Back to results
US 4,788,195 AGranted
4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
AssigneeAmerican Cyanamid Company
InventorsLawrence W. Torley, Bernard D. Johnson, John P. Dusza
Life of this patent
Estimating the term…
Abstract
This disclosure describes novel 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines having anti-asthmatic activity.
Claims16
A compound selected from the group consisting of those of the formula:
- ##STR7## wherein R.sub.1 is hydrogen, alkyl(C.sub.1 -C.sub.3), --COCO.sub.2 C.sub.2 H.sub.5 or N,N-dimethylaminoethyl;
- R.sub.2 is mono- or poly-substituted phenyl wherein the substituents are alkyl(C.sub.1 -C.sub.6), alkoxy(C.sub.1 -C.sub.3), chloro, bromo, iodo, trifluoromethyl, hydroxy, phenyl, amino, monoalkyl(C.sub.1 -C.sub.3)amino, dialkyl(C.sub.1 -C.sub.3)amino, alkyl(C.sub.1 -C.sub.3)keto, propenyloxy, carboxyl, oxyacetic acid, oxyacetic acid ethyl ester, sulfanilamido, N,N-dialkyl(C.sub.1 -C.sub.3)sulfanilamido, N-methylpiperazinyl, piperidinyl, 1H-imidazol-1-yl, 1H-triazol-1-yl, 1H-benzimidazol-2-yl, 1-naphthyl, cyclopentyl, 3,4-dimethylbenzyl or moieties of the formulae:
- ##STR8## wherein R is alkyl(C.sub.1 -C.sub.3), X is oxygen (--O--) or sulfur (--S--), m is 1-3, n is 2 or 3, R.sub.6 is hydrogen, alkyl(C.sub.1 -C.sub.3), alkoxy (C.sub.1 -C.sub.3), chloro, bromo, iodo or trifluoromethyl, R.sub.7 is 1H-imidazol-1-yl or morpholino and R.sub.8 is alkyl(C.sub.1 -C.sub.3), phenyl or monosubstituted phenyl wherein the substituents are alkyl (C.sub.1 -C.sub.3), halogen or trifluoromethyl;
- R.sub.3 is 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 2-methyl-3-pyridinyl, 4-methyl-3-pyridinyl, 2-furanyl, 5-methyl-2-furanyl, 2,5-dimethyl-3-furanyl, 2-thienyl, 3-thienyl, 5-methyl-2-thienyl, 2-pheno-thiazinyl, 4-pyrazinyl, 2-benzofuranyl, 2-(pyridine-N-oxide), 3-(pyridine-N-oxide), 4-(pyridine-N-oxide), 1H-indol-2-yl, 1H-indol-3-yl, 1-methyl-1H-pyrrol-2-yl, 4-quinolinyl, 4-pyri-dinyl methyl iodide, dimethylaminophenyl or N-acetyl-N-methylaminophenyl;
- R.sub.4 is hydrogen or alkyl(C.sub.1 -C.sub.3);
- and R.sub.5 is hydrogen or alkyl(C.sub.1 -C.sub.3);
- and the pharmacologically acceptable acid-addition salts thereof.
4 more elements
Dependencies are inferred from the claim text.