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    • 2. 发明授权
    • Pyridyl imidazole derivatives and processes for the preparation thereof
    • 吡啶基咪唑衍生物及其制备方法
    • US5691348A
    • 1997-11-25
    • US750460
    • 1996-12-08
    • Sung-Eun YooKyu-Yang YiSang-Hee LeeHye-Ryung KimJee-Hee SuhNak-Jeong KimSeon-Ju KimOk-Ja ChaYoung-Ah ShinWha-Sup ShinSung-Hou LeeYi-Sook JungByung-Ho LeeHo-Won SeoHye-Suk Lee
    • Sung-Eun YooKyu-Yang YiSang-Hee LeeHye-Ryung KimJee-Hee SuhNak-Jeong KimSeon-Ju KimOk-Ja ChaYoung-Ah ShinWha-Sup ShinSung-Hou LeeYi-Sook JungByung-Ho LeeHo-Won SeoHye-Suk Lee
    • A61K31/435A61K31/44A61P9/12A61P43/00C07D471/04
    • C07D471/04
    • Novel pyridyl imidazole derivatives of formula(I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity: ##STR1## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl group, OR.sup.1 (wherein R.sup.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl radical), or NR.sup.2 R.sup.3 (wherein R.sup.2 and R.sup.3 are independently a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical); B is a group of the following formula ##STR2## D is a hydrogen; a halogen; a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; tetrazol-5-yl; a perfluoro-C.sub.1 -C.sub.4 alkyl group; or N(R.sup.1).sub.2, OR.sup.1, CO.sub.2 R.sup.1 or CON(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; E is a hydrogen; a halogen; a straight or branched C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; a perfluoro-C.sub.1 -C.sub.4 alkyl group; NO.sub.2 ; or N(R.sup.1).sub.2 or OR.sup.1, wherein R.sup.1 is the same as defined above; and n is 0 or an integer of 1 to 4.
    • PCT No.PCT / KR95 / 00075 Sec。 371日期1996年12月6日第 102(e)日期1996年12月6日PCT归档1995年6月7日PCT公布。 出版物WO95 / 34564 日期:1995年12月21日新型式(I)吡啶基咪唑衍生物有效抑制血管紧张素II的作用,具有优异的抗高血压活性:d或环状C 1 -C 6烷基或链烯基,OR 1(其中R 1为氢或直链 ,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,支链或环状的C 1 -C 6烷基); B是一组下列公式: 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)2或N(R 1)2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 其中R1与上述相同; 四唑-5-基; 全氟-C 1 -C 4烷基; 或N(R1)2,OR1,CO2R1或CON(R1)2,其中R1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)2或N(R 1)2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,其中 R1与上述定义相同; 全氟-C 1 -C 4烷基; NO2; 或N(R1)2或OR1,其中R1与上述定义相同; n为0或1〜4的整数。