DICHLOROACETATE OF N,N-DISUBSTITUTED N-[4-(1-METHYL-1H-INDOLE-3-YL)-PYRIMIDINE-2-YL]-5-METHOXYBENZENE-1,2,4-TRIAMINE AS EGFR MODULATOR FOR TREATING CANCER Russian patent published in 2016 - IPC C07D403/04 A61K31/506 A61P35/00 

Abstract RU 2603960 C1

FIELD: chemistry, medicine.

SUBSTANCE: invention relates to novel salt - dichloroacetate N-{2-[(2-dimethylaminoethyl)methyl-amino]-5-[4-(1-methyl-1H-indole-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}acrylamide, which has properties of EGFR inhibitor and can be used for treating cancer types, mediated by EGFR and its mutants selected from L858R, 1790M and Exon19. Compound may be used for treating ovarian cancer, cervical cancer, colorectal cancer, breast cancer, pancreatic cancer, glioma, glioblastoma, prostate cancer, melanoma, leukemia, non-Hodgkin lymphoma, stomach cancer, lung cancer and hepatocellular cancer, gastrointestinal stromal tumors (GIST), thyroid cancer, bile duct cancer, endometrial cancer, renal cancer, anaplastic large cell lymphoma, acute myeloid leukemia, multiple myeloma, melanoma and mesothelioma. Preferably compound can be used for preventing and/or treating mutations of epidermal growth factor receptor EGFRm of non-small cell lung cancer (NSCLC), which also have resistent mutation T790M. N-{2-[(2-dimethylaminoethyl)methyl-amino]-5-[4-(1-methyl-1H-indole-3-yl)pyrimidin-2-ylamino]-4-methoxyphenyl}acrylamide dichloroacetate corresponds to general formula 1

.

EFFECT: prevention and/or treatment of mutations of epidermal growth factor receptor EGFRm in non-small cell lung cancer (NSCLC).

12 cl, 2 tbl, 6 ex

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RU 2 603 960 C1

Authors

Ivashchenko Aleksandr Vasilevich

Ignatev Vasilij Gennadevich

Repik Aleksej Evgenevich

Shafeev Mikhail Ajratovich

Dates

2016-12-10Published

2015-11-19Filed