1,2,4-triazinones-5

Details 1,2,4-triazinones-5 1,2,4-triazinones-5

C - Chemistry, Metallurgy

07

D

260/248.6

C07D 253/06 (2006.01) C07D 213/55 (2006.01) C07D 213/61 (2006.01) C07D 213/65 (2006.01) C07D 213/73 (2006.01) C07D 253/075 (2006.01) C07D 403/00 (2006.01)

Patent

CA 1124717

ABSTRACT OF THE DISCLOSURE Pharmacologically active compounds are disclosed of the general formula: Image FORMULA 3 wherein Het' is a 2- or 4-imidazolyl ring optionally substituted by lower alkyl (preferably methyl), halogen (preferably chlorine or bromine), trifluoromethyl or hydroxymethyl, a 2-pyridyl ring optionally substituted by one or two groups (which may be the same or different) selected from lower alkyl (preferably methyl), lower alkoxy (preferably methoxy), halogen (preferably chlorine or bromine), amino and hydroxy, a 2-pyridyl ring with a phenyl, carbocyclic or cyclic ether ring containing 2 oxygen atoms fused to it, a 2-thiazolyl ring, a 3- isothiazolyl ring optionally substituted by chlorine or bromine, a 3-(1,2,5) thiadiazolyl ring optionally substituted by chlorine or bromine, or a 2-(5-amino- 1,3,4-thiadiazolyl) ring; Z' is sulphur or a methylene group; x is 1 to 5; Y is a 1- or 2-naphthyl ring, a 2,3-dihydro-1,4-benzodioxinyl or a 1,3-benzodioxolyl ring, a phenyl ring substituted with one or more alkyl, lower alkoxy, halogen, arylalkoxy, hydroxy, alkoxyalkoxy, trifluoromethyl, di(lower alkyl) amino, phenoxy, halo- phenoxy, alkoxyphenoxy, phenyl, halophenyl or alkoxy- phenyl groups, a 5 or 6 membered heterocycle such as a pyridine, furan, thiophen, thinzole, oxazole, isothiazole, imidazole, pyrimidine, pyrazine or pyridazine ring, which ring is optionally substituted by lower alkyl, lower alkoxy or may have a benzene ring fused to it, or when x is other than 1 Y may also be phenyl; or a pharmaceutically acceptable salt thereof. These compounds have been found to block histamine H2- and H1- receptors. The compounds also show anti-inflammatory activity.

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