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US 4,070,472 AGranted
Guanidino, thioureido, isothioureido and nitrovinylamino derivatives of pyridine
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham John Durant, Charon Robin 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.
Claims14
A compound of the formula:
- ##STR18## 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 pyridine which is attached at a ring carbon and which is optionally substituted by lower alkyl, hydroxyl, halogen or amino;
- Z is sulphur or a methylene group;
- m is 0, 1 or 2;
- n is 2or 3;
- and the sum of m and n is 3 or 4;
- X.sub.1 and X.sub.2, which are the same, are sulphur, CHNO.sub.2 or NY wherein Y is hydrogen, or lower alkyl;
- W is NH or sulphur;
- and q is an integer from 2 to 8;
- or a pharmaceutically acceptable acid addition salt thereof, provided that W is sulphur only when X.sub.1 and X.sub.2 are NH.
8 more elements
Dependencies are inferred from the claim text.