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    • 2. 发明申请
    • PIRYDYL IMIDAZOLE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
    • 吡啶基咪唑衍生物及其制备方法
    • WO1995034564A1
    • 1995-12-21
    • PCT/KR1995000075
    • 1995-06-07
    • KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYYOO, Sung, EunYI, Kyu, YangLEE, Sang, HeeKIM, Hye, RyungSUH, Jee, HeeKIM, Nak, JeongKIM, Seon, JuCHA, Ok, JaSHIN, Young, AhSHIN, Wha, SupLEE, Sung, HouJUNG, Yi, SookLEE, Byung, HoSEO, Ho, WonLEE, Hye, Suk
    • KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    • C07D471/04
    • C07D471/04
    • Novel pyridyl imidazole derivatives of formula (I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity, wherein A is a straight, branched or cyclic C1-C6 alkyl or alkenyl group, OR (wherein R is a hydrogen, or a straight, branched or cyclic C1-C6 alkyl or alkenyl radical), or NR R (wherein R and R are independently a hydrogen, or a straight, branched or cyclic C1-C6 alkyl radical); B is a group of formula (II); D is a hydrogen; a halogen; a straight, branched or cyclic C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl group which is optionally substituted with OH, a C1-C4 alkoxy radical, CO2R , COR , CON(R )2 or N(R )2, wherein R is the same as defined above; tetrazol-5-yl; a perfluoro-C1-C4 alkyl group; or N(R )2, OR , CO2R or CON(R )2, wherein R is the same as defined above; E is a hydrogen; a halogen; a straight or branched C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl group which is optionally substituted with OH, a C1-C4 alkoxy radical, CO2R , COR , CON(R )2 or N(R )2, wherein R is the same as defined above; a perfluoro-C1-C4 alkyl group; NO2; or N(R )2 or OR , wherein R is the same as defined above; and n is 0 or an integer of 1 to 4.
    • 式(I)的新型吡啶基咪唑衍生物有效地抑制血管紧张素II的作用并具有优异的抗高血压活性,其中A是直链,支链或环状的C 1 -C 6烷基或链烯基,OR 1(其中R 1, 是氢或直链,支链或环状的C 1 -C 6烷基或链烯基)或NR 2 R 3(其中R 2和R 3独立地是氢或直链,支链 或环状C 1 -C 6烷基); B是式(II)的一组; D是氢; 卤素 任选被OH,C 1 -C 4烷氧基,CO 2 R 1,COR 1,CON(R 1)取代的直链,支链或环状C 1 -C 6烷基,C 2 -C 6烯基或C 2 -C 6炔基 >)2或N(R 1)2,其中R 1与上述定义相同; 四唑-5-基; 全氟-C 1 -C 4烷基; 或N(R 1)2,OR 1,CO 2 R 1或CON(R 1)2,其中R 1与上述定义相同; E是氢; 卤素 任选被OH,C 1 -C 4烷氧基,CO 2 R 1,COR 1,CON(R 1)烷基取代的直链或支链C 1 -C 6烷基,C 2 -C 6烯基或C 2 -C 6炔基, 2或N(R 1)2,其中R 1与上述定义相同; 全氟-C 1 -C 4烷基; NO2; 或N(R 1)2或OR 1,其中R 1与上述定义相同; n为0或1〜4的整数。