Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...
Patent
1982-03-01
1984-05-29
Gerstl, Robert
Drug, bio-affecting and body treating compositions
Antigen, epitope, or other immunospecific immunoeffector
Bacterium or component thereof or substance produced by said...
424251, 424263, 424269, 424270, 424272, 424273R, 424273P, 544194, 544204, 544317, 544335, 544336, 544408, 546297, 546308, 548128, 548130, 548132, 548133, 548184, 548193, 548230, 548235, 548255, 548265, 548266, 548301, 548362, C07D23942, C07D23934, A61K 3151
Patent
active
044514638
ABSTRACT:
This invention relates to alcohol 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.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 alkyl, 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 hydrogen and R.sup.1 is hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C arylalkyl or 7-11C aroyl, the aryl, arylalkyl and aroyl radicals being optionally substituted, 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 oxygen or sulphur; R.sup.3, R.sup.4 and R.sup.5 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.
REFERENCES:
patent: 4242350 (1980-12-01), Yellin et al.
patent: 4242351 (1980-12-01), Yellin et al.
patent: 4244966 (1981-01-01), Lippmann et al.
patent: 4267189 (1981-05-01), Lippmann et al.
patent: 4315009 (1982-02-01), Jones et al.
patent: 4342765 (1982-08-01), Jones et al.
patent: 4362728 (1982-12-01), Yellin
Gerstl Robert
Imperial Chemical Industries plc
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