84545-15-3Relevant academic research and scientific papers
HALOALKYLGUANIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND METHODS, PROCESSES AND INTERMEDIATES
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, (2008/06/13)
The invention relates to guanidine derivatives 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 1 and R 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 1 and R 2 is halogen substituted, or R 2 is hydrogen and R 1 is R 5--E--W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R. sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring; 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; D is O or S; and R. sup.3 and R 4 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.
