Further use of pyrimidine derivatives
AssigneeCiba-Geigy Corporation
InventorsJurg Zimmermann, Giorgio Caravatti
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Abstract
The invention relates to the use of known N-phenyl-2-pyrimidine derivatives for inhibiting proteinkinase C in warm-blooded animals as antitumor agents. ##STR1## The substituents in formula I are as defined in claim 1.
Claims11
A method of treatment of warm-blooded animals suffering from a protein kinase C dependent tumoral disease, which comprises treating warm-blooded animals in need of such treatment with an effective tumor-inhibiting amount of a compound of formula I ##STR7## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.3 is 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-methyl-3-pyridyl, 4-methyl-3-pyridyl, 2-furyl, 5-methyl-2-furyl, 2,5-dimethyl-3-furyl, 2-thienyl, 3-thienyl, 5-methyl-2-thienyl, 2-phenothiazinyl, 4-pyrazinyl, 2-benzofuryl, N-oxido-2-pyridyl, N-oxido-3-pyridyl, N-oxido-4-pyridyl, 1H-indol-2-yl, 1H-indol-3-yl, 1-methyl-1H-pyrrol-2-yl, 4-quinolinyl, 1-methyl-pyridinium-4-yliodide, dimethylaminophenyl or N-acetyl-N-methylaminophenyl, R.sub.4 is hydrogen, C.sub.1 -C.sub.3 alkyl, --CO--CO--O--C.sub.2 H.sub.5 or N,N-dimethylaminoethyl, at least one of R.sub.5, R.sub.6, R.sub.7 and R.sub.8 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkoxy, chloro, bromo, iodo, trifluoromethyl, hydroxy, phenyl, amino, mono-(C.sub.1 -C.sub.3 -alkyl)amino, di(C.sub.1 -C.sub.3 alkyl)amino, C.sub.2 -C.sub.4 alkanoyl, propenyloxy, carboxy, carboxymethoxy, ethoxycarbonylmethoxy, sulfanilamido, N,N-di(C.sub.1 -C.sub.3 alkyl)sulfanilamido, N-methylpiperazinyl, piperidinyl, 1H-imidazol-1-yl, 1H-triazol-1-yl, 1H-benzimidazol-2-yl, 1-naphthyl, cyclopentyl, 3,4-dimethylbenzyl or a radical of one of the formulae:
- --CO.sub.2 R, --NH--C(.dbd.O)--R, --N(R)--C(.dbd.O)--R, --O--(CH.sub.2).sub.n --N(R)--R, --C(.dbd.O)--NH--(CH.sub.2).sub.n --N(R)--R, --CH(CH.sub.3)--NH--CHO, --C(CH.sub.3).dbd.N--OH, --C(CH.sub.3).dbd.N--O--CH.sub.3, --C(CH.sub.3)--NH.sub.2, --NH--CH.sub.2 --C(.dbd.O)--N(R)--R, ##STR8## --(CH.sub.2).sub.m --R.sub.10, --X--(CH.sub.2).sub.m --R.sub.10 or ##STR9## wherein R is C.sub.1 -C.sub.3 alkyl, X is oxygen or sulfur, m is 1, 2 or 3, n is 2 or 3, R.sub.9 is hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, chloro, bromo, iodo or trifluoromethyl, R.sub.10 is 1H-imidazol-1-yl or morpholinyl, and R.sub.11 is C.sub.1 -C.sub.3 alkyl or unsubstituted phenyl or phenyl which is monosubstituted by C.sub.1 -C.sub.3 alkyl, halogen or trifluoromethyl, and the other substituents R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are hydrogen, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.