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    • 1. 发明公开
    • Process for the preparation of imidazole, triazole and tetrazole derivatives and their use as selective 5-HT-1 receptor agonists
    • 一种用于咪唑,三唑和四唑衍生物的制备和它们作为选择性5-HT 1受体激动剂的使用过程
    • EP0778275A1
    • 1997-06-11
    • EP97200467.5
    • 1992-01-24
    • MERCK SHARP & DOHME LTD.
    • Baker, RaymondMatassa, VictorStreet, Leslie J.
    • C07D403/04C07D403/06C07D409/04C07D409/06C07D403/14C07D409/14A61K31/445
    • C07D231/12C07D233/56C07D249/08C07D401/14C07D403/04C07D403/06C07D403/14C07D409/04
    • A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT 1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
      wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring;
         two, three or four of V,W,X,Y and Z represent nitrogen and the remainder represent carbon provided that, when two of V,W,X,Y and Z represent nitrogen and the remainer represent carbon, then the said nitrogen atoms are in non-adjacent positions within the five-membered ring;

      A 1 represents hydrogen, methyl, ethyl, benzyl or amino;
      A 2 represents a non-bonded electron pair when four of V,W,X,Y and Z represent notrogen and the other represents carbon; or, when two or three of V,W,X,Y and Z represent nitrogen and the remainder represent carbon, A 2 represents hydrogen, methyl, ethyl, benzyl or amino;
      E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms;
      F represents a group of formula

      U represents nitrogen or C-R 2 ;
      B represents oxygen, sulphur or N-R 3 ;
      R 1 represents -CH 2 .CHR 4 .NR 6 R 7 or a group of formula

      in which the broken line represents an optional chemical bond; and R 2 ,R 3 ,R 4 ,R 5 ,R 6 and R 7 independently represent hydrogen or C 1-6 alkyl.
    • 一类substituiertem咪唑,三唑和四唑衍生物是5-HT 1样受体的选择性激动剂和治疗是有用的。因此临床病症,特别是偏头痛和相关病症,对此受体论文的选择性激动剂被指示。 worin的虚线圆darstellt在五元环中任何位置的两个不相邻双键; 两个,三个或V的4,W,X,Y和Z表示氮,余下的表示碳条件是,当V中的两个,W,X,Y和Z表示氮,滞留者表示碳,则所述氮原子 是在五元环内的非相邻位置; A <1> darstellt氢,甲基,乙基,苄基或氨基; A <2> darstellt非成键电子对当V四个,W,X,Y和Z表示notrogen和其他darstellt碳; 或者,当两个或三个的V,W,X,Y和Z表示氮,余下的表示碳,A <2> darstellt氢,甲基,乙基,苄基或氨基; E表示一个键或一个直链或支链的亚烷基链含有1至4个碳原子; ˚Fdarstellt式的基团 u的darstellt氮或C-R <2>; 乙darstellt氧,硫或N-R <3>; [R <1> darstellt -CH2.CHR <4> .NR <6> - [R <7>或式的基团,其中任选的化学键的虚线darstellt; 且R <2>,R <3>,R <4>,R <5> - [R <6>和R <7>独立地代表氢或C 1-6烷基。