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    페룰릭산 이합체 및 그의 약학적 허용 염, 그 제조방법 및치매 치료를 위한 그의 용도
    21.
    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。

    메틸리덴-헤테로싸이클릭 화합물
    23.
    发明公开
    메틸리덴-헤테로싸이클릭 화합물 有权
    甲基 - 杂环化合物

    公开(公告)号：KR1020130010784A

    公开(公告)日：2013-01-29

    申请号：KR1020110071653

    申请日：2011-07-19

    Applicant: 한국과학기술연구원

    Inventor： 노은주 ,  신계정 ,  송혜승 ,  양정은 ,  김남윤 ,  배애님 ,  남길수 ,  추현아 ,  지완근

    IPC: C07D417/10 ,  C07D417/12 ,  C07D277/36 ,  A61K31/427

    Abstract: PURPOSE: A methylidene-heterocyclic compound and a pharmaceutical composition containing the same are provided to strongly suppress IkappaB kinase-b(IKK-b) and to treat various inflammatory diseases. CONSTITUTION: A methylidene-heterocyclic compound is denoted by chemical formula 1. A pharmaceutical composition for preventing and treating inflammatory diseases contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases include rheumatoid arthritis, juvenile arthritis, asthma, spondyloarthopathies, gout, osteoarthritis, allergic rhinitis, atopic dermatitis, systemic lupuserythematosus, psoriasis, ulcerative colitis, SIRS, sepsis, or polymyositis. A method for preparing the compound of chemical formula 1 comprises: a step of cyclizing an aniline compound of chemical formula 2 and preparing a 3-phenyl rhodanine compound of chemical formula 3; and a step of condensing the compound of chemical formula 3 with aldehyde compound of R2-C(O)H under an acidic condition. [Reference numerals] (AA) Step 1; (BB) Step 2

    Abstract translation: 目的：提供亚甲基杂环化合物和含有它们的药物组合物以强烈抑制IkappaB激酶b（IKK-b）并治疗各种炎性疾病。 构成：亚甲基杂环化合物由化学式1表示。用于预防和治疗炎性疾病的药物组合物含有化学式1的化合物作为活性成分。 炎性疾病包括类风湿性关节炎，青少年关节炎，哮喘，脊椎动物病痛，痛风，骨关节炎，过敏性鼻炎，特应性皮炎，系统性红斑狼疮，牛皮癣，溃疡性结肠炎，SIRS，败血症或多发性肌炎。 制备化学式1的化合物的方法包括：使化学式2的苯胺化合物环化并制备化学式3的3-苯基绕丹宁化合物的步骤; 和在酸性条件下将化学式3的化合物与R2-C（O）H的醛化合物缩合的步骤。 （附图标记）（AA）步骤1; （BB）步骤2

    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물
    28.
    发明公开
    신규 피라졸로피리미딘계 유도체, 그의 제조방법 및 이를 유효성분으로 하는 약학적 조성물 失效
    作为循环依赖性激酶抑制剂的吡唑并嘧啶衍生物及其制备方法

    公开(公告)号：KR1020040026462A

    公开(公告)日：2004-03-31

    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，毒性低。 因此，可用于预防和治疗由CDK激活引起的肝癌，乳腺癌，胃癌，结肠癌或直肠癌。 构型：吡唑并嘧啶衍生物由式（1）表示，其中R 1包括邻，间或对位取代基，并且是溴，氯，氟，甲氧基，氢，硝基或氨基; R2是氢或C3以下的低级烷基; R3是氢或C3以下的低级烷基或羟乙基; 并且n是0或1的整数。由式（1）表示的吡唑并嘧啶衍生物的制备方法包括以下步骤：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℃。 C化2〜5小时，在室温下反应3〜12小时，得到式（II）的6-甲基磺酰基吡唑并嘧啶; 和式（II）的6-甲基磺酰基吡唑并嘧啶与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在70-100℃下与羟乙基胺的亲核取代反应。 C 1〜6小时。

    신남산 이합체, 그 제조방법 및 퇴행성 뇌질환 치료를위한 그의 용도
    29.
    发明公开
    신남산 이합체, 그 제조방법 및 퇴행성 뇌질환 치료를위한 그의 용도 失效
    活性酸二酯，其制备方法及其用于治疗神经病变疾病的方法

    公开(公告)号：KR1020030090970A

    公开(公告)日：2003-12-01

    申请号：KR1020020028871

    申请日：2002-05-24

    Applicant: 한국과학기술연구원 ,  주식회사 싸이제닉

    Inventor： 김동진 ,  신계정 ,  유재훈 ,  이희설

    IPC: A61K31/195 ,  C07C69/734

    CPC classification number: C07C229/44 ,  C07C45/71 ,  C07C47/575 ,  C07C59/68 ,  C07C67/343 ,  C07C69/734

    Abstract: PURPOSE: Provided are cinnamic acid dimers, and their preparation method and use for treating neurodegenerative disease. The cinnamic acid dimers have improving effect on learning capability and memory and minimize adverse side effect. CONSTITUTION: Cinnamic acid dimers are characteristically represented by the formula(1), wherein R is hydrogen or a C1-C5 lower alkyl group; X is oxygen or -NH, -NCH3; Y is -OCH3, -NHCH3 or -N(CH3)2; spacer is a carbon, oxygen or nitrogen containing C2-C8 alkyl group; and X and Y linked together by the spacer are positioned at ortho, meta, or para site.

    Abstract translation: 目的：提供肉桂酸二聚体及其制备方法和用于治疗神经变性疾病的用途。 肉桂酸二聚体具有改善对学习能力和记忆的作用，并尽量减少不良副作用。 构成：肉桂酸二聚体的特征性由式（1）表示，其中R是氢或C1-C5低级烷基; X是氧或-NH，-NCH 3; Y是-OCH 3，-NHCH 3或-N（CH 3）2; 间隔物是含有碳，氧或含氮的C 2 -C 8烷基; 并且通过间隔物连接在一起的X和Y位于邻位，间位或对位。

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