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Details for Patent: 4,018,931

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Details for Patent: 4,018,931

Title: Pharmacologically active thiourea and urea compounds
Abstract:The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
Inventor(s): Durant; Graham John (Welwyn Garden City, EN), Emmett; John Colin (Codicote, EN), Ganellin; Charon Robin (Welwyn Garden City, EN)
Assignee: Smith Kline & French Laboratories Limited (Welwyn Garden City, EN)
Filing Date:Dec 04, 1975
Application Number:05/637,494
Claims:1. 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 an imidazole or pyrazole 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 alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof with the proviso that X.sub.1 is ##STR30## only when Y and E are sulphur and R.sub.1 is methyl and with the proviso that when X.sub.1 is other than hydrogen or lower alkyl and X.sub.2 is other than hydrogen, X.sub.1 and X.sub.2 are attached at carbon atoms.

2. A pharmaceutical composition of claim 1 in which the heterocyclic compound is N-methyl-N'-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]thiourea.

3. A pharmaceutical composition of claim 1 in which the pharmaceutical composition is in the form of a tablet or capsule.

4. A pharmaceutical composition of claim 1 in which the heterocyclic compound is present in an amount of from about 50 mg. to about 250 mg.

5. A method of inhibiting H-2 histamine receptors 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: ##STR31## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being an imidazole or pyrazole ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR32## 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 alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof with the proviso that X.sub.1 is ##STR33## only when Y and E are sulphur and R.sub.1 is methyl and with the proviso that when X.sub.1 is other than hydrogen or lower alkyl and X.sub.2 is other than hydrogen, X.sub.1 and X.sub.2 are attached at carbon atoms.

6. A method of claim 5 in which the heterocyclic compound is N-methyl-N'-[2-((5-methyl-4-imidazolyl)methylthio)ethyl]thiourea.

7. A method of claim 5 in which the heterocyclic compound is administered orally.

8. A method of claim 5 in which the heterocyclic compound is administered in a daily dosage regimen of from about 150 mg. to about 1000 mg.

9. A method of inhibiting gastric acid secretion which comprises administering 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: ##STR34## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being an imidazole or pyrazole ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR35## 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 alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof with the proviso that X.sub.1 is ##STR36## only when Y and E are sulphur and R.sub.1 is methyl and with the proviso that when X.sub.1 is other than hydrogen or lower alkyl and X.sub.2 is other than hydrogen, X.sub.1 and X.sub.2 are attached at carbon atoms.

10. A method of claim 9 in which the heterocyclic compound is N-methyl-N'-[2-((5-methyl-4-imidazolyl)methylthio)-ethyl]thiourea.
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