Pyrimidine derivatives and processes for the preparation thereof
AssigneeCiba-Geigy Corporation
InventorJurg Zimmermann
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Abstract
There are described N-phenyl-2-pyrimidine-amine derivatives of formula I ##STR1## wherein R.sub.1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R.sup.2, R.sup.3, R.sup.9, X, Y, n and R.sup.10 are defined in claim 1 These compounds can be used, for example, in the therapy of tumoral diseases.
Claims23
An N-phenyl-2-pyrimidine-amine compound of formula I ##STR9## wherein R.sub.1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen,
- R.sub.2 and R.sub.3 are each independently of the other hydrogen or lower alkyl, one or two of the radicals R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each nitro, fluoro-substituted lower alkoxy or a radical of formula II
- --N(R.sub.9)--C(.dbd.X)--(Y).sub.n --R.sub.10 (II)
- wherein
- R.sub.9 is hydrogen or lower alkyl,
- X is oxo, thio, imino, N-lower alkyl-imino, hydroximino or O-lower alkyl-hydroximino,
- Y is oxygen or the group NH,
- n is 0 or 1 and
- R.sub.10 is an aliphatic radical having at least 5 carbon atoms, or an aromatic, aromatic-aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or hetero-cyclicaliphatic radical,
- and the remaining radicals R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are each independently of the others hydrogen, lower alkyl that is unsubstituted or substituted by free or alkylated amino, piperazinyl, piperidinyl, pyrrolidinyl or by morpholinyl, or lower alkanoyl, trifluoromethyl, free, etherified or esterifed hydroxy, free, alkylated or acylated amino or free or esterified carboxy,
- or a salt of such a compound having at least one salt-forming group.
Dependencies are inferred from the claim text.