DICHLOROACETATES OF SUBSTITUTED N4-[2-(DIMETHYLPHOSPHORYL)PHENYL]-N2-(2-METHOXY-4-PIPERIDIN-1-YLPHENYL)-5-CHLOROPYRIMIDINE-2,4-DIAMINES AS MODULATORS OF ALK AND EGFR, INTENDED FOR TREATING CANCER Russian patent published in 2017 - IPC C07F9/53 A61K31/66 A61P35/00 

Abstract RU 2606951 C1

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds – dichloroacetates of substituted N4-[2-(dimethylphosphoryl)phenyl]-N2-(2-methoxy-4-piperidin-1-ylphenyl)-5-chloropyrimidine-2,4-diamine of general formula 1, which are modulators of ALK and EGFR and can be used for preventing and/or treating cancer, in particular for treating non-small cell lung cancer (NSCLC), including with metastases in brain. In formula 1

R represents dimethylamine group or 4-methylpiperazin-1-yl fragment, and k is a number 1, 2 or 3. Invention also relates to a pharmaceutical composition, containing said compound as an active component in therapeutically effective amount in combination with pharmaceutically acceptable diluent and/or carrier. Composition can be made in form of tablets, capsules or injections, placed in a pharmaceutically acceptable packaging.

EFFECT: invention also relates to a method of producing a compound of formula 1 by reacting a compound of general formula 2, where R is a dimethylamine group or 4-methylpiperazin-1-yl fragment, with 1, 2 or 3 equivalents of 2,2-dichloroacetic acid.

11 cl, 2 tbl, 10 ex

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RU 2 606 951 C1

Authors

Ivashchenko Aleksandr Vasilevich

Ignatev Vasilij Gennadevich

Repik Aleksej Evgenevich

Shafeev Mikhail Ajratovich

Dates

2017-01-10Published

2015-11-19Filed