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Details for Patent: 4,018,928

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Details for Patent: 4,018,928

Title: Pyridyl substituted aminoalkyl-thioureas and ureas
Abstract:The compounds are pyridyl substituted aminoalkylthioureas and ureas which are inhibitors of H-2 histamine receptors. A compound of this invention is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.
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:Oct 29, 1975
Application Number:05/626,682
Claims:1. A pharmaceutical composition to inhibit H-2 histamine receptors, said composition being suitable for oral or parenteral administration, comprising a pharmaceutical carrier and in an effective amount to inhibit said receptors a pyridyl compound of the formula: ##STR8## 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 ##STR9## X.sub.2 is hydrogen or when X.sub.1 is lower alkyl, lower alkyl or halogen; k is 1 or 2 and m is 2 or 3, provided that the sum of k and m is 3 or 4; Y is NH; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, or dimethylaminoethyl 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-pyridyl-amino)-propyl]thiourea.

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

4. A pharmaceutical composition of claim 3 wherein X.sub.1 is hydrogen, methyl, bromo, hydroxyl or amino and X.sub.2 is hydrogen; E is sulphur and R.sub.1 is methyl.

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

6. 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.

7. 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 pyridyl compound of the formula: ##STR10## 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 ##STR11## 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 NH; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.

8. A method of claim 7 in which the pyridyl compound is N-methyl-N'-[3-(2-pyridylamino)propyl]thiourea.

9. A method of claim 7 in which the pyridyl compound is N-methyl-N'-[2-(2-pyridylmethylamino)ethyl]thiourea.

10. A method of claim 7 in which the pyridyl compound is administered in a daily dosage of from about 150 mg. to about 750 mg.

11. 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: ##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 NH; E is oxygen or sulphur; R.sub.1 is hydrogen, lower alkyl, or dimethylaminoethyl or a pharmaceutically acceptable addition salt thereof.
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