首页> 外国专利> Heterocykliske derivater, farmaceutiske præparater indeholdende disse, deres anvendelse ved behandlingen af histaminformidlede tilstande i hjernen samt fremgangsmåder til deres fremstilling

Heterocykliske derivater, farmaceutiske præparater indeholdende disse, deres anvendelse ved behandlingen af histaminformidlede tilstande i hjernen samt fremgangsmåder til deres fremstilling

机译:杂环衍生物,含有它们的药物制剂,其在治疗组胺介导的脑部疾病中的用途及其制备方法

摘要

Compounds of the formula (I) : …CHEM… or pharmaceutically acceptable salts thereof, wherein : …??R1 and R2 are independently C1-4alkyl; or R1 and R2 together with the nitrogen atom to which they are joined represent a pyrrolidino, piperidino or hexahydroazepino ring; Y is straight-chain or branched-chain C1-4alkyl; n is 2 to 5; m is 0 or 1; when m is 1, Z is inter alia an optionally substituted pyridine, pyrimidine, oxazole, thiazole, imidazole, benzoxazole benzthiazole or N-alkylbenzimidazole ring; when m is 0, Z is an optionally substituted imidazole, pyrazole or benzimidazole ring. …??The compounds are histamine H2-receptors antagonists and relatively lipophilic and can penetrate the blood-brain barrier and are useful in treating diseases mediated via histamine H2- receptors. Processes for their preparation, pharmaceutical compositions and methods of use are described.
机译:式(I)化合物:……或其药学上可接受的盐,其中:…·R 1和R 2独立地为C 1-4烷基; R 1和R 2以及与它们连接的氮原子一起表示吡咯烷基,哌啶子基或六氢氮杂环庚烷环; Y是直链或支链的C1-4烷基; n为2至5; m为0或1;当m为1时,Z尤其是任选取代的吡啶,嘧啶,恶唑,噻唑,咪唑,苯并恶唑苯并噻唑或N-烷基苯并咪唑环;当m为0时,Z为任选取代的咪唑,吡唑或苯并咪唑环。该化合物是组胺H2受体拮抗剂,相对亲脂,可以穿透血脑屏障,可用于治疗通过组胺H2受体介导的疾病。描述了其制备方法,药物组合物和使用方法。

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