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Details for Patent: 4,221,802

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Details for Patent: 4,221,802

Title: Pharmacologically active guanidine compounds for inhibiting H-2 histamine receptors
Abstract:The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines 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:Feb 07, 1979
Application Number:06/010,105
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: ##STR15## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a benzimidazole ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR16## 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 NR.sub.2 ; R.sub.1 is hydrogen, lower alkyl or di-lower alkylamino-lower alkyl; and R.sub.2 is hydrogen, nitro or cyano, or pharmaceutically acceptable addition salt thereof.

2. A method of claim 1 in which the heterocyclic compound is N-[2-(2-benzimidazolylmethylthio)ethyl]-N'-cyano-N"-methylguanidine.

3. A method of claim 1 in which the heterocyclic compound is administered orally.

4. 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.

5. 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: ##STR17## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a benzimidazole ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR18## 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 NR.sub.2 ; R.sub.1 is hydrogen, lower alkyl or di-lower alkylamino-lower alkyl; and R.sub.2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable addition salt thereof.

6. 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: ##STR19## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a benzimidazole ring; X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR20## 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 NR.sub.2 ; R.sub.1 is hydrogen, lower alkyl or di-lower alkylamino-lower alkyl; and R.sub.2 is hydrogen, nitro or cyano, or a pharmaceutically acceptable addition salt thereof.

7. A pharmaceutical composition of claim 6 in which the heterocyclic compound is N-[2-(2-benzimidazolylmethylthio)ethyl]-N'-cyano-N"-methylguanidine.

8. A pharmaceutical composition of claim 6 in which the pharmaceutical composition is in the form of a tablet or capsule.

9. A pharmaceutical composition of claim 6 in which the heterocyclic compound is present in an amount of from about 50 mg. to about 250 mg.
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