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    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법
    42.
    发明公开
    칼슘이온 채널 조절제로서 유효한 이미다졸릴알킬카르보닐유도체 및 그의 제조방법 失效
    新型咪唑啉酮衍生物作为钙通道调节剂及其制备方法

    公开(公告)号：KR1020100001288A

    公开(公告)日：2010-01-06

    申请号：KR1020080061148

    申请日：2008-06-26

    Applicant: 한국과학기술연구원

    Inventor： 최경일 ,  남길수 ,  김혜란 ,  임혜원 ,  서선희 ,  백이연 ,  김윤지 ,  신희섭 ,  김동진 ,  배애님 ,  정혜진 ,  조용서 ,  추현아 ,  노은주 ,  강순방 ,  신계정 ,  한호규 ,  신동윤 ,  정찬성 ,  남기달 ,  강용구 ,  이재균 ,  박웅서 ,  김영수 ,  김은경 ,  김기선 ,  정혜선 ,  금교창 ,  이철주 ,  최기현

    IPC: C07D233/61

    CPC classification number: C07D233/60 ,  C07D209/48 ,  C07D233/54 ,  C07D233/61 ,  C07D403/06

    Abstract: PURPOSE: A novel imidazolylalkylcarbonyl derivative which is effective as calcium ion channel regulator is provided to effectively block T-type calcium ion channel, prevent and treat brain diseases, heart diseases and pain. CONSTITUTION: An imidazolylalkylcarbonyl derivative is denoted by chemical formula 1. The imidazolylalkylcarbonyl derivative of chemical formula 1 is prepared by performing amide bond of piperazine derivative of chemical formula 3 with imidazolylalkylcarboxylic acid of chemical formula 2. The amide bond is performed using binder selected from phosphonium system, ammonium system, carbodiimide system, imidazolinium, and organic phosphine system. A method for preparing the imidazolylalkylcarboxylic acid of chemical formula 2 comprises: a step of performing hetero-michael addition reaction of ethy alkenoate with imidazole compound under the presence of KF/Al2O3 catalyst to produce ethoxycarbonylalkylimidazole compound of chemical formula 2a; and a step of hydrolyzing the ethoxycarbonylalkylimidazole compound of chemical formula 2a to prepare imidazolylalkylcarboxylic acid of chemical formula 2.

    Abstract translation: 目的：提供一种有效阻断T型钙离子通道，预防和治疗脑疾病，心脏病和疼痛的新型咪唑烷基羰基衍生物，作为钙离子通道调节剂有效。 构成：化学式1表示咪唑烷基羰基衍生物。化学式1的咪唑烷基羰基衍生物通过化学式3的哌嗪衍生物与化学式2的咪唑基烷基羧酸的酰胺键进行制备。酰胺键使用选自鏻 系统，铵系统，碳二亚胺系统，咪唑啉鎓和有机膦系统。 制备化学式2的咪唑基烷基羧酸的方法包括：在KF / Al 2 O 3催化剂存在下，进行异丁烯酸乙酯与咪唑化合物的异迈克尔加成反应，生成化学式2a的乙氧基羰基烷基咪唑化合物的步骤; 以及水解化学式2a的乙氧基羰基烷基咪唑化合物以制备化学式2的咪唑基烷基羧酸的步骤。

    베이커 이스트를 이용한 피라진 화합물의 제조 방법
    43.
    发明授权
    베이커 이스트를 이용한 피라진 화합물의 제조 방법 失效
    베이커이스트를이용한피라진화합물의제조방법

    公开(公告)号：KR100466371B1

    公开(公告)日：2005-01-13

    申请号：KR1020030026907

    申请日：2003-04-29

    Applicant: 한국과학기술연구원

    Inventor： 김유승 ,  강순방 ,  금교창 ,  장민석 ,  모길웅 ,  오희영

    IPC: C12P17/12

    Abstract: PURPOSE: Methods for preparing tetrasubstitued pyrazines using baker's yeast are provided, thereby easily and environment-friendly preparing tetrasubstitued pyrazines in water under mild condition. CONSTITUTION: The method for preparing tetrasubstitued pyrazines of formula (2) using baker's yeast comprises the steps of: (1) preparing a solution of baker's yeast; and (2) dissolving beta-keto alpha-oxime carbonyl derivatives of formula (1) in hydrophilic organic solvent and adding the solution into the baker's yeast solution to carry out chemoselective microbial reduction, wherein R1 is methyl, ethyl or phenyl; R2 is hydrogen, methyl or benzyl; R3 is methoxy, ethoxy, benzyloxy or phenylamine; the organic solvent is selected from benzene, toluene and hexane.

    Abstract translation: 目的：提供使用面包酵母制备四取代吡嗪的方法，由此在温和条件下容易且环境友好地制备四取代吡嗪在水中。 构成：使用面包酵母制备式（2）的四取代吡嗪的方法包括以下步骤：（1）制备面包酵母溶液; （2）将式（1）的β-酮基α-肟羰基衍生物溶解于亲水性有机溶剂中，并将该溶液加入面包酵母溶液中进行化学选择性微生物还原，其中R1为甲基，乙基或苯基; R2是氢，甲基或苄基; R3是甲氧基，乙氧基，苄氧基或苯胺; 有机溶剂选自苯，甲苯和己烷。

    피롤리디논 유도체, 이의 제조 방법 및 이를 포함하는제약 조성물
    44.
    发明授权
    피롤리디논 유도체, 이의 제조 방법 및 이를 포함하는제약 조성물 失效
    피롤리디논유도체，이의제조방법및이를포함하는제품조성물

    公开(公告)号：KR100437972B1

    公开(公告)日：2004-07-02

    申请号：KR1020010066578

    申请日：2001-10-27

    Applicant: 한국과학기술연구원

    Inventor： 김유승 ,  강순방 ,  금교창 ,  장민석 ,  공재양 ,  정대영

    IPC: C07D413/14

    CPC classification number: C07D413/14

    Abstract: The present invention relates to substituted pyrrolidinone compounds of formula 1, wherein n is 0 or 1; Aza is a heterocycle optionally substituted with C1-4 alkyl, or C1-4 alkyl substituted with a heterocycle, which represents a saturated or unsaturated five- or six-membered ring having nitrogen(s) as a heteroatom, which are muscarinic acetylcholine receptor agonists and useful as nootropics and therapeutic agents for cerebral neural diseases such as Alzheimer's disease; and pharmaceutically acceptable salts thereof; processes for the preparation thereof; and pharmaceutical compositions comprising these compounds or salts.

    Abstract translation: 本发明涉及式1的取代的吡咯烷酮化合物，其中n是0或1; Aza是任选被C1-4烷基或被杂环取代的C1-4烷基取代的杂环，所述杂环代表具有氮作为杂原子的饱和或不饱和五元或六元环，其为蕈毒碱乙酰胆碱受体激动剂 作为阿尔茨海默病等脑神经疾病的促智药和治疗药有用; 和其药学上可接受的盐; 其制备方法; 和包含这些化合物或盐的药物组合物。

    무스카린성 아세틸콜린 수용체에 작용하는테트라하이드로피리딘 유도체
    45.
    发明公开
    무스카린성 아세틸콜린 수용체에 작용하는테트라하이드로피리딘 유도체 失效
    具有高亲和力的四烯雌二醇衍生物用于葡萄糖型乙酰胆碱受体

    公开(公告)号：KR1020030034816A

    公开(公告)日：2003-05-09

    申请号：KR1020010066568

    申请日：2001-10-27

    Applicant: 한국과학기술연구원

    Inventor： 김유승 ,  강순방 ,  금교창 ,  장민석 ,  공재양 ,  정대영

    IPC: C07D401/06 ,  A61K31/435 ,  A61K31/40

    CPC classification number: C07D401/06

    Abstract: PURPOSE: A tetrahydropyridine derivative having high affinity for muscarine type acetylcholine receiptor is provided, thereby the tetrahydropyridine derivative can be useful as a recognition improving agent and a nervous disease treating agent. CONSTITUTION: The tetrahydropyridine derivative having high affinity for a muscarine type acetylcholine receiptor is represented by formula(1), wherein m is 0 or 1; n is 1 or 2; R1 is hydrogen, C1-4 alkyl, C2-4 alkynyl or aryl; and R3 is C1-4 alkyl. The process for preparing the tetrahydropyridine derivative comprises (i) condensation of a compound of formula(5) with R1ONH2-HCl to prepare a compound of formula(8); and (ii) reacting the compound of formula(8) with alkyl iodide to prepare alkyl pyrimidine salt and reducing the alkyl pyrimidine salt.

    Abstract translation: 目的：提供对毒蕈碱型乙酰胆碱受体具有高亲和力的四氢吡啶衍生物，由此四氢吡啶衍生物可用作识别改善剂和神经疾病处理剂。 构成：对毒蕈碱型乙酰胆碱受体具有高亲和力的四氢吡啶衍生物由式（1）表示，其中m为0或1; n为1或2; R1是氢，C1-4烷基，C2-4炔基或芳基; 并且R 3是C 1-4烷基。 制备四氢吡啶衍生物的方法包括（i）式（5）化合物与R1ONH2-HCl缩合以制备式（8）化合物; 和（ii）使式（8）化合物与烷基碘反应制备烷基嘧啶盐并还原烷基嘧啶盐。

    알릴화된 7-히드록시쿠마린 유도체의 제조방법
    46.
    发明授权
    알릴화된 7-히드록시쿠마린 유도체의 제조방법 失效
    알릴화된7-히드록시쿠마린유도체의제조방법

    公开(公告)号：KR100377327B1

    公开(公告)日：2003-03-26

    申请号：KR1020020036479

    申请日：2002-06-27

    Applicant: 한국과학기술연구원

    Inventor： 김유승 ,  강순방 ,  금교창 ,  조상원

    IPC: C07D311/16

    Abstract: PURPOSE: Provided is a method for preparing allylated 7-hydroxycoumarin derivatives effectively and economically in high yield. CONSTITUTION: The method for preparing allylated 7-hydroxycoumarin is characterized by reacting allylhalide of the formula(1) with 7-hydroxycoumarin of the formula(2) to manufacture allylated 7-hydroxycoumarin derivative of the formula(3).

    Abstract translation: 目的：提供一种高产率有效和经济地制备烯丙基化7-羟基香豆素衍生物的方法。 构成：烯丙基化7-羟基香豆素的制备方法的特征在于使式（1）的烯丙基卤化物与式（2）的7-羟基香豆素反应，制备式（3）的烯丙基化7-羟基香豆素衍生物。

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