SPIROCYCLIC NITRILES AS PROTEASE INHIBITORS Russian patent published in 2017 - IPC C07C255/46 C07D221/20 C07D317/72 A61K31/277 A61K31/357 A61K31/438 A61P19/00 A61P35/00 

FIELD: biotechnology.

SUBSTANCE: invention relates to formula (I) compounds and physiologically acceptable salts thereof, which provide inhibitory activity against K, B and S cathepsins. In formula (I), partial cycles and , each independently from each other, are selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, dioxolane, 1,3-dioxolane and piperidine, wherein the two partial cycles are unsubstituted; X is a covalent bond; Y is -C(O)-; Z is -N(R26)-(C(R24)(R25))_m-CN; R26 represents a hydrogen atom; m is integer 1; R24 and R25, and the carbon atom to which they are attached, form a cycloalkyl selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, which is unsubstituted; R1 represents a hydrogen atom; R2 and R3 are the same or different and each independently represents a hydrogen atom or -(C₀-C₃)-alkylene-C-(R27)(R28)(R29); R27 represents a hydrogen atom, -(C₁-C₉)-alkyl, -(C₀-C₄)-alkylene-(C₃-C₆)-cycloalkyl; R28 and R29 are identical or different and independently represent a hydrogen atom, -(C₁-C₄)-alkyl; or R28 and R29 with the carbon atom to which they are attached, form -(C₃-C₆)-cycloalkyl; or R2 and R3 with the carbon atom to which they are attached, form a three to six member cycloalkyl, which is unsubstituted. The invention also relates to methods for formula (I) compounds preparation, methods for preparation of physiologically acceptable salts and N-oxides thereof, medicament containing them, and formula (I) compounds application for the manufacture of a medicament for prophylaxis, prevention and treatment of diseases, related to inhibitory activity against K, B and S cathepsins.

EFFECT: higher efficiency of compounds application.

10 cl, 2 tbl, 105 ex