SULTAM-BASED COMPOUND AND METHOD OF USE THEREOF Russian patent published in 2021 - IPC C07D275/03 C07D417/04 C07D417/14 A61K31/425 A61K31/433 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to compounds of formulas I and II, or pharmaceutically acceptable salts thereof, which can be used in preparing a drug preparation for treating cancer caused by an IDH1 mutation. In formula (I) X is selected from CH₂ or NR⁵; R¹ is C_3-6cycloalkyl, which can be optionally substituted with one or more groups independently selected from R⁶; R² is selected from phenyl or 5–6-member heteroaryl containing 1 to 2 heteroatoms N, which can be optionally substituted with one or more groups independently selected from R⁷; R³ is selected from 5–6 membered heteroaryl containing 1 to 2 heteroatoms N, or phenyl-CH₂-, which can be optionally substituted with one or more groups independently selected from R⁸; R⁴ is halogen; R⁵ is selected from hydrogen or C_1-6alkyl; R⁶ is halogen; R⁷ is selected from halogen, cyano, C_1-3haloalkyl, oxo or ; R⁸ is selected from halogen, cyano or C_2-6alkynyl; R⁹ is selected from H or 5–6-member heteroaryl containing 1 to 2 heteroatoms N, which can be optionally substituted with one or more groups independently selected from R¹⁰; R¹⁰ is cyano; m is equal to 1. In formula (II), X is selected from CH₂ or NR⁵; R¹ is C_3-6cycloalkyl, which can be optionally substituted with one or more groups independently selected from R⁶; R² is selected from phenyl or 5–6-member heteroaryl containing 1 to 2 heteroatoms N, which can be optionally substituted with one or more groups independently selected from R⁷; R³ is selected from 5–6 membered heteroaryl containing 1 to 2 heteroatoms N, or phenyl-CH₂-, which can be optionally substituted with one or more groups independently selected from R⁸; R⁵ is selected from hydrogen or C_1-6alkyl; R⁶ is halogen; R⁷ is selected from halogen, cyano, C_1-3haloalkyl, oxo or ; R⁸ is selected from halogen, cyano or C_2-6alkynyl; R⁹ is selected from H or 5–6 membered heteroaryl containing from 1 to 2 heteroatoms N, which can be optionally substituted with one or more groups independently selected from R¹⁰; R¹⁰ is cyano. Invention also relates to a method of treating cancers caused by an IDH1 mutation, comprising administering a therapeutically effective amount of a compound of formula I or II or a pharmaceutically acceptable salt thereof to a patient in need thereof, and to a pharmaceutical composition for inhibiting IDH1 isocitrate dehydrogenase mutation, which contains a therapeutically effective amount of a compound of formula I or II.

EFFECT: sultam-based compound and a method for use thereof are disclosed.

21 cl, 3 dwg, 3 tbl, 27 ex