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2. 发明公开

EP0778275A1 Process for the preparation of imidazole, triazole and tetrazole derivatives and their use as selective 5-HT-1 receptor agonists 失效
标题翻译：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
公开(公告)号：EP0778275A1
公开(公告)日：1997-06-11
申请号：EP97200467.5
申请日：1992-01-24
申请人： MERCK SHARP & DOHME LTD.
发明人： Baker, Raymond , Matassa, Victor , Street, Leslie J.
IPC分类号： C07D403/04 , C07D403/06 , C07D409/04 , C07D409/06 , C07D403/14 , C07D409/14 , A61K31/445
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/04
摘要： 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.
摘要翻译：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。

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