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    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물
    15.
    发明授权
    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물 失效
    신규피라졸로피리미딘계유도체，그의제조방법및이를유효성분으로하는약학적조성물

    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。

    ＲＮＡ 표적 분자에 대해 특이성이 향상된네오마이신-클로람페니콜 헤테로 이합체 및 그의 제조방법
    16.
    发明授权
    ＲＮＡ 표적 분자에 대해 특이성이 향상된네오마이신-클로람페니콜 헤테로 이합체 및 그의 제조방법 失效
    RNA표적분자에대해특이성이향상된네오마이신 - 클로람페니콜헤테로이합체및그의제조방RNA

    公开(公告)号：KR100450864B1

    公开(公告)日：2004-10-01

    申请号：KR1020010073358

    申请日：2001-11-23

    Applicant: 한국과학기술연구원

    Inventor： 유재훈 ,  이종국 ,  권미윤 ,  신계정

    IPC: C07H15/232

    CPC classification number: C07H5/10 ,  C07H15/232

    Abstract: The present invention relates to heterodimeric conjugates of neomycin-chloramphenicol, of formula 1, their preparation and their use. Because of their heterodmieric structure, they can recognize both stem and loop of RNA motif and show binding ability to a certain RNA such that they have an enhanced pharmaceutical efficacy and reduced side effect which can be caused by non-specific drugs. For these reasons, they can be effectively used as an antiviral agent, an antibacterial agent or an anticancer drugs.

    Abstract translation: 本发明涉及式1的新霉素 - 氯霉素的异二聚体缀合物，它们的制备及其用途。 由于它们具有异源性结构，因此它们可以识别RNA基序的茎和环，并显示对某种RNA的结合能力，从而具有增强的药效和减少可能由非特异性药物引起的副作用。 由于这些原因，它们可以有效地用作抗病毒剂，抗菌剂或抗癌药物。

    아지리디닐퀴놀린디온 유도체와 그의 제조방법
    17.
    发明授权
    아지리디닐퀴놀린디온 유도체와 그의 제조방법 失效
    아지리디닐퀴놀린디온유도체와그의제조방법

    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。

    5'-헤테로아릴티오메틸피롤리딘-3'-일티오기를 갖는 신규 1-베타메틸카바페넴 유도체 및 그의 제조방법
    18.
    发明授权
    5'-헤테로아릴티오메틸피롤리딘-3'-일티오기를 갖는 신규 1-베타메틸카바페넴 유도체 및 그의 제조방법 失效
    5'-헤테로아릴티메틸피롤리딘-3'-일티오기를갖는신규1-베타메틸카바페넴유도체및그의제조방5

    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。

    페룰릭산 이합체 및 그의 약학적 허용 염, 그 제조방법 및치매 치료를 위한 그의 용도
    19.
    发明公开
    페룰릭산 이합체 및 그의 약학적 허용 염, 그 제조방법 및치매 치료를 위한 그의 용도 失效
    无菌酸二酯，其药用盐，其制备方法及其用于治疗感染的用途

    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。

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