发明授权
US4288443A Substituted furan compounds and pharmaceutical compositions containing
them
失效
取代的呋喃化合物和含有它们的药物组合物
- 专利标题: Substituted furan compounds and pharmaceutical compositions containing them
- 专利标题(中): 取代的呋喃化合物和含有它们的药物组合物
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申请号: US124115申请日: 1980-02-25
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公开(公告)号: US4288443A公开(公告)日: 1981-09-08
- 发明人: Duncan B. Judd , John W. Clitherow , Barry J. Price , John Bradshaw
- 申请人: Duncan B. Judd , John W. Clitherow , Barry J. Price , John Bradshaw
- 申请人地址: GB2 London
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB2 London
- 优先权: GBX42256/77 19771011
- 主分类号: A61K31/34
- IPC分类号: A61K31/34 ; A61K31/341 ; A61P1/04 ; C07D307/52 ; C07D307/56 ; C07D307/68 ; C07D307/54
摘要:
The invention relates to compounds of the general formula ##STR1## and physiologically acceptable salts and N-oxides, hydrates and bioprecursors thereof, in which R.sub.1 and R.sub.2 which may be the same or different each represent hydrogen, C.sub.1-8 alkyl, C.sub.4-8 cycloalkyl, C.sub.3-6 alkenyl, aralkyl with 1 to 4 carbon atoms in the alkyl residue or C.sub.1-8 alkyl interrupted by an oxygen atom or a group ##STR2## in which R.sub.5 represents hydrogen or C.sub.1-8 alkyl, or R.sub.1 and R.sub.2 may together with the nitrogen atom to which they are attached, form a saturated monocyclic 5 to 7 membered heterocyclic ring which may additionally contain the heterofunction O or ##STR3## R.sub.3 represents straight or branched chain C.sub.1-8 alkyl, alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue, C.sub.1-8 hydroxyalkyl, C.sub.1-8 alkoxycarbonyl, alkyl thioalkyl with 1 to 8 carbon atoms in each alkyl residue, halogen or aryl;R.sub.4 represents hydrogen, C.sub.1-8 alkyl, C.sub.3-6 alkenyl or alkoxyalkyl with 1 to 8 carbon atoms in each alkyl residue;X represents --O-- or --S--;Y represents .dbd.S, .dbd.O, .dbd.NR.sub.6 or .dbd.CHNO.sub.2 where R.sub.6 represents hydrogen, nitro, cyano, C.sub.1-8 alkyl, aryl, C.sub.1-8 alkylsulphonyl or arylsulphonyl;m represents an integer from 2 to 4 inclusive; andn represents an integer which is 1 or 2, or additionally when X is --S-- n may also be zero.The invention also relates to processes for the production of such compounds, pharmaceutical compositions containing them and certain novel intermediates used in their production, i.e. amines of the formula ##STR4## and alcohols of the formula ##STR5## The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.
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