CASPASE INHIBITOR PRODRUGS Russian patent published in 2011 - IPC C07D498/04 C07D498/12 A61K31/429 A61P9/00 A61P25/00 

FIELD: medicine.

SUBSTANCE: invention refers to a compound of formula l where R¹ represents CH₂CI, CH₂F or-C_1-2alkyl-R3R4; R³ represents -O-; R⁴ represents phenyl, where said R⁴ group is optionally substituted by 0-5 groups J where J represents halogen; R² represents C_6-10aryl; or a group: where Y represents CH, AA² represents C₁-C₇alkyl, R⁸ and R⁹ represents hydrogen or halogen; or a group: where Y represents CH, AA² represents C₁-C₇alkyl, and R6 represents hydrogen, P⁴ represents -(T)_p-R, where T represents -C(O)O-group, R represents C₁-C₁₂alkyl, and p is equal to 1; or a group: where A² represents O, R⁷ and R⁸ together with atom whereto attached form a (10-14)members tricyclic unsaturated ring, e.g. carbazole; or a group: where AA² represents C₁-C₇alkyl, and R¹⁵ represents 2-tert-butylphenyl. The declared compounds are caspase inhibitor prodrugs which under certain conditions can be transformed into biologically active compounds, particularly caspase inhibitors. Also, said invention refers to methods of producing said compounds and to a pharmaceutical composition exhibiting caspase inhibitory action on the basis of the said compounds.

EFFECT: what is produced are new compounds and based pharmaceutical composition which can find application in medicine for treating the diseases associated with inflammatory or degenerative conditions.

13 cl, 5 ex