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Pyridopyrazine and quinoxaline derivatives, processes for their preparation, and pharmaceutical compositions containing them
Pyridopyrazine and quinoxaline derivatives, processes for their preparation, and pharmaceutical compositions containing them
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机译:吡咯并吡嗪和喹喔啉衍生物,其制备方法以及含有它们的药物组合物
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摘要
There are described compounds of formula I,;in which R1 is phenyl substituted by halogen, alkoxy, alkyl, carboxy-alkyl, -NR4R5, carboxy or alkoxy carbonyl,;R3 is hydrogen, alkyl, mono- or di-carboxy alkyl, halo, alkoxy, phenyl, halo-phenyl, hydroxy, phenoxy, thiol, thioalkoxy, thiophenoxy, -NR4Rs, cyano, -COOH, carboxyureido, -CF3, -CORe, hydroxyalkyl, aminoalkyl, or alkoxy substituted by NR4R5,;ring A is a benzene or a pyridine ring which optionally carries up to 4 substituents R3, which may be the same or different,;R4 and Rs, which may be the same or different, each represent hydrogen, phenyl, halophenyl or alkyl, the alkyl optionally being substituted by alkoxy or by a mono- or di- alkyl or unsubstituted amino group; or R4 and Rs, together with the nitrogen atom to which they are attached, form a piperidine, morpholine or an optionally alkyl substitued piperazine ring, and;R6 is hydrogen or alkyl,;provided that (i) when R, is phenyl substituted by chlorine or bromine, ring A is not a benzene ring substituted by chlorine or bromine, or (ii) when R, is phenyl substituted by methoxy R3 is not phenyl,;and pharmaceutically acceptable salts, esters and amides thereof.;There are also described methods for making the compounds and pharmaceutical, e.g. anti-inflammatory, compositions containing the compounds.
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机译:描述了式I的化合物, <图像文件=“ IMGA0001.GIF” he =“ 20” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 50” /> Chemistry>; in其中R 1 Sub>是被卤素,烷氧基,烷基,羧基-烷基,-NR 4 Sub> R 5 Sub>,羧基或烷氧基羰基取代的苯基; R 3 Sub>是氢,烷基,单或二羧基烷基,卤素,烷氧基,苯基,卤代苯基,羟基,苯氧基,硫醇,硫代烷氧基,硫代苯氧基,-NR 4 Sub> R s Sub>,氰基,-COOH,羧基脲基,-CF 3 Sub>,-CORe,羟烷基,氨基烷基或被NR 4 Sub>取代的烷氧基R 5 Sub> ,;环A为苯或吡啶环,其任选地带有多达4个可以相同或不同的取代基R 3 Sub>;可以相同或不同的4 Sub>和R s Sub>分别代表氢,苯基,卤代苯基或烷基,所述烷基任选地被烷氧基或被单或二烷基取代或未取代的氨基;或R 4 Sub>和R s Sub>,与它们所连接的氮原子一起形成哌啶,吗啉或烷基取代的哌嗪环, > 6 Sub>是氢或烷基,但前提是:(i)当R 1是被氯或溴取代的苯基时,环A不是被氯或溴取代的苯环,或(ii)当R 1是苯基时被甲氧基R 3 Sub>取代的不是苯基;及其药学上可接受的盐,酯和酰胺。;还描述了制备化合物和药物的方法,例如抗炎药,含有该化合物的组合物。
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