Back to results
US 4,301,165 AGranted
Pharmacologically active compounds
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham J. Durant, Charon R. Ganellin
Life of this patent
Estimating the term…
Abstract
The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino), N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.
Claims13
A compound of the formula:
- ##STR23## wherein R.sub.1 and R.sub.2, which may be the same or different, each represent a grouping of the structure:
- Het--(CH.sub.2).sub.m Z--(CH.sub.2).sub.n --
- wherein Het is a nitrogen containing membered heterocyclic ring selected from imidazole, pyrazole or triazole which is optionally substituted by lower alkyl, hydroxyl, halogen or amino, except that R.sub.1 and R.sub.2 are not both imidazolyl containing groups;
- Z is sulphur or a methylene group;
- m is 0, 1 or 2;
- n is 2 or 3 and the sum of m and n is 3, 4 or when Y is other than hydrogen, methyl, or hydroxyl, 2;
- X.sub.1 and X.sub.2, which may be the same or different, are each sulphur, CHNO.sub.2 or NY wherein Y is hydrogen, hydroxy, lower alkyl, cyano, CONH.sub.2 or SO.sub.2 R.sub.3 ;
- R.sub.3 is lower alkyl, phenyl, tolyl, trifluoromethyl or amino;
- W is NH, and when X.sub.1 and X.sub.2 are NH, W may also be sulphur;
- and q is an integer from 2 to 8;
- or a pharmaceutically acceptable acid addition salt thereof.
8 more elements
Dependencies are inferred from the claim text.