PYRROLTRIAZINE KINASE INHIBITORS Russian patent published in 2008 - IPC C07D487/04 A61K31/53 

FIELD: chemistry, pharmaceuticals.

SUBSTANCE: description is given of new derivatives of pyrroltriazine with general formula I , where X represents O, CO, CO₂, NHCO₂, CONH; Y represents O or CO₂, or X and/or Y are absent; Z represents O or N, or is absent; R¹ - H, CH₃, halogen; R² - H, CH₃, C₂H₅, hydroxymethyl, methylpiperazinyl, pirrolidinylethyl, triazolylmethyl, triazolylethyl, phenylmethyl or morpholinylpropyl, R³ - H, CH₃, C₂H₅ or phenyl; R⁴ - phenyl, possibly substituted with indolyl, possibly substituted, 2,3-dihydro-1,4-benzodioxynyl, pyridinyl, possibly substituted, benzotriazolyl, benzothiazolyl, phtalazinyl, possibly substituted, pyrazolyl, possibly substituted, phenoxyphenyl, indazolyl, possibly substituted, pyrazolopyrimidine, possibly substituted, or pyrazolopyridine. R⁵ - hydrogen of methyl, or is absent, when Z represents O or is absent, R⁶ - H or N(CH₃)₂. Both R⁴ and R⁵ do not represent H, when Z represents N, and R² does not represent H, if X represents NHCO₂, or their pharmaceutical salts. The compounds of formula I inhibit thyrosine kinase activity of growth factor receptors, such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, and are thus suitable for use as anticancer agents. Compounds with formula I are also important for curing other diseases, associated with signal transduction channels, working due to the growth factor receptors.

EFFECT: obtaining new derivatives of pyrroltriazine, suitable for use as anticancer agents.

3 cl, 143 ex