C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/505 (2006.01) A61K 31/506 (2006.01) A61P 35/00 (2006.01) C07D 239/42 (2006.01)
Patent
CA 2149147
Described are N-phenyl-2-pyrimidineamine derivatives of formula (I) wherein R1 is a substituted cyclic radical, the cyclic radical being bonded to a ring carbon atom in each case and being selected from phenyl, pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, -C(=O)-OR3, -C(=O)-R4, -SO2-N(R5)-R6, -N(R7)- R8, -OR9 and fluorine-substituted lower alkyl, wherein R3, R4, R5, R6, R7, R8 and R9 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino; and R2 is selected from halogen, cyano, carbamoyl, -C(=O)-OR10, -C(=O)-R11, -SO2-N(R12)- R13, -N(R14)-R15, -OR16 and fluorine-substituted lower alkyl, wherein R10, R11, R12, R13, R14, R15 and R16 are each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino. Those compounds can be used, for example, in the treatment of tumour diseases.
L'invention se rapporte à des dérivés de N-phényl-2-pyrimidineamine de formule (I) dans laquelle R¿1? est un radical cyclique substitué, lequel est fixé à un atome de carbone cyclique dans chaque cas et choisi parmi phényle, pyridyle, pyrazinyle, thiazolyle, pyrimidinyle, pyridazinyle et imidazolyle, les substituants dudit radical cyclique étant choisis parmi un ou plusieurs des groupes halogène, cyano, carbamyle, -C(=O)-OR¿3?, -C(=O)-R¿4?, -SO¿2?-N(R¿5?)-R¿6?, -N(R¿7?)-R¿8?, -OR¿9?, et alcoyle inférieur substitué par du fluor, dans lesquels R¿3?, R¿4?, R¿5?, R¿6?, R¿7?, R¿8? et R¿9? sont chacun, indépendamment des autres, hydrogène ou alcoyle inférieur non substitué ou substitué par mono- ou di-alcoylamine inférieure; et R¿2? est choisi parmi des groupes halogène, cyano, carbamyle, -C(=O)-OR¿10?, -C(=O)-R¿11?, -SO¿2?-N(R¿12?)-R¿13?, -N(R¿14?)-R¿15?, -OR¿16? et parmi alcoyle inférieur substitué par du fluor, dans lesquels R¿10?, R¿11?, R¿12?, R¿13?, R¿14?, R¿15? et R¿16? sont chacun, indépendamment des autres, hydrogène ou alcoyle inférieur non substitué ou substitué par mono- ou di-alcoylamine inférieure. On peut utiliser ces composés, par exemple, dans le traitement des affections tumorales.
Ag Ciba-Geigy
Fetherstonhaugh & Co.
Novartis Ag
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