COMPOUNDS AND COMPOSITIONS FOR MODULATING KINASE ACTIVITY OF EGFR MUTANTS Russian patent published in 2025 - IPC A61K31/5377 A61K31/506 A61P35/00 C07D403/04 C07D403/14 C07D409/14 C07D405/14 C07D413/14 C07D401/14 

Abstract RU 2838180 C1

FIELD: pharmaceutics.

SUBSTANCE: present invention relates to a pharmaceutical composition and use thereof for treating non-small cell lung cancer. Disclosed composition contains, as an active ingredient, a compound selected from: N-(2-(dimethylamino)-5-(4-(4-((dimethylamino)methyl)-3-methyl-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxyphenyl)acrylamide, N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(3-cyclopropyl-4-((dimethylamino)methyl)-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(4-(azetidin-1-ylmethyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(4-((ethyl(methyl)amino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(3-cyclopropyl-4-((dimethylamino)methyl)-1H-pyrazol-1-yl)-5-methylpyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(4-(azetidin-1-ylmethyl)-3-cyclopropyl-1H-pyrazol-1-yl)-5-methylpyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, N-(5-(4-(4-((dimethylamino)methyl)-3-isopropyl-1H-pyrazol-1-yl)-5-methylpyrimidin-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, or a pharmaceutically acceptable salt thereof.

EFFECT: disclosed pharmaceutical composition demonstrates inhibitory activity against certain mutant forms of EGFR and is used to treat non-small cell lung cancer.

2 cl, 1 dwg, 7 tbl, 159 ex

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RU 2 838 180 C1

Authors

Suh Byung-Chul

Salgaonkar Paresh Devidas

Lee Jaekyoo

Koh Jong Sung

Song Ho-Juhn

Lee In Yong

Lee Jaesang

Jung Dong Sik

Kim Jung-Ho

Kim Se-Won

Dates

2025-04-11Published

2024-03-04Filed