8-(1-{4-{(5-CHLORO-4-{(2-(DIMETHYLPHOSPHORYL)PHENYL)AMINO}PYRIMIDIN-2-YL)AMINO)-3-METHOXYPHENYL}PIPERIDIN-4-YL)-1-METHYL-1,8-DIAZASPIRO(4.5)DECAN-2-ONE AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS AS AN ALK AND EGER MODULATOR FOR TREATMENT OF CANCER Russian patent published in 2018 - IPC C07F9/6558 C07F9/6561 A61K31/675 A61P35/00 

Abstract RU 2654695 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to novel 8-(1-{4-{(5-chloro-4-{(2-(dimethylphosphoryl)phenyl)amino}pyrimidin-2-yl)amino)-3-methoxyphenyl}piperidin-4-yl)-1-methyl-1,8-diazaspiro(4.5)decan-2-one of formula 1 below, and its pharmaceutically acceptable salts. 1. Invention also relates to an anti-cancer pharmaceutical composition; to use of a compound of general formula 1 for use with an additional anticancer agent for simultaneous, separate or sequential administration in the treatment of cancer. Invention relates to a process for the preparation of a compound of formula 1 by reacting 8-(1-{4-amino-3-methoxyphenyl}piperidin-4-yl)-1-methyl-1,8-diazaspiro(4.5)decan-2-one hydrochloride with 2,5-dichloro-N-[2-(dimethylphosphoryl)phenyl]pyrimidin-4-amine. Invention also relates to a process for the manufacture of a medicament by mixing a compound of general formula 1 and pharmaceutically acceptable excipients, followed by formation of a tablet, capsule or injection, placed in a pharmaceutically acceptable package.

EFFECT: compounds possess the properties of anaplastic lymphoma (ALK) kinase inhibitor and epidermal growth factor receptor (EGFR) and are intended for the treatment of cancer, in particular cancer, which is non-small cell lung cancer (NSCLC), including metastases in the brain.

15 cl, 2 tbl, 10 ex

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RU 2 654 695 C1

Authors

Ivashchenko Aleksandr Vasilevich

Ignatev Vasilij Gennadevich

Repik Aleksej Evgenevich

Shafeev Mikhail Ajratovich

Dates

2018-05-22Published

2017-07-28Filed