|Title:|| Pharmacologically active guanidine compounds|
|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:||Mar 21, 1980|
|Claims:||1. A 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 or 3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridine) 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 a pharmaceutically acceptable addition salt thereof. |
2. A compound of claim 1 wherein Y is oxygen or sulphur.
3. A compound of claim 1 wherein Y is NH.
4. A compound of claim 1 wherein said unsaturated heterocyclic nucleus is benzimidazole or 3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridine) and R.sub.2 is hydrogen or nitro.
5. A compound of claim 4 wherein k is 1 and m is 2.
6. A compound of claim 1, said compound being N-[2-(2-benzimidazolylmethylthio)ethyl]-N'-cyano-N"-methylguanidine.
7. A compound of claim 1, said compound being N-cyano-N'-methyl-N"-[2-(3-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridyl)methyl thio)ethyl]guanidine.