2-AMINO-SUBSTITUTED 6-METHOXY-4-TRIFLUOROMETHYL-9H-PYRIMIDO[4,5B]INDOLES, METHOD FOR THEIR PRODUCTION, APPLICATION AND PREDIMINARIES Russian patent published in 2017 - IPC C07D487/04 A61P35/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to new 2-amino-substituted 6-methoxy-4-trifluoromethyl-9H-pyrimido[4,5-b]indoles of general formula I and their pharmaceutically acceptable salts, as well as to the new compounds of formula (II), preceding the compounds of formula (I). The compounds of formula I possess anti-tumor activity and are useful in the therapy of myelogenous leukemia and colon cancer. In the formula (I), R=C₁-C₆-alkyl; C₁-C₃-alkyl-O-CH₂CH₂-; R¹C₆H₄CH₂-, where R¹=H_, Me, MeO; , where R²=H or Me. In the formula (II), X means S (IIa), SO₂ (IIb). The method for preparation of formula (I) compounds comprises intramolecular cyclization of N-(5-iodo-2-methylthio-6-trifluoromethylpyrimidin-4-yl)-N-methyl-N-(4-methoxyphenyl) amine to form 9-methyl-2-methylthio-6-methoxy-4-trifluoromethyl-9H-pyrimido[4,5-b]indole, at heating in the presence of a base and a catalyst, subsequent oxidation and nucleophilic substitution of the 2-methylsulfonyl group in the resulting product with the corresponding primary amine.

EFFECT: increased activity of the composition.

11 cl, 1 tbl, 8 ex