Heterocyclic derivatives

Details Heterocyclic derivatives Heterocyclic derivatives

1982-03-01

1989-01-03

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544218, 544295, 544296, 544298, 544331, 544333, 544357, 544364, 544366, 544367, 544369, 548128, 548130, 548131, 548133, 548184, 548190, 548191, 548194, 548225, 548228, 548235, 548252, 548255, 548263, 548265, 548266, 548267, 548269, 548336, 548348, 548374, A61K 31495, C07D40304

Patent

active

047957557

ABSTRACT:
This invention relates to heterocyclic 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, 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 2-6 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; 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; and R.sup.3 and R.sup.4 are a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

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patent: 4165378 (1979-08-01), Gilman et al.
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patent: 4242351 (1980-12-01), Yellin et al.
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patent: 4315009 (1982-02-01), Jones et al.
patent: 4342765 (1982-08-01), Jones et al.
patent: 4362728 (1982-12-01), Yellin et al.
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"Derwent Abstracts", 74415 C/42, B03, Yama 2/28/79.
"Derwent Abstracts", 74408 C/42, B03, Yama, 3/2/79.

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