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    4-메틸이미다졸-5-카보닐구아니딘 유도체, 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 허혈성 심장질환의 예방 및 치료용 약학적 조성물
    1.
    发明授权
    4-메틸이미다졸-5-카보닐구아니딘 유도체, 이의 약학적으로허용가능한 염, 이의 제조방법 및 이를 유효성분으로함유하는 허혈성 심장질환의 예방 및 치료용 약학적 조성물 失效
    4-甲基咪唑烷-5-甲磺酰胺衍生物，其药学上可接受的盐，制备方法和药物组合物，用于预防和治疗含有作为活性成分的同种异体心脏疾病

    公开(公告)号：KR100820173B1

    公开(公告)日：2008-04-08

    申请号：KR1020070024124

    申请日：2007-03-12

    Applicant: 한국화학연구원

    Inventor： 이규양 ,  이선경 ,  윤성준 ,  이병호 ,  오광석 ,  정이숙

    IPC: C07D233/90 ,  A61K31/4164

    CPC classification number: C07D233/90

    Abstract: A novel 4-methylimidazol-5-ylcarbonylguanidine derivative is provided to show strong inhibitory activity on NHE-1, a sodium and hydrogen exchange passage, and show excellent heart protecting effect, thereby being usefully used as a therapeutic agent of ischemic heart diseases or a heat protecting agent such as a fibrinolytic enzyme. A 4-methylimidazol-5-ylcarbonylguanidine derivative represented by the formula(1) is at least one selected from the group consisting of (2-(2,3-dichlorophenyl)-4-methyl-1H-imidazol-5-ylcarbonyl)guanidine bis-methanesulfonate, (2-(2,5-dichlorophenyl)-4-methyl-1H-imidazol-5-ylcarbonyl)guanidine bis-methanesulfonate, (2-(3,5-dichlorophenyl)-4-methyl-1H-imidazol-5-ylcarbonyl)guanidine, (2-(2-methoxy-5-chlorophenyl)-4-methyl-1H-imidazol-5-ylcarbonyl)guanidine bis-methanesulfonate, and (2-(2-methoxy-5-fluorophenyl)-4-methyl-1H-imidazol-5-ylcarbonyl)guanidine bis-methanesulfonate and is prepared by reacting a carboxylic acid derivative having a leaving group(L) represented by the formula(2) with guanidine, wherein each R^1 and R^2 is independently H, halogen, trihalomethyl, mesyl, nitro, amino, C1-5 linear or branched alkyl or OR^3(wherein R^3 is H, trihalomethyl, C1-5 linear or branched alkyl or phenyl); X is H, C1-5 linear or branched alkyl or phenyl; and L is halogen, hydroxy, alkoxy, mesylate, or tosylate. A pharmaceutical composition for preventing and treating ischemic cardiac diseases comprises the 4-methylimidazol-5-ylcarbonylguanidine derivative or a pharmaceutically acceptable salt thereof as an effective ingredient.

    Abstract translation: 提供了一种新的4-甲基咪唑-5-基羰基胍衍生物，以显示对NHE-1，钠和氢交换通道的强抑制活性，并且显示出优异的心脏保护作用，从而可用作缺血性心脏病的治疗剂或 热保护剂如纤维蛋白溶解酶。 由式（1）表示的4-甲基咪唑-5-基羰基胍衍生物是选自（2-（2,3-二氯苯基）-4-甲基-1H-咪唑-5-基羰基）胍 （2-（2,5-二氯苯基）-4-甲基-1H-咪唑-5-基羰基）双 - 甲磺酸胍，（2-（3,5-二氯苯基）-4-甲基-1H-咪唑 （2-（2-甲氧基-5-氯苯基）-4-甲基-1H-咪唑-5-基羰基） - 双 - 甲磺酸胍和（2-（2-甲氧基-5-氟苯基） -4-甲基-1H-咪唑-5-基羰基）双 - 甲磺酸胍，通过使具有式（2）表示的离去基团（L）的羧酸衍生物与胍反应制备，其中每个R 1和R ^ 2独立地是H，卤素，三卤代甲基，甲磺酰基，硝基，氨基，C 1-5直链或支链烷基或OR 3（其中R 3是H，三卤代甲基，C 1-5直链或支链烷基或苯基）; X是H，C 1-5直链或支链烷基或苯基; 和L是卤素，羟基，烷氧基，甲磺酸酯或甲苯磺酸酯。 用于预防和治疗缺血性心脏病的药物组合物包含4-甲基咪唑-5-基羰基胍衍生物或其药学上可接受的盐作为有效成分。

    도라지 막분리 추출물을 유효성분으로 함유하는 심근경색의 예방 또는 치료용 약학적 조성물
    4.
    发明公开
    도라지 막분리 추출물을 유효성분으로 함유하는 심근경색의 예방 또는 치료용 약학적 조성물 无效
    用于预防或治疗含有作为活性成分的白藜芦醇的膜分离提取物的心肌梗塞的药物组合物

    公开(公告)号：KR1020110061976A

    公开(公告)日：2011-06-10

    申请号：KR1020090118532

    申请日：2009-12-02

    Applicant: 한국화학연구원

    Inventor： 김은주 ,  김영섭 ,  유시용 ,  차미란 ,  유대석 ,  정이숙

    IPC: A61K36/346 ,  A61P9/10

    Abstract: PURPOSE: A pharmaceutical composition containing Platycodon grandiflorum membrane-separated extract is provided to reduce lipid peroxide concentrate and to prevent or treat myocardial infarcton. CONSTITUTION: A pharmaceutical composition for preventing or treating myocardial infarction contains Platycodon grandiflorum membrane-separated extract as an active ingredient. A method for preparing the extract comprises: a step of adding water, organic solvent, or mixture solvent thereof to Platycodon grandiflorum; and a step of isolating membrane. The organic solvent is alcohol of C1-C4, acetic acid ethyl, methylene chloride or chloroform.

    Abstract translation: 目的：提供含有桔梗大蒜膜分离提取物的药物组合物，以减少脂质过氧化物浓缩物并预防或治疗心肌梗死。 构成：用于预防或治疗心肌梗死的药物组合物含有桔梗膜分离提取物作为活性成分。 制备提取物的方法包括：将水，有机溶剂或其混合溶剂加入到大蒜中的步骤; 和隔离膜的步骤。 有机溶剂是C1-C4，乙酸乙酯，二氯甲烷或氯仿的醇。

    신규의치환된이미다졸유도체및그의제조방법
    5.
    发明授权
    신규의치환된이미다졸유도체및그의제조방법 失效
    新的取代的咪唑衍生物及其制备方法

    公开(公告)号：KR100303944B1

    公开(公告)日：2001-11-22

    申请号：KR1019930026610

    申请日：1993-12-06

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  이상희 ,  김혜령 ,  서지희 ,  김낙정 ,  김선주 ,  차옥자 ,  신영아 ,  신화섭 ,  이승호 ,  정이숙 ,  이병호 ,  서호원

    IPC: C07D403/10

    Abstract: PURPOSE: Provided are novel substituted imidazole derivatives, represented by the formula(1) and their pharmaceutically acceptable salts, a pharmaceutical composition containing them and their preparation method. The compounds are used in inhibiting the high blood pressure by inhibiting the action of Angiotensin II. CONSTITUTION: The imidazole derivatives are represented by the formula(1), wherein A and B are independently -CH2 or -CO- but not -CO- simultaneously; Z is halogen atom or trifluorophenyl, C1-C14 alkenyl group; R is X substituted phenyl or thiophenyl, furanyl and imidazoyl(where x is -(CH2)n-X' and n is an integer of 0-4), and X' is hydrogen, -N-(C1-C4 alkyl)2, C1-C4 alkyl N substituted or unsubstituted piperazine, 3-or 2-oxopiperazine, morpholine, piperidine, thiomorpholine or imidazole. The typical method of synthesis comprises the steps of: manufacturing 5-(4-((thiomorpholine-4-yl)methyl)-2-butyl-4-chloro-1-((2'-(1H- tetrazole-5-yl)bipheyl-4-yl)methyl)imidazole by dissolving 4-chlorobenzoic acid into benzene and adding thionylchloride, refluxing, concentrating and dissolving again in methylene chloride; adding this product to the methylene chloride solution of 2-butyl-4-chloro-5-(hydroxymethyl)-1-((2'-((1-ethoxyethyl)-1H-tetrazole-5-yl)biphenyl-4 -yl)methyl)imidazole and triethylamine; dissolving this compound in tetrahydrofuran(THF) and adding thiomorpholine and refluxing with heating for 20 hours and extracting with ethylacetate; and dissolving this compound in THF, adding 1N HCl, stirring at room temperature for 17 hours, neutralizing with 1N NaOH and extracting with ethyl acetate.

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