| 摘要 |
<p>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:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="26" wi="86" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry></p><p>in which R<Sup>1</Sup> and R<Sup>2</Sup>, 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</Sup> and R<Sup>2</Sup> is halogen substituted, or R<Sup>2</Sup> is hydrogen and R<Sup>1</Sup> is R<Sup>3-</Sup>E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, S0<Sub>2</Sub> or NR<Sup>4</Sup> in which R<Sup>4</Sup> is H or 1-6C alkyl, R<Sup>3</Sup> is H or 1-6C alkyl optionally substituted by 1 or 21-4C alkyls, or R<Sup>3</Sup> and R<Sup>4</Sup> are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R<Sup>2</Sup> is H and R<Sup>1</Sup> 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 or7-11C aroyl; ring X is a heterocyclic ring.</p><p>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 and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.</p> |
