SUBSTITUTED N2-(4-AMINO-2-METHOXYPHENYL)-N4-[2-(DIMETHYLPHOSPHORYL)-PHENYL]-5-CHLORO-PYRIMIDINE-2,4-DIAMINES AS MODULATORS OF ALK AND EGFR, APPLICABLE FOR TREATING CANCER Russian patent published in 2017 - IPC C07F9/53 C07D471/04 C07D471/10 C07D487/10 C07D221/20 A61K31/66 A61P35/00 

Abstract RU 2607371 C1

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted N2-(4-amino-2-methoxyphenyl)-N4-[2-(dimethylphosphoryl)-phenyl]-5-chloro-pyrimidine-2,4-diamines of general formula 1 and their stereoisomers, N4-[2-(dimethylphosphoryl)-phenyl]-N2-{4-[4-(1-methyl-1,8-diaza-spiro[4.5]dec-8-yl)-piperidin-1-yl]-2-methoxyphenyl}-5-chloro-pyrimidine-2,4-diamine and their pharmaceutically acceptable salts. Compounds have anti-cancer effect and can be used for preparing a drug for preventing or treating cancer, in particular, non-small cell lung cancer (NSCLC), including with metastases in brain. In compounds of general formula 1 1, R denotes a substitute, selected from a series (a)-(o): (a)-(c), (e)-(i), (k)-(l), (m)-(o), in which R2, R3, R4 and R5 are optionally identical C1-C4alkyls; n is an optionally identical number 1 or 2; arrow indicates binding point of substitute. Invention also relates to a method of producing compounds of formula 1.

EFFECT: method comprises reacting compounds of general formula 2, 1_1(17) where R is a substitute selected from corresponding substitutes given above, with N-[2-(dimethylphosphoryl)phenyl]-2,5-dichloro-pyrimidine-4-amine of formula 1_1(17).

12 cl, 2 tbl, 4 ex

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RU 2 607 371 C1

Authors

Ivashchenko Aleksandr Vasilevich

Ignatev Vasilij Gennadevich

Repik Aleksej Evgenevich

Shafeev Mikhail Ajratovich

Dates

2017-01-10Published

2015-11-19Filed