NOVEL CYSTEINE PROTEASE INHIBITORS AND THERAPEUTIC APPLICATION THEREOF Russian patent published in 2011 - IPC C07D241/38 C07D491/113 C07D495/04 A61K31/495 A61K31/498 A61K31/4985 A61K31/499 A61P35/00 A61P25/28 A61P9/00 A61P31/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of the formula I

, where: m equals 0, 1 or 2, where if m=0, disappears such that an open ring or single bond forms, n equals 0, 1 or 2, wherein when n=0, disappears such that an open ring or single bond forms; m' and n' are independently equal to 0, 1 or 2; X denotes a carbon atom; Y denotes a carbon or sulphur atom; provided that m and n are not equal to 0 at the same time; denotes a single or double bond, if needed; --- absence of a bond or a single bond, if needed; R₁ is selected from a group comprising CN, Hal, OAIk, OH, NRCN, C(CN)=C(OH)(OAlk), SR, NRR', (Alk)_p-C(O)NRR', piperidine, wherein Alk is optionally substituted with Hal or OAlk, where p=0 or 1; R₃, R₄, R₅ and R₆ are identical or different and are independently selected from a group comprising H, OAIk, Alk, Hal, OH; R₂ is selected from a group comprising H and O, and p'=0 or 1; R₇ is selected from a group comprising H, O, OH, N-OH, N-aryl, N-OAlk, N-O-aryl, N-O-Alk-aryl, N-NR-CONRR', N-O-CO-Alk, or 2 R₇, bonded with the same Y, together form lioksalan; wherein said Alk is optionally substituted with OAlk, -CO-(NR-Alk-CO)p'-OAlk, and p'=0 or 1; R and R', which are identical or different, are independently selected from a group comprising H, and Alk; or pharmaceutically acceptable salt or optical isomer or diastereomer thereof, except those compounds for which: R₃, R₄, R₅, R₆=H, R₁=CN, denotes a single bond, and denotes -C(=N-(2,4,6-trimethylphenyl))-, -C(=N-(2,6- dimethylphenyl))-, -C(=N-(2,6-diethylphenyl))-, -C(=N(2-methylphenyl))-, -C(=N(2-ethylphenyl))-, -C(=N-(2-trifluoromethylphenyl))-, -C(=N-(2-isopropylphenyl))-, -C(=N-phenyl)-, -C(=N-(naphthyl)- or -C(=O)-, -CH₂-, or R₃, R₅, R₆=H, R₄=OMe, R₁=CN, denotes a single bond, and denotes -C(=O)-, or R₃, R₄, R₅, R₆=H, R₁=NH₂, denotes a single bond, and denotes -CH₂- or -CH₂-CH₂-; or R₃, R₄, R₅, R₆=H, R,=NH₂, denotes -CH₂- or -CH₂-CH₂-, and denotes a single bond. The invention also relates to a cysteine protease based pharmaceutical composition based on compounds of formula I, use of the compound of formula I to prepare a drug for inhibiting cysteine protease, for treating and preventing cancer, as well as inflammatory diseases and others.

EFFECT: novel compounds which can be used in medicine are obtained and described.

38 cl, 43 ex, 2 tbl