Pharmacologically active guanidine compounds
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham J. Durant, John C. Emmett, Charon R. Ganellin
Life of this patent
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Abstract
The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histarine activity.
Claims9
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:
- ##STR16## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a 3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridine) ring;
- X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, 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, 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.
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:
- ##STR18## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a 3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridine) ring;
- X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR19## 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.
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:
- ##STR20## wherein A is such that there is formed together with the carbon atom shown an unsaturated heterocyclic nucleus, said unsaturated heterocyclic nucleus being a 3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridine ring;
- X.sub.1 is hydrogen, lower alkyl, hydroxyl, trifluoromethyl, benzyl, halogen, amino or ##STR21## 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.
Dependencies are inferred from the claim text.