4-Pyrimidones compositions, and methods of use

Claim 1

A compound of the formula: ##STR11## wherein Het' is a 2- or 4-imidazolyl ring optionally monosubstituted by lowr alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl ring optionally monosubstituted by lower alkyl, lower alkoxy, halogen, amino or hydroxy, a 2-pyridyl ring which is disubstituted by lower alkoxy groups, or which has a phenyl, carbocyclic or cyclic either ring containing two oxygen atoms fused to it, a 2-thiazolyl ring, a 3-isothiazolyl ring optionally monosubstituted by chlorine or bromine, a 3-(1,2,5)-thiadiazolyl ring optionally monosubstituted by chlorine or bromine, a 2-(5-amino-1,3,4-thiadiazolyl)ring; Z is sulphur or a methylene group; X is oxygen or sulphur; W is methylene, oxygen or sulphur; m and n are such that their sum is from 1 to 4 when W is oxygen or sulphur, or from 0 to 4 when W is methylene; A is a 1- or 2-naphthyl ring or a phenyl ring substituted with one lower alkyl group; and Y 3 is hydrogen; or a pharmaceutically acceptable acid addition salt thereof.

Claim 16

A method of simultaneously blocking histamine H 1 -receptors and histamine H 2 -receptors which comprises administering to an animal in need thereof an effective amount of a compound of the formula: ##STR12## wherein Het' is a 2- or 4-imidazolyl ring optionally monosubstituted by lower alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl ring optionally monosubstituted by lower alkyl, lower alkoxy, halogen, amino or hydroxy, a 2-pyridyl ring which is disubstituted by lower alkoxy groups, or which has a phenyl, carbocyclic or cyclic ether ring containing two oxygen atoms fused to it, a 2-thiazolyl ring, a 3-isothiazolyl ring optionally monosubstituted by chlorine or bromine, a 3-(1,2,5-)-thiadiazolyl ring optionally monosubstituted by chlorine or bromine, or a 2-(5-amino-1,3,4-thiadiazolyl)ring; Z is sulphur or a methylene group; X is oxygen or sulphur; W is methylene, oxygen or sulphur; m and n are such that their sum is from 1 to 4 when W is oxygen or sulphur, or from 0 to 4 when W is methylene; A is a 1- or 2-naphthyl ring, a phenyl ring substituted with one lower alkyl group and when --(CH 2 ) m --W(CH 2 ) n --is an alkylene group other than a methylene group, A may also be phenyl; and Y is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof.

Claim 17

A method of simultaneously blocking histamine H 1 -receptors and histamine H 2 -receptors which comprises administering to an animal in need thereof an effective amount of a compound of the formula: ##STR12## wherein Het' is a 2- or 4-imidazolyl ring optionally monosubstituted by lower alkyl, halogen, trifluoromethyl or hydroxymethyl, a 2-pyridyl ring optionally monosubstituted by lower alkyl, lower alkoxy, halogen, amino or hydroxy, a 2-pyridyl ring which is disubstituted by lower alkoxy groups, or which has a phenyl, carbocyclic or cyclic ether ring containing two oxygen atoms fused to it, a 2-thiazolyl ring, a 3-isothiazolyl ring optionally monosubstituted by chlorine or bromine, a 3-(1,2,5-)-thiadiazolyl ring optionally monosubstituted by chlorine or bromine, or a 2-(5-amino-1,3,4-thiadiazolyl)ring; Z is sulphur or a methylene group; X is oxygen or sulphur; W is methylene, oxygen or sulphur; m and n are such that their sum is from 1 to 4 when W is oxygen or sulphur, or from 0 to 4 when W is methylene; A is a 1- or 2-naphthyl ring, a phenyl ring substituted with one lower alkyl group and when --(CH 2 ) m --W(CH 2 ) n --is an alkylene group other than a methylene group, A may also be phenyl; and Y is hydrogen or lower alkyl; or a pharmaceutically acceptable acid addition salt thereof.