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US 4,285,952 AGranted
Pyridyl, thiazolyl and isothiazolyl alkyl bisamidines
AssigneeSmith Kline & French Laboratories Limited
InventorsGraham J. Durant, Peter D. Miles
Life of this patent
Estimating the term…
Abstract
Bisamidines carrying one unsaturated nitrogen heterocycle-containing substituent, representative of which is 1-[N'-(2-(5-methyl-4-imidazolyl)methylthio)ethyl)guanidino]-8-[N'-methylgu anidino]octane, are histamine H.sub.2 -antagonists.
Claims11
A compound of the structure ##STR5## in which Het is a 5- or 6-membered fully unsaturated heterocycle containing at least one nitrogen atom, said heterocycle being pyridine optionally substituted by lower alkyl, trifluoromethyl, hydroxymethyl, halogen, hydroxy, lower alkoxy or amino;
- or thiazole or isothiazole which are attached at a ring carbon and which are optionally substituted by lower alkyl, trifluoromethyl, hydroxymethyl, halogen or lower alkoxy;
- Z is sulphur or methylene;
- m is 0, 1 or 2, n is 2 or 3, and m+n is 3 or 4;
- R is hydrogen or lower alkyl;
- each of X.sup.1 and X.sup.2 is sulphur, a nitromethylene group CHNO.sub.2, or an imino group NY, where Y is hydrogen, hydroxy, lower alkyl, cyano or carbamoyl CONH.sub.2 ;
- and
- q is from 2 to 12;
- in the form of the free base or its pharmaceutically-acceptable acid addition salts.
5 more elements
Dependencies are inferred from the claim text.