni的金属; x和y中的每一个代表1或2，并且z是1,2或3; A选自由式7-13表示的十三酸配体; B代表H 2 O或选自式7-13代表的十三配位体; R 1和R 2各自选自-OH，-NH 2，-COOH，-NHCOCH 2 COCH 3和-NH-（C 6 H 5）; 并且R3-R9中的至少一个是-NHCOCHBrCH2Br或-NHCOCBr = CH2，并且R3-R9的其余取代基中的每一个选自-H，-NH2，-SO3H，-OH，-COOH， - （C 6 H 5）CH 3，-NHSO 2 - （C 6 H 5）， - NHSO 2 - （C 6 H 5）Cl，-NHSO 2 - （C 6 H 5）COOH，-NHCOCH 3，-NH 2 CH 3， - -N（CH 2）5，-NO 2，-NHCONH 2，-CONH 2，-N（C 2 H 4 OH）2和-OC 2 H 5。

公开(公告)号：KR100468352B1

公开(公告)日：2005-01-27

申请号：KR1020020057933

申请日：2002-09-24

Applicant: 한국과학기술연구원

Inventor： 유경호 ,  김동찬 ,  신계정 ,  김동진

IPC: C07D487/04

Abstract: PURPOSE: A pyrazolopyrimidine derivative as a cyclin-dependent kinase inhibitor and a process for preparing the same are provided. The compound inhibits cyclin-dependent kinase(CDK) regulating cell division cycle and has low toxicity. Therefore, it can be useful for prevention and treatment of liver cancer, breast cancer, stomach cancer, colon cancer or rectal cancer caused by activation of CDK. CONSTITUTION: A pyrazolopyrimidine derivative is represented by the formula(1), wherein R1 comprises ortho, meta, or para substituent, and is bromo, chloro, fluoro, methoxy, hydrogen, nitro or amino; R2 is hydrogen or C3 or less of lower alkyl; R3 is hydrogen or C3 or less of lower alkyl, or hydroxyethyl; and n is an integer of 0 or 1. A method for preparing the pyrazolopyrimidine derivative represented by the formula(1) comprises the steps of: reacting 6-methylmercaptopyrazolopyrimidine of the formula(IV) with meta-chloroperbenzoic acid in the presence of an organic solvent such as chloroform or dichloromethane at -10 to 10 deg. C for 2 to 5 hours and at room temperature for 3 to 12 hours to prepare 6-methylsulfonylpyrazolopyrimidine of the formula(II); and nucleophilic substitution reaction of 6-methylsulfonylpyrazolopyrimidine of the formula(II) with hydroxyethylamine in the presence of a mixed organic solvent of isopropanol or n-butanol and dimethylsulfoxide or dimethylformamide at 70 to 100 deg. C for 1 to 6 hours.

Abstract translation: 目的：提供了作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶衍生物及其制备方法。 该化合物抑制细胞周期蛋白依赖性激酶（CDK）调节细胞分裂周期并具有低毒性。 因此，它可用于预防和治疗由CDK活化引起的肝癌，乳腺癌，胃癌，结肠癌或直肠癌。 结构式：吡唑并嘧啶衍生物由式（1）表示，其中R 1包含邻位，间位或对位取代基，并且是溴，氯，氟，甲氧基，氢，硝基或氨基; R2是氢或C3或更少的低级烷基; R3是氢或C3或更少的低级烷基或羟乙基; 制备式（1）代表的吡唑并嘧啶衍生物的方法包括下列步骤：使式（IV）的6-甲基巯基吡唑并嘧啶与间氯过苯甲酸在有机 溶剂如氯仿或二氯甲烷在-10至10℃下进行。 （II）的6-甲基磺酰基吡唑并嘧啶;将式（II）的6-甲基磺酰基吡唑并嘧啶在室温下搅拌2至5小时，并在室温下反应3至12小时。 （II）的6-甲基磺酰基吡唑并嘧啶与羟基乙胺在异丙醇或正丁醇和二甲基亚砜或二甲基甲酰胺的混合有机溶剂存在下在70-100℃下进行亲核取代反应。 C 1至6小时。

公开(公告)号：KR100390767B1

公开(公告)日：2003-07-10

申请号：KR1020000062695

申请日：2000-10-24

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  유경호 ,  신계정 ,  김동찬

IPC: C07D403/04

CPC classification number: C07D401/04

Abstract: The present invention relates to aziridinylquinolinedione derivatives having an anti-tumor effect of formula (1), a process for their preparation and their use as an anti-cancer agent, wherein R is a hydrogen atom or C1-C4 alkyl; one of R and R is an aziridinyl or 2-methylaziridinyl and the other one is a halogen atom, C1-C4 alkoxy, azido, or amino.

Abstract translation: 本发明涉及具有式（1）的抗肿瘤作用的氮丙啶基喹啉二酮衍生物，它们的制备方法以及它们作为抗癌剂的用途，其中R 1是氢。 是氢原子或C 1 -C 4烷基; R 2中的一个是R 2。 并且R 3是氢。 是吖丙啶基或2-甲基氮丙啶基，另一个是卤素原子，C 1 -C 4烷氧基，叠氮基或氨基。

公开(公告)号：KR100385093B1

公开(公告)日：2003-05-22

申请号：KR1020000049675

申请日：2000-08-25

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  김동찬

IPC: C07D417/14

Abstract: PURPOSE: Provided are a novel 1-β-methylcarbapenem derivative useful as antibiotics, its pharmaceutically acceptable salt, its manufacturing method and a pharmaceutical composition. containing it. CONSTITUTION: 1-β-methylcarbapenem derivative is represented by the formula(1), wherein R is represented by formulae; X is trifluormethyl or C1-C3 alkyl; Y is C1-C3 linear or branched aliphatic alkyl, C1-C3 sulfonamido alkyl in which one or two C1-C3 alkyl groups are substituted, C1-C3 alkyl substituted or unsubstituted C1-C3 carbo amidoalkyl group, C1-C3 hydroxyalkyl group, and C1-C3 alkyl substituted C1-C3 aminoalkyl or aryl; and Z is C1-C3 alkyl group.

Abstract translation: 目的：提供一种可用作抗生素的新型1-＆amp;β-甲基碳代青霉烯衍生物，其药学上可接受的盐，其制备方法和药物组合物。 包含它。 构成：1-β-甲基碳代青霉烯衍生物由式（1）表示，其中R由式表示; X是三氟甲基或C 1 -C 3烷基; Y是C1-C3直链或支链脂族烷基，其中一个或两个C1-C3烷基被取代的C1-C3亚磺酰氨基烷基，C1-C3烷基取代或未取代的C1-C3碳酰氨基烷基，C1-C3羟烷基和 C 1 -C 3烷基取代的C 1 -C 3氨基烷基或芳基; Z是C1-C3烷基。

公开(公告)号：KR1020020080686A

公开(公告)日：2002-10-26

申请号：KR1020010020411

申请日：2001-04-17

Applicant: 한국과학기술연구원

Inventor： 유재훈 ,  신계정 ,  김동진 ,  이경식

IPC: C07C255/33

CPC classification number: C07C217/22 ,  C07C45/673 ,  C07C45/71 ,  C07C47/575 ,  C07C51/38 ,  C07C59/68

Abstract: PURPOSE: Provided are a ferulic acid dimer, a pharmaceutically acceptable salt thereof, a method for preparing the same, its use in treating dementia, and an intermediate of the ferulic acid dimer. CONSTITUTION: The ferulic acid dimer is represented by formula 1. In the formula 1, X is carbon, oxygen or nitrogen, and n is 0-3. The salt of the ferulic acid dimer is an inorganic salt including sodium salt, potassium salt, magnesium salt, and calcium salt, or an organic salt including angelic acid, ricin, ethanolamine, N,N'-dibenzylethylene diamine, and alpha-tocopherol. The method comprises reacting a hydroxybenzaldehyde compound of formula 2(wherein X is carbon, oxygen or nitrogen, and n is 0-3) with malonic acid to form the ferulic acid dimer of formula 1.

Abstract translation: 目的：提供阿魏酸二聚物，其药学上可接受的盐，其制备方法，其用于治疗痴呆的用途和阿魏酸二聚体的中间体。 构成：阿魏酸二聚体由式1表示。在式1中，X是碳，氧或氮，n是0-3。 阿魏酸二聚体的盐是包括钠盐，钾盐，镁盐和钙盐的无机盐，或包括当归酸，蓖麻毒素，乙醇胺，N，N'-二苯基乙二胺和α-生育酚的有机盐。 该方法包括使式2的羟基苯甲醛化合物（其中X为碳，氧或氮，n为0-3）与丙二酸反应，形成式1的阿魏酸二聚体。

公开(公告)号：KR1019960010631A

公开(公告)日：1996-04-20

申请号：KR1019940022936

申请日：1994-09-12

Applicant: 한국과학기술연구원

Inventor： 박상우 ,  김동진 ,  박웅서 ,  김동찬

IPC: C07D239/30

Abstract: 다음 구조식(Ⅱ)의 2,4,5,6-테트라클로로피리미딘과 불화칼륨을 술포란 용매 중, 상간이동축매 존재 하에 반응시키는 것으로 이루어지는 다음 구조식(Ⅰ)의 5-클로로-2,4,6-트리플루오로피리미딘의 제조방법. 본 발명의 방법에 의해 낮을 난응온도에서 단시간에 소망되는 5-클로로, 2,4,6-트리플루오로피리미딘을 높은 수율 및 순도로 얻을 수 있다.

公开(公告)号：KR102132847B1

公开(公告)日：2020-07-13

申请号：KR1020190162945

申请日：2019-12-09

Applicant: 한국과학기술연구원

Inventor： 김동진 ,  강용구 ,  금교창 ,  김윤경 ,  류훈 ,  임성수 ,  김도희 ,  이동수 ,  이윤상 ,  최유리 ,  이지훈

IPC: C07D277/66 ,  A61K31/428 ,  A61P25/28

公开(公告)号：KR101715127B1

公开(公告)日：2017-03-15

申请号：KR1020150152289

申请日：2015-10-30

Applicant: 한국과학기술연구원 ,  서울대학교병원

Inventor： 박기덕 ,  배애님 ,  김동진 ,  조남철 ,  박종현 ,  최지원 ,  연슬기 ,  하태환 ,  장보고 ,  주은지 ,  김성민 ,  천소영 ,  김희정 ,  장재완

IPC: A61K31/513 ,  A61K31/505 ,  A61K31/18

Abstract: 본발명은피리미딘카복실레이트유도체또는이의약제학적으로허용가능한염 또는이의용매화물을유효성분으로함유하여 NMO-IgG와아쿠아포린 4 단백질의결합을저해시킴으로써 NMO-IgG와아쿠아포린 4 단백질의결합에의해유발되는질병, 바람직하게는시신경척수염또는퇴행성신경계질환을예방또는치료할수 있는약학조성물에관한것이다.

公开(公告)号：KR1020170024600A

公开(公告)日：2017-03-07

申请号：KR1020170024145

申请日：2017-02-23

Applicant: 한국과학기술연구원

Inventor： 김영수 ,  김동진 ,  김혜연 ,  조수민 ,  김태송 ,  김현진 ,  이세진 ,  고재영 ,  노지훈 ,  황교선

IPC: G01N33/49 ,  G01N33/50 ,  G01N33/68 ,  G01N15/06

CPC classification number: G01N33/6893 ,  A61K38/1716 ,  C07K14/4711 ,  G01N33/6827 ,  G01N33/6896 ,  G01N2333/4709 ,  G01N2800/2821

Abstract: 본발명은체내단백질응집체의용해를이용한단백질의비정상적인응집또는미스폴딩과관련된질환또는질병을진단하는혈액진단키트에관한것으로베타아밀로이드의단량체화조성물을투여하기전과후의혈장내 베타아밀로이드단량체의농도를측정함으로써, 베타아밀로이드의응집을원인으로하는알츠하이머병 등의질병또는질환뿐만아니라단백질응집으로인한다른질병또는질환의응집된단백질의용해를통한농도분석으로단백질의비정상적인응집또는미스폴딩과관련된질환또는질병의정확한진단이가능하며, 이로인하여베타아밀로이드및 단백질의집적을막아주는기전의약물들의효과를볼 수있으며체내의베타아밀로이드및 약물로단량체화되는과정중 혈액쪽으로이동하게되는단백질의분석을이용하여혈액학적으로진단하므로분석의정확성이높다.

Abstract translation: 本公开涉及能够精确诊断与蛋白质的异常聚集或错误折叠相关的疾病或病症的诊断试剂盒，包括由淀粉样蛋白（例如阿尔茨海默氏症）聚集引起的疾病或疾病，以及由其他的聚集引起的疾病或疾病 蛋白质，基于解离之前和之后的聚集蛋白质的浓度分析。

公开(公告)号：KR1020160149854A

公开(公告)日：2016-12-28

申请号：KR1020150087599

申请日：2015-06-19

Applicant: 한국과학기술연구원

Inventor： 김윤경 ,  김동진 ,  박기덕 ,  임성수 ,  김도희 ,  마무눌하크

IPC: C07K14/47 ,  C12N15/85 ,  G01N33/50

CPC classification number: C07K14/47 ,  C12N15/85 ,  G01N33/50

Abstract: 본발명은전이성타우단백질및 이의제조방법에관한것이다. 신경세포내타우단백질응집은알츠하이머, 측두엽변성증, 픽병, 피질기조퇴행및 퇴행성핵산마비등 다양한타우병증질환을야기한다. 최근, 타우단백질이프리온단백질처럼세포간에전이되어정상세포내의타우단백질응집을유도한다는보고가이어지고있으나, 타우단백질내에서어느부분이전이성을가지는지, 전이메커니즘이어떻게이루어지는가에대한연구는미비한실정이다. 본발명은전이성을가지는타우단백질응집체의분리에관한것으로, 타우단백질응집체의전이메카니즘을밝히고, 전이억제후보물질의개발에기여할수 있을것으로기대된다.

Abstract translation: 本发明涉及转移性tau蛋白及其制备方法。 神经细胞中tau蛋白的聚集引起各种甲状腺疾病，例如阿尔茨海默病，颞叶变性，皮克病，皮质基底变性和进行性核上性麻痹。 最近有连续的报道，像朊病毒蛋白一样，tau蛋白在细胞之间转移以诱导正常细胞中的tau蛋白聚集。 然而，关于tau蛋白中哪个区域具有转移或如何发生转移机制的研究是不完整的。 本发明涉及具有转移的tau蛋白聚集体的分离，预期本发明可有助于建立tau蛋白聚集体的转移机制和抑制转移抑制候选物质的发展。