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Details for Patent: 4,027,026

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Details for Patent: 4,027,026

Title: Pharmaceutical compositions and methods of inhibiting H-2 histamine receptors with pyridyl substituted thioalkyl- and oxyalkyl-thioureas and ureas
Abstract:Pharmaceutical compositions and methods of inhibiting H-2 histamine receptors with pyridyl substituted thioalkyl- and oxyalkyl-thioureas and ureas.
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:Jun 13, 1975
Application Number:05/586,670
Claims:1. 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 pyridyl compound of the formula: ##STR12## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR13## 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 or sulphur; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylamino- lower alkyl, or a pharmaceutically acceptable addition salt thereof.

2. A pharmaceutical composition of claim 1 in which the pyridyl compound is N-methyl-N'-[3-(2-pyridylthio)-propyl]-thiourea.

3. A pharmaceutical composition of claim 1 wherein k is 1 and m is 2.

4. A pharmaceutical composition of claim 1 in which X.sub.1 is hydrogen, methyl, bromo, hydroxyl or amino and X.sub.2 is hydrogen; Y and E are sulphur and R.sub.1 is methyl.

5. A pharmaceutical composition of claim 1 in which the pyridyl compound is N-methyl-N'-[2-((3-hydroxy-2-pyridyl)methylthio)ethyl]thiourea.

6. A pharmaceutical composition of claim 1 in which the pyridyl compound is N-methyl-N'-[2-((3-bromo-2-pyridyl)methylthio)ethyl]thiourea.

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

8. 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 pyridyl compound of the formula: ##STR14## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR15## 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 or sulphur; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylamino-lower alkyl, or a pharmaceutically acceptable addition salt thereof.

9. A method of claim 8 in which the pyridyl compound is N-methyl-N'-[3-(2-pyridylthio)propyl]thiourea.

10. A method of claim 8 in which the pyridyl compound is N-methyl-N'-[2-((3-hydroxy-2-pyridyl)methylthio)-ethyl]thiourea.

11. A method of claim 8 in which the pyridyl compound is N-methyl-N'-[2-((3-bromo-2-pyridyl)methylthio)ethyl]thiourea.

12. A method of claim 8 in which the pyridyl compound is administered in a daily dosage of from about 150 mg. to about 750 mg.

13. 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 pyridyl compound of the formula: ##STR16## wherein A is such that there is formed together with the carbon atom shown a pyridine ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, halogen, amino or ##STR17## 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 or sulphur; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, benzoyl or di-lower alkylamino-lower alkyl, or a pharmaceutically acceptable addition salt thereof.
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