C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) C07D 401/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01)
Patent
CA 2093203
There are described N-phenyl-2-pyrimidine-amine derivatives of formula I Image wherein R1 is pyrazinyl, 1-methyl-1H pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each cast is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstitut ed or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2 and R3 are each independently of the other hydrogen or lower alkyl, one or two of the radicals R4, R5, R6, R7 and R8 are each nitro, fluoro- substituted lower alkoxy or a radical of formula II -N(R9)-C(=X)-(Y)n-R10 (II), wherein R9 is hydrogen or lower alkyl, - X is oxo, thio, imino, N-lower alkyl-imino, hydroximino or O-lower alkyl- hydrox- imino, Y is oxygen or the group NH, n is a or 1 and R10 is an aliphatic radical having at least 5 carbon atoms, or an aromatic, aromatic- aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or heterocyclic- aliphatic radical, and the remaining radicals R4, R5, R6, R7 and R8 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, trifluoro- methyl, free, etherified or esterifed hydroxy, free, alkylated or acylated amino or free or esterified carboxy. These compounds can be used, for example, in the therapy of tumoral diseases.
Ag Ciba-Geigy
Fetherstonhaugh & Co.
Novartis Ag
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