FIELD: pharmacology.
SUBSTANCE: described are C-6 modified indazolyl pyrrolotriaxolines of formula I and their pharmaceutically acceptable salts, where R is selected from group consisting of phenylm phenyl substituted with halogen atom, non-substituted oxazolyl, thienyl, thiazolyl, pyridyl, pyrazinyl; R1 is selected from group consisting of methyl, ethyl and isopropyl; R2 is selected from group consisting of benzyl, imidazolylethyl, (methylimidazolyl)-ethyl, pyperidinylethyl, pyridinylpropyl and other, given in item 1 of invention formula, X is selected from group consisting of bond, O, NR3; and N(R3)2; R3 is independently selected from group consisting of hydrogen, methoxyethyl, diethylaminoethyl, pyrrolidinylethyl. Also described are pharmaceutical composition for treatment of proliferative disease, methods of disease treatment. Compounds of formula I inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4, which makes them useful as anti-cancer agents.
EFFECT: compounds are anti-cancer agents and are useful for treatment of other diseases connected with pathways of signal transduction acting through growth factor receptors.
23 cl, 4 tbl, 175 ex
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Authors
Dates
2009-05-27—Published
2003-12-12—Filed