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公开(公告)号：EP0181163B1
公开(公告)日：1989-12-20
申请号：EP85307929.1
申请日：1985-10-31
发明人： Young, Rodney Christopher , Smith, Ian Ross , Brown, Thomas Henry , Mitchell, Robert Christopher
IPC分类号： C07D295/08 , C07D213/74 , C07D215/38 , C07D239/42 , C07D277/82 , C07D277/42 , C07D235/30 , C07D217/22 , C07D277/46 , C07D239/94 , C07D277/68
CPC分类号： C07D213/74 , C07D215/38 , C07D215/42 , C07D217/22 , C07D231/12 , C07D233/64 , C07D235/12 , C07D235/30 , C07D239/42 , C07D239/94 , C07D263/58 , C07D277/42 , C07D277/82
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2.发明公开Heterocyclic phenoxy derivatives having an antihistamine H2 activity 失效Heterocyclische Phenoxyderivate die eine Antihistamin-H2-Wirkung besitzen。
公开(公告)号：EP0181163A2
公开(公告)日：1986-05-14
申请号：EP85307929.1
申请日：1985-10-31
发明人： Young, Rodney Christopher , Smith, Ian Ross , Brown, Thomas Henry , Mitchell, Robert Christopher
IPC分类号： C07D295/08 , C07D213/74 , C07D215/38 , C07D239/42 , C07D277/82 , C07D277/42 , C07D235/30 , C07D217/22 , C07D277/46 , C07D239/94 , C07D277/68
CPC分类号： C07D213/74 , C07D215/38 , C07D215/42 , C07D217/22 , C07D231/12 , C07D233/64 , C07D235/12 , C07D235/30 , C07D239/42 , C07D239/94 , C07D263/58 , C07D277/42 , C07D277/82
摘要： Compounds of the formula (I):
or pharmaceutically acceptable salts thereof, wherein :
R 1 and R 2 are independently C 1-4 alkyl; or R 1 and R 2 together with the nitrogen atom to which they are joined represent a pyrrolidino, piperidino or hexahydroazepino ring; Y is straight-chain or branched-chain C 1-4 alkyl; 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 H 2 -receptors antagonists and relatively lipophilic and can penetrate the blood-brain barrier and are useful in treating diseases mediated via histamine H 2 -receptors. Processes for their preparation, pharmaceutical compositions and methods of use are described.摘要翻译： 式（I）的化合物：其或其药学上可接受的盐，其中：R 1和R 2独立地是C 1-4烷基; 或R 1和R 2与它们所连接的氮原子一起代表吡咯烷子基，哌啶子基或六氢氮杂环; Y是直链或支链C 1-4烷基; n为2〜5; m为0或1; 当m为1时，Z特别是任选取代的吡啶，嘧啶，恶唑，噻唑，咪唑，苯并恶唑苯噻唑或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。 化合物是组胺H2受体拮抗剂并且相对亲脂并且可以渗透血脑屏障，并且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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公开(公告)号：EP0181163A3
公开(公告)日：1987-02-25
申请号：EP85307929
申请日：1985-10-31
发明人： Young, Rodney Christopher , Smith, Ian Ross , Brown, Thomas Henry , Mitchell, Robert Christopher
IPC分类号： C07D295/08 , C07D213/74 , C07D215/38 , C07D239/42 , C07D277/82 , C07D277/42 , C07D235/30 , C07D217/22 , C07D277/46 , C07D239/94 , C07D277/68
CPC分类号： C07D213/74 , C07D215/38 , C07D215/42 , C07D217/22 , C07D231/12 , C07D233/64 , C07D235/12 , C07D235/30 , C07D239/42 , C07D239/94 , C07D263/58 , C07D277/42 , C07D277/82
摘要： Compounds of the formula (I):
or pharmaceutically acceptable salts thereof, wherein : R 1 and R 2 are independently C 1-4 alkyl; or R 1 and R 2 together with the nitrogen atom to which they are joined represent a pyrrolidino, piperidino or hexahydroazepino ring; Y is straight-chain or branched-chain C 1-4 alkyl; 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 H 2 -receptors antagonists and relatively lipophilic and can penetrate the blood-brain barrier and are useful in treating diseases mediated via histamine H 2 -receptors. Processes for their preparation, pharmaceutical compositions and methods of use are described.
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