PHARMACEUTICAL USE OF KETOAMIDE-BASED COMPOUND Russian patent published in 2024 - IPC A61K31/404 A61K31/4412 A61K31/4025 A61K31/4439 A61K31/498 A61K31/4709 A61K31/4155 A61K31/437 A61P11/00 A61P31/14 

FIELD: medicine; pharmaceutics.

SUBSTANCE: invention relates to use of a ketoamide compound of formula (A), or a pharmaceutically acceptable salt, enantiomer or diastereomer thereof, wherein the compound is used as 3CL protease inhibitor and a human cathepsin L inhibitor for the treatment, prevention and/or alleviation of the disease caused by the new coronavirus infection (2019-nCov) of 2019, as well as to use in the manufacture of a medicinal agent for treating, preventing and/or alleviating the clinical course of diseases caused by the new coronavirus infection (2019-nCov) of 2019, and a method of treating, preventing and/or alleviating the clinical course of diseases caused by the new coronavirus infection (2019-nCov) of 2019, comprising the step of administering to a subject in need thereof, a therapeutically effective amount of a ketoamide compound of formula (A), or a pharmaceutically acceptable salt thereof. Also disclosed is a compound of formula (A), with the exception of compounds A1-A253, and a pharmaceutical composition for treating, preventing and/or alleviating the clinical course of diseases based thereon. In general formula (A), R¹ and R² are each independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-C10-alkyl, substituted or unsubstituted C3-C10-cycloalkyl, substituted or unsubstituted C3-C10-cycloalkyl-C1- C10-alkylene, substituted or unsubstituted C6-C20-aryl, substituted or unsubstituted C6-C20-aryl-C1-C10-alkylene, substituted or unsubstituted C6-C20-aryl-C2-C10-alkenylene; R³ is selected from the group consisting of substituted or unsubstituted C1-C10-alkyl, substituted or unsubstituted C2-C10-alkenyl, substituted or unsubstituted C2-C10-alkynyl, substituted or unsubstituted C3-C8-cycloalkyl, substituted or unsubstituted C3-C8-cycloalkyl-C1-C10-alkylene, substituted or unsubstituted C6-C20-aryl, substituted or unsubstituted C6-C20-aryl-C1-C10-alkylene, substituted or unsubstituted C6-C20-aryl-C2-C6-alkenylene, substituted or unsubstituted C6-C20-aryl-C2-C6-alkynylene; R⁴ is selected from the group consisting of 9–10-member heteroaromatic ring containing 1, 2 or 3 heteroatoms selected from N, O and S, 5-member heteroaromatic ring containing 1, 2 or 3 N, and 6-member heteroaromatic ring containing 1, 2 or 3 N; said groups are substituted or unsubstituted; where "substituted" refers to a hydrogen atom in a group substituted with 1, 2, 3 or 4 substituents selected from the group consisting of halogen, hydroxyl, C1-C6 alkyl, halogenated C1-C6 alkyl, C1-C6 alkoxy, halogenated C1- C6 alkoxy, C1-C6 alkylthio and halogenated C1-C6 alkylthio; R⁶ is hydrogen; when -NR⁵ and a neighboring group -(C=O)-CH₂- form a ring, R⁵ is -(CH₂)_n-, n is 2 or 3; when -NR⁵ does not form a ring with neighboring group -(C=O)-CH₂-, R⁵ is selected from the group consisting of hydrogen, substituted or unsubstituted C1-C10-alkyl, substituted or unsubstituted C3-C10-cycloalkyl; wherein in R¹, R², R³, R⁴, R⁵ and R⁶ "substituted" group each independently denotes substitution with 1, 2, 3 or 4 substituents selected from the group consisting of halogen, hydroxyl, mercapto group, nitro group, cyano group, C1-C8-alkyl, halogenated C1-C8-alkyl, C1-C8-alkoxy group, halogenated C1-C8-alkoxy group.

EFFECT: treating, preventing and/or alleviating the clinical course of the diseases caused by the new coronavirus infection (2019-nCov) of 2019.

17 cl, 2 dwg, 2 tbl, 314 ex