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    신규의치환된이미다졸유도체및그의제조방법
    13.
    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.

    벤조피란 유도체와 그의 제조방법
    17.
    发明授权
    벤조피란 유도체와 그의 제조방법 失效
    新型苯并噻吩衍生物及其制备方法

    公开(公告)号：KR1019930011040B1

    公开(公告)日：1993-11-20

    申请号：KR1019900019034

    申请日：1990-11-23

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  이규양 ,  서지희 ,  신화섭 ,  이병호

    IPC: C07D405/04

    Abstract: Novel benzopyran derivatives of formula (I) are prepared by O- nitration at C-3 hydroxy group of cromakalim of formula (II) in the anhydride acetic acid or C.H2SO4. In the formula (I), R1 R2=H, NO2, nitryl; R3= 2-oxo-1-pyrrolidinyl. Compound (I) are useful as antihypertensive and vasodilating agents.

    Abstract translation: 式（I）的新型苯并吡喃衍生物通过在酸酐乙酸或C.H 2 SO 4中通过式（II）的cromakalim的C-3羟基进行O-硝化来制备。 在式（I）中，R1R2 = H，NO2，硝基; R3 = 2-氧代-1-吡咯烷基。 化合物（I）可用作抗高血压药和血管舒张剂。

    인단 유도체와 그의 제조방법
    18.
    发明授权
    인단 유도체와 그의 제조방법 失效
    制备印度衍生物的方法

    公开(公告)号：KR1019930006765B1

    公开(公告)日：1993-07-23

    申请号：KR1019910001326

    申请日：1991-01-26

    Applicant: 한국화학연구원

    Inventor： 유성은 ,  서지희 ,  이규양 ,  신화섭 ,  이병호 ,  서호원

    IPC: C07D207/26 ,  C07D207/24

    Abstract: Indane derivs. of formula (I) are new. In (I), R1= nitro, nitrile, halogen, amino, CF3, -(C=NH)-OMe, -NHCOCS3, -NHCSCX3, - COR4, -OCX3 OR -CSR4; X=H or halogen; R4=H, amino, lower alkyl or alkoxy, or opt. substd. phenyl; R2=-NO5R6, a gp. of formula (II), a gp. of formula (III), a gp. of formula (IV), etc.; R5 and R6 each=H, lower alkyl, cyclopropyl, cyclopropyl methyl or benzyl; n = 1 or 2; Y=CH2, O, S or -NR4; R3=H, OH, nitrooxy, formyloxy, alkanoyloxy, haloalkanoyloxy, alkoxycarbonyl, aroyloxy or carbamoyloxy. The cpds. (2) may be used in the treatment of hypertension.

    Abstract translation: indane派生。 式（I）的化合物是新的。 在（I）中，R1 =硝基，腈，卤素，氨基，CF3， - （C = NH）-OMe，-NHCOCS3，-NHCSCX3，-COR4，-OCX3或-CSR4; X = H或卤素; R4 = H，氨基，低级烷基或烷氧基，或选择。 substd。 苯基; R2 = -NO5R6，gp。 的式（II），gp。 的式（III），gp。 的式（IV）等; R5和R6各自为H，低级烷基，环丙基，环丙基甲基或苄基; n = 1或2; Y = CH 2，O，S或-NR 4; R3 = H，OH，硝基氧基，甲酰氧基，烷酰氧基，卤代烷酰氧基，烷氧基羰基，芳氧基或氨基甲酰氧基。 cpds。 （2）可用于治疗高血压。

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