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    메틸리덴-헤테로싸이클릭 화합물
    21.
    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
    26.
    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
    27.
    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。

    신규 1-베타메틸카바페넴 유도체 및 그의 제조방법
    29.
    发明公开
    신규 1-베타메틸카바페넴 유도체 및 그의 제조방법 失效
    新一代甲基胆碱衍生物及其制备方法

    公开(公告)号：KR1020020003789A

    公开(公告)日：2002-01-15

    申请号：KR1020000038284

    申请日：2000-07-05

    Applicant: 한국과학기술연구원

    Inventor： 김동진 ,  박상우 ,  신계정 ,  유경호 ,  강용구 ,  서경재

    IPC: C07D477/10

    CPC classification number: C07D477/20 ,  C07D413/06 ,  C07D417/06

    Abstract: PURPOSE: Provided are novel 1 β-Methylcarbapenem derivatives and their preparation process, which derivatives show stability to dihydropeptidase-I, and have antibacterial effects on both gram positive and gram negative bacteria. Thus, they are used as antibacterial agents. CONSTITUTION: Novel 1 β-Methylcarbapenem derivatives have substituted 5-(2-isoxazolyl ethenyl)pyrrolidine-3-thio or 5-(2-isothiazolyl ethenyl)pyrrolidine-3-thio group as a main functional group at 1-beta methylcarbapenem represented by the formula(1). A pharmaceutical composition for an antibacterial agent contains the 1 β-Methylcarbapenem derivatives, as active ingredients. In the formula(1), R is described as in the description and has cis- or trans stereomer, X is hydrogen, methoxycarbonyl, hydroxymethyl, methylaminomethyl, C1-C4 alkoxy or halogen atom, and Y is hydrogen or halogen atom.

    Abstract translation: 目的：提供新型1型β-甲基碳青霉烯衍生物及其制备方法，该衍生物显示对二氢肽酶-I的稳定性，对革兰氏阳性菌和革兰氏阴性菌均具有抗菌作用。 因此，它们被用作抗菌剂。 构成：新型1β-甲基碳青霉烯衍生物具有取代的5-（2-异恶唑基乙烯基）吡咯烷-3-硫基或5-（2-异噻唑基乙烯基）吡咯烷-3-硫基作为主要官能团，以1-β甲基碳青霉烯为代表 公式（1）。 作为抗菌剂的药物组合物含有作为活性成分的1β-甲基碳青霉烯衍生物。 在式（1）中，R如说明书所述，具有顺式或反式立体异构体，X为氢，甲氧基羰基，羟甲基，甲基氨基甲基，C1-C4烷氧基或卤原子，Y为氢或卤素原子。

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