发明公开
EP0181163A3 Heterocyclic phenoxy derivatives having an antihistamine H2 activity
失效
具有抗病毒H2活性的间苯二酚衍生物
- 专利标题: Heterocyclic phenoxy derivatives having an antihistamine H2 activity
- 专利标题(中): 具有抗病毒H2活性的间苯二酚衍生物
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申请号: EP85307929申请日: 1985-10-31
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公开(公告)号: EP0181163A3公开(公告)日: 1987-02-25
- 发明人: Young, Rodney Christopher , Smith, Ian Ross , Brown, Thomas Henry , Mitchell, Robert Christopher
- 申请人: SMITH KLINE & FRENCH LABORATORIES LIMITED
- 专利权人: SMITH KLINE & FRENCH LABORATORIES LIMITED
- 当前专利权人: SMITH KLINE & FRENCH LABORATORIES LIMITED
- 优先权: GB8427878 19841103; GB8517714 19850713
- 主分类号: C07D295/08
- 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
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.
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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