SYNERGISTIC COMBINATIONS OF PI3K- AND MEK-INHIBITORS Russian patent published in 2017 - IPC A61K31/4184 A61K31/4439 A61K47/00 A61P35/00 

Abstract RU 2607944 C2

FIELD: pharmaceutics.

SUBSTANCE: group of inventions relates to pharmaceutics. Described is a pharmaceutical composition and a combination of a phosphatidylinositol-3-kinase (PI3K) inhibitor and mitogen-activated protein kinase (MEK) inhibitor for treating colorectal cancer, having BRAF mutation, KRAS mutation, PIK3CA mutation or combination thereof and without PTEN mutation; pancreatic cancer, having KRAS mutation; non-small-cell lung cancer with KRAS mutation; or melanoma, having PTEN mutation. PI3K inhibitor used is 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-pyridin-4-yl]-thiazol-2-yl}-amide)-2-amide of (S)-pyrrolidine-1,2-dicarboxylic acid or its pharmaceutically acceptable salt. MEK inhibitor used is (2-hydroxyethoxy)-amide of (S)-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid or pharmaceutically acceptable salt thereof. Also described is a method of treating said diseases with combination and use of said combination for preparing a drug for treating said diseases.

EFFECT: use of said two inhibitors provides a synergistic effect of using said composition or a combination.

6 cl, 2 dwg, 3 ex

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RU 2 607 944 C2

Authors

Fritch Kristin

Khuan Sichzhun

Bem Markus

Di Tomazo Emmanyuell

Kosart Yan Gse

Dates

2017-01-11Published

2012-08-30Filed