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42. 发明公开

EP0708776A1 ANTIALLERGIC IMIDAZOAZEPINES 失效
标题翻译：抗惊厥药咪唑安定
公开(公告)号：EP0708776A1
公开(公告)日：1996-05-01
申请号：EP94924248.0
申请日：1994-07-06
申请人： JANSSEN PHARMACEUTICA N.V.
发明人： JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth
IPC分类号： A61K31 , A61P11 , A61P17 , A61P27 , A61P37 , C07D401 , C07D405 , C07D409 , C07D471 , C07D487 , C07D491 , C07D495 , C07D513 , C07D519
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/14 , C07D491/14 , C07D495/14 , C07D513/04
摘要： The present invention is concerned with novel imidazoazepines of formula (I), the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein each of the dotted lines independently represents an optional bond; -A-B- is a radical of formula -X-CH=CH- (a-1); -CH=CH-X- (a-2); or -CH=CH-CH=CH- (a-3); X represents O, S or NR1; R1 represents hydrogen or C¿1-6?alkyl; -^¨B7-^¨B7-^¨B7-^¨B7Y is a radical of formula =O (b-1); -OH (b-2); or =N-OH (b-3); and L represents hydrogen, C1-4alkylcarbonyl, C1-4alkyloxycarbonyl, phenylcarbonyl, C1-6alkyl or C1-6alkyl substituted with C1-4alkyloxycarbonyl, hydroxycarbonyl, aryl, aryloxy or a radical of formula (c), wherein -D-Z- is -S-CH=CH-, -S-CH2-CH2-, -S-CH2-CH2-CH2-, -CH=CH-CH=CH- or -CH2-CH2-CH2-CH2-; and aryl is phenyl or phenyl substituted with halo, hydroxy or C1-4alkyloxy. Compositions comprising said compounds, processes for preparing the same and the use of these compounds for treating allergic diseases.
摘要翻译：本发明涉及式（I）的新型咪唑并吖庚因，其药学上可接受的加成盐和立体化学异构形式，其中每个虚线独立地表示任选的键; -A-B-是式-X-CH = CH-（a-1）的基团; -CH = CH-X-（a-2）; 或-CH = CH-CH = CH-（a-3）; X代表O，S或NR1; R1代表氢或C1-6烷基; B7是B = O（b-1）的基团。 -OH（b-2）; 或= N-OH（b-3）; 和L代表氢，C1-4烷基羰基，C1-4烷氧基羰基，苯基羰基，C1-6烷基或被C1-4烷氧基羰基，羟基羰基，芳基，芳氧基或式（c）基团取代的C1-6烷基，其中-DZ-为-S- CH = CH - ， - S-CH 2 -CH 2 - ， - S-CH 2 -CH 2 -CH 2 - ， - CH = CH-CH = CH-或-CH 2 -CH 2 -CH 2 -CH 2 - 芳基是苯基或被卤素，羟基或C 1-4烷氧基取代的苯基。包含所述化合物的组合物，其制备方法以及这些化合物用于治疗过敏性疾病的用途。

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