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Details for Patent: 4,307,101
| Title: | Inhibitors of H-2 histamine receptors |
| Abstract: | The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity. |
| Inventor(s): | Durant; Graham J. (Welwyn Garden City, GB2), Emmett; John C. (Codicote, GB2), Ganellin; Charon R. (Welwyn Garden City, GB2) |
| Assignee: | Smith Kline & French Laboratories Limited (Welwyn Garden City, GB2) |
| Filing Date: | Mar 17, 1980 |
| Application Number: | 06/130,760 |
| Claims: | 1. 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: ##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 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine 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. 2. 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: ##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 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring; X.sub.1 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 alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof. 3. A pharmaceutical composition of claim 2 in which the heterocyclic compound is N-methyl-N'-[2-(3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridyl)methylthio)ethy l]thiourea. 4. A pharmaceutical composition of claim 2 in which the pharmaceutical composition is in the form of a tablet or capsule. 5. A pharmaceutical composition of claim 2 in which the heterocyclic compound is present in an amount of from about 50 mg. to about 250 mg. 6. A method of claim 1 in which the heterocyclic compound is N-methyl-N'-[2-(3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridyl)methylthioethyl ]thiourea. 7. A method of claim 1 in which the heterocyclic compound is administered orally. 8. A method of claim 1 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 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 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine 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 alkylamino-lower alkyl or a pharmaceutically acceptable addition salt thereof. |
