HETEROCYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS AS CATHEPSIN S TRANSPORTATION INHIBITORS Russian patent published in 2011 - IPC C07D413/12 C07D411/12 C07D295/182 C07D498/04 A61K31/422 A61K31/423 A61K31/424 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of general formula

,

where R₁ is selected from formulae

, and ,

n equals 0; R₆ and R₇ are independently selected from hydrogen, C₁-C₆alkyl, cyanoC₁-C₆alkyl, C₃-C₆cycloalkylC₀-C₄alkyl and C₆arylC₀-C₄alkyl; or R₆ and R₇ together with a carbon atom to which they are bonded form a 6-member heterocycloalkyl with one nitrogen atom; wherein any alkyl in R₆ and R₇ can optionally contain a methylene group substituted with an O atom; wherein any aryl in R₆ and R₇ or formed by a combination of R₆ and R₇ can be optionally substituted with one radical independently selected from: halide, C₁-C₆alkyl, -XC(O)OR₁₀; where X denotes a bond; R₁₀ is independently selected from C₁-C₆alkyl; R₈ is selected from C₅-C₉heteroarylC₀-C₄alkyl containing 2-3 heteroatoms independently selected from N, O and S; wherein any heteroaryl in R₈ can be optionally substituted with one radical independently selected from: halide, C₁-C₆alkyl, C₃-C₆cycloalkyl; R₂ denotes hydrogen; R₃ and R₄ are independently selected from hydrogen, C₁-C₆alkyl, C₃-C₆cycloalkylC₀-C₄alkyl and C₆arylC₀-C₄alkyl; wherein any alkyl in R₃ and R₄ can optionally contain a methylene group substituted with a S(O)₂ group; R₅ is selected from C₅-C₆heterocycloalkyl with 1-2 heteroatoms selected from N and O, and NR₁₂R₁₃; where R₁₂ and R₁₃ are independently selected from C₁-C₆alkyl; as well as pharmaceutically acceptable salts and isomers thereof. The invention also relates to use of compounds of formula (I) in preparing a medicinal agent, and to a pharmaceutical composition having cathepsin S inhibiting properties, which contains a therapeutically effective amount of the compound of formula (I) in combination with a pharmaceutically acceptable filler.

EFFECT: obtaining compounds which can be used as cathepsin S inhibitors.

10 cl, 12 dwg, 2 tbl, 9 ex