Carbonyl derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514322, 514323, 514324, 546279, 546275, 514337, 546276, 546277, 514252, 546278, 546280, 514255, 544211, 546281, 514269, 546282, 546283, 514272, 546284, 546193, 514274, 546194, 546261, 514256, 546262, 546265, 514275, 546307, 546308, 514318, 546309, 546293, 514332, 546296, 546297, 514335, 546141, 546142, 514340, 546143, 546145, 514341, 546153, 546155, 514342, 546156, 544284, 514343, 544295, 544296, 514352, 544198, 544199, 514353, 544209, 544210, 514344, 544212, 544194, 514348, 544317, 544205, 514349, 544207,

Patent

active

046579087

ABSTRACT:
The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where 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.5 -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.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 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; D is O or S; R.sup.4 is H or 1-6C alkyl; R.sup.3 is H 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.

REFERENCES:
patent: 4496564 (1985-01-01), Yellin et al.
patent: 4496571 (1985-01-01), Yellin et al.
patent: 4604465 (1986-08-01), Yellin et al.

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