Pharmacologically active thiourea and urea compounds as inhibitors of H-2 histamine receptors
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham John Durant, John Colin Emmett, Charon Robin Ganellin
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Abstract
The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
Claims13
A pharmaceutical composition to inhibit H-2 histamine receptors comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a heterocyclic compound of the formula:
- ##STR28## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a pyrimidine, pyrazine or pyridazine ring;
- X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR29## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen, k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4;
- Y is oxygen, sulphur or NH;
- E is oxygen or sulphur;
- and R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylaminolower alkyl or a pharmaceutically acceptable addition salt thereof.
A method of inhibiting H-2 histamine receptors which comprises administering to an animal in need thereof in an effective amount to inhibit said receptors a heterocyclic compound of the formula:
- ##STR30## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a pyrimidine, pyrazine or pyridazine ring;
- X.sub. is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR31## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen, k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4;
- Y is oxygen, sulphur or NH;
- E is oxygen or sulphur;
- and R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylaminolower alkyl or a pharmaceutically acceptable addition salt thereof.
A method of inhibiting gastric acid secretion which comprises administering to an animal in need thereof in an effective amount to inhibit gastric acid secretion a heterocyclic compound of the formula:
- ##STR32## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a pyrimidine, pyrazine or pyridazine ring;
- X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR33## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen, k is 0 to 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4;
- y is oxygen, sulphur or NH;
- E is oxygen or sulphur;
- and R.sub.1 is hydrogen, lower alkyl benzoyl or di-lower alkylaminolower alkyl or a pharmaceutically acceptable addition salt thereof.
Dependencies are inferred from the claim text.