Method of inhibiting histamine activity with quanidine compounds
AssigneeSmith Kline & French Laboratories Limited
InventorsJames Whyte Black, Graham John Durant, John Colin Emmett, Charon Robin Ganellin
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Abstract
A method of inhibiting histamine activity, in particular inhibiting H-2 histamine receptors, by administering heterocyclicalkylguanidines.
Claims5
A method of inhibiting H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, which comprises administering internally to an animal requiring inhibition of said H-2 histamine receptors in an amount sufficient to inhibit said H-2 histamine receptors a compound of the formula:
- ##STR7## in which:
- n is 2 to 5;
- A taken together with the carbon and nitrogen atoms to which it is attached forms a triazole;
- R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl;
- R.sub.2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R.sub.1 and R.sub.2 together form an ethylene bridge and
- R.sub.3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
A method of inhibiting gastric acid secretion which comprises administering internally to an animal requiring inhibition of gastric acid secretion in an amount sufficient to inhibit gastric acid secretion a compound of the formula ##STR8## in which:
- n is 2 to 5;
- A taken together with the carbon and nitrogen atoms to which it is attached forms a triazole;
- R.sub.1 is hydrogen, alkyl having 1 to 4 carbon atoms or benzyl;
- R.sub.2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R.sub.1 and R.sub.2 together form an ethylene bridge and
- R.sub.3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
A method of producing anti-inflammatory activity which comprises administering to an animal requiring said activity in an amount sufficient to produce said activity a compound of the formula:
- ##STR9## in which:
- n is 2 to 5;
- A taken together with the carbon and nitrogen atoms to which it is attached forms a triazole;
- R.sub.1 hydrogen, alkyl having 1 to 4 carbon atoms or benzyl;
- R.sub.2 is hydrogen, alkyl having 1 to 4 carbon atoms, benzyl, imidazolylethyl or amino or R.sub.1 and R.sub.2 together form an ethylene bridge and
- R.sub.3 is hydrogen, alkyl having 1 to 4 carbon atoms, alkylthio having 1 to 4 carbon atoms or amino or pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.