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US 4,728,648 AGranted
Histamine antagonist triadiazole derivatives, compositions, and method of use therefor
AssigneeSmith Kline & French Laboratories Limited
InventorsAndrew D. Gribble, Robert J. Ife
Life of this patent
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Abstract
New 3,4-diamino-1,2,5-thiadiazole oxide derivatives which are histamine H.sub.1 -antagonists. A specific compound of this invention is 3-[3-[N-(4-fluorobenzyl)-N-pyrid-2-yl-amino]propylamino]-4-[pyrimidin-4-yl -methylamino]-1,2,5-thiadiazole-1-oxide.
Claims22
A compound of formula (1):
- ##STR7## or a pharmaceutically acceptable salt thereof, where R.sup.1 and R.sup.2 are the same or different and are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;
- R.sup.3 is optionally substituted phenyl or optionally substituted pyridyl, where the optional substituents are one or more C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or hydroxy groups or halogen atoms;
- or furanyl or thienyl optionally substituted by a C.sub.1-6 alkyl group;
- a is from 1 to 6;
- b is from 2 to 4;
- R.sup.4 is CH.sub.2 R.sup.5 where R.sup.5 is phenyl substituted by sulphonamido or a carboxyl group or an ester thereof, pyridyl substituted with a carboxyl group or an ester thereof and optionally further substituted with a C.sub.1-6 alkyl group, N-oxo-pyridyl optionally substituted with a C.sub.1-6 alkyl group, or an imidazolyl, pyridazinyl, pyrimidinyl, pyrazinyl or benzimidazolyl group;
- and
- r is 1 or 2.
5 more elements
Dependencies are inferred from the claim text.