| abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to novel compounds of the formula I n , 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; R 1 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; R 3 , R 4 , R 5 and R 6 are identical or different and are independently selected from a group comprising H, OAIk, Alk, Hal, OH; R 2 is selected from a group comprising H and O, and p'=0 or 1; R 7 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 R 7 , 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: R 3 , R 4 , R 5 , R 6 =H, R 1 =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)-, -CH 2 -, or R 3 , R 5 , R 6 =H, R 4 =OMe, R 1 =CN, denotes a single bond, and denotes -C(=O)-, or R 3 , R 4 , R 5 , R 6 =H, R 1 =NH 2 , denotes a single bond, and denotes -CH 2 - or -CH 2 -CH 2 -; or R 3 , R 4 , R 5 , R 6 =H, R,=NH 2 , denotes -CH 2 - or -CH 2 -CH 2 -, 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. n EFFECT: novel compounds which can be used in medicine are obtained and described. n 38 cl, 43 ex, 2 tbl |