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    신규의치환된이미다졸유도체및그의제조방법
    1.
    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.

    이소옥사졸리딘 유도체와 그의 제조방법
    3.
    发明授权
    이소옥사졸리딘 유도체와 그의 제조방법 失效
    ISOOXAZOLIDINE衍生物及其制备方法

    公开(公告)号：KR1019920003608B1

    公开(公告)日：1992-05-04

    申请号：KR1019890010565

    申请日：1989-07-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이상희 ,  정낙철 ,  김혜령

    IPC: C07D413/10

    Abstract: 5-[4-[5-[3-(4-Fluorophenyl) isoxazolidyl phenyl -(1H)tetrazole of formula (I) is new. Also claimed is the prepn. of (I) which comprises (a) reacting an aldehyde deriv. of formula (II) with a hydroxy amine cpd. to obtain an oxime deriv. of formula (III), (b) halogenating (III) and reacting the obtd. halogenated oxime deriv. with a styrene cpd. of formula (IV), and (c) reacting the obtd. cpd. with an azide cpd. to form (I). The cpd. (I) has an effect on blood pressure and on the contractility of the cardiac muscle.

    Abstract translation: 式（I）的5- [4- [5-（3-氟-4-苯基）异恶唑烷基苯基 - （1H）四唑是新的。 还声称是prepn。 （I），其包含（a）使醛衍生物反应。 的式（II）与羟基胺cpd反应。 得到肟衍生物。 （III），（b）卤化（III）并使该反应物反应。 卤代肟衍生物。 与苯乙烯cpd。 式（Ⅳ），（c）使该反应物反应。 CPD。 与叠氮化合物cpd。 形成（I）。 cpd。 （I）对血压和心肌的收缩力有影响。

    피리다지논 유도체와 그의 제조방법
    10.
    发明授权
    피리다지논 유도체와 그의 제조방법 失效
    吡咯烷酮衍生物

    公开(公告)号：KR1019930011304B1

    公开(公告)日：1993-11-29

    申请号：KR1019900020229

    申请日：1990-12-10

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  정낙철 ,  김형백 ,  신화섭 ,  이상희 ,  이상조 ,  서지희 ,  김혜령 ,  이상구 ,  김낙정 ,  김선주 ,  이병호 ,  이승호 ,  서호원

    IPC: C07D237/04

    Abstract: Ryridazinone derivatives of formula (I) are new. In formula (I), R1= methyl, hydroxymethyl, nitrosylmethyl, monohalomethyl, dihalomethyl or trihalomethyl; X,Y=H, nitro, cyano, -NHCOR3 or - NHSO2R4 (R3,R4= C1-6 alkyl, substituted phenyl or halogen-substd. alkyl); R2=H, C1-6 alkyl, branched alkyl, cyclic alkyl, alkene, alkyne or halogen-substd. alkyl, alkene, alkyne or phenyl-substd. alkyl, alkene, alkyne. Compounds (I) are useful as cardiotonics for enhancing contractile force of cardiac muscle and (I) have antihypertensive activities.

    Abstract translation: 式（I）的哒嗪酮衍生物是新的。 在式（I）中，R 1 =甲基，羟甲基，亚硝基甲基，单卤代甲基，二卤代甲基或三卤代甲基; X，Y = H，硝基，氰基，-NHCOR 3或-NHSO 2 R 4（R 3，R 4 = C 1-6烷基，取代的苯基或卤素取代的烷基）; R2 = H，C1-6烷基，支链烷基，环烷基，烯烃，炔烃或卤素取代基。 烷基，烯烃，炔或苯基。 烷基，烯烃，炔烃。 化合物（I）可用作增强心肌收缩力的强心剂，（I）具有抗高血压活性。

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