发明授权
- 专利标题: Nitrogen heterocycles
- 专利标题(中): 氮杂环
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申请号: US356503申请日: 1982-03-09
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公开(公告)号: US4460584A公开(公告)日: 1984-07-17
- 发明人: Derrick F. Jones , Keith Oldham
- 申请人: Derrick F. Jones , Keith Oldham
- 申请人地址: GB2 London
- 专利权人: Imperial Chemical Industries PLC
- 当前专利权人: Imperial Chemical Industries PLC
- 当前专利权人地址: GB2 London
- 优先权: GBX8108048 19810313
- 主分类号: C07D239/47
- IPC分类号: C07D239/47 ; A61K31/505 ; A61P1/04 ; A61P43/00 ; C07D239/46 ; C07D249/12 ; C07D401/12 ; C07D403/06 ; C07D403/12 ; C07D521/00 ; A61K31/44
摘要:
The invention relates to nitrogen heterocycles which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.3 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.4 in which R.sup.4 is H or 1-6C alkyl, R.sup.3 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.3 R.sup.4 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.1 is H, 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene, or a 1-8C alkylene into which is optionally inserted one or two groups; ring Y is a heterocyclic ring described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
公开/授权文献
- US5461157A Process for preparing pyrrolidinylacetamide derivatives 公开/授权日:1995-10-24
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