Pharmacologically active compounds
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham J. Durant, John C. Emmett, Charon R. Ganellin
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Abstract
Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.
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 to an animal in need of inhibition of said receptors in an effective amount to inhibit said receptors a heterocyclic compound of the formula:
- ##STR4## wherein A taken together with the nitrogen and carbon atoms show forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups;
- R is a grouping of the formula:
- Het--CH.sub.2 Z(CH.sub.2).sub.n --
- wherein Het is a nitrogen containing heterocyclic ring selected from pyridine, thiazole, isothiazole or thiadiazole, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen;
- Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
A method of inhibiting gastric acid secretion which comprises administering internally to an animal in need of inhibition of gastric acid secretion in an effective amount to inhibit gastric acid secretion a heterocyclic compound of the formula:
- ##STR5## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups;
- R is a group of the formula:
- Het--CH.sub.2 Z(CH.sub.2).sub.n --
- wherein Het is a nitrogen containing heterocyclic ring selected from pyridine, thiazole, isothiazole or thiadiazole, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen;
- Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptacle acid addition salt thereof.
A pharmaceutical composition to inhibit H-2 histamine receptors, said H-2 histamine receptors being those histamine receptors which are not inhibited by mepyramine but are inhibited by burimamide, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a heterocyclic compound of the formula:
- ##STR6## wherein A taken together with the nitrogen and carbon atoms shown forms a pyridine ring, said ring having a keto or thione group and optionally substituted by one or two lower alkyl, phenyl or benzyl groups;
- R is a grouping of the formula:
- Het--CH.sub.2 Z(CH.sub.2).sub.n --
- wherein Het is a nitrogen containing heterocyclic ring selected from pyridine, thiazole, isothiazole or thiadiazole, said ring being optionally substituted by lower alkyl, amino, hydroxy or halogen;
- Z is sulphur or a methylene group and n is 2 or 3 or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.