PYRROLIDINE DERIVATIVES APPLICABLE AS CATEPSIN DERIVATIVES Russian patent published in 2015 - IPC C07D401/04 C07D403/04 C07D413/04 C07D487/04 A61K31/44 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (I) such as below, or to their pharmaceutically acceptable salts, wherein R¹ means H, C_1-8alkyl morpholinyl, haloC_1-8alkylamino, C_1-8alkyloxadiazolyl, hydroxyl, halopyrrolidinyl, azetidinyl, C_1-8alkylamino, amino, cyano C_1-8alkylamino, halophenylC_1-8alkylamino or cyanoC_3-8cycloalkylamino; R², R³, R⁴, R⁵ and R⁶ independently mean H, C_1-8alkyl, haloC_1-8alkyl, hydroxyC_1-8alkyl, C_1-8alkoxy, haloC_1-8alkyloxy, halogen, hydroxyl, cyanopyrazinyloxy, halogen, hydroxyl, cyanopyrazinyloxy, pyrazolyl, C_1-8alkylpyrazolyl, imidazolyl, benzimidazolyl, 6-oxo-6H-piridazinyl, C_1-8alkyl-6-oxo-6H-pyridazinyl, piperazinyl, N-C_1-8alkylpiperazinyl, piperidinyl, difluoropyrrolidinyl, phenylimidazolyl, oxo-pyrrolidinyl, oxo-oxazolidinyl, morpholinyl, oxo-morpholinyl, oxo-pyridinyl, 2-oxo-2H-pyrazinyl, difluoropiperidinyl, haloC_1-8alkylpiperidinyl, piperidinylC_1-8alkoxy, oxetanyloxy, C_1-8alkylpyrazolyl, halopyridinyl, C_1-8alkylpyridinyl, C_3-8cycloalkyl, C_3-8 cycloalkylC_1-8alkyl, halophanyl, C_1-8alkylcarbonylamino-C_3-8-cycloalkyl-C_1-8alkyl, haloC_1-8alkylpiperazinyl, C_1-8alkylamino, C_1-8alkoxy-C_1-8alkylpiperazinyl, C_3-8cycloalkylpiperazinyl, hexahydropyrrolo[1,2-a]pyrazinyl, 5,6-dihydro-8H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl, C_1-8alkylimidazolyl, azetidinyl, C_3-8cycloalkylpiperazinyl, C_1-8alkylimidazolyl, C_1-8alkoxy C_1-8alkoxy, imidazo[4,5-c]pyridinyl, C_1-8alkylpiperazinyl, hexahydro-pyrrolo[1,2-a]pyrazinyl, haloazetidinyl, pyrimidinyl and C_2-8alkenyloxy; A¹ means -CH₂-, carbonyl, -C(O)O- or is absence; A² means N, CR⁷; A³ means N, CR⁸; A⁴ means N, CR⁹; R⁷ means H, C_1-8alkyl, haloC_1-8alkyl, halogen, hydroxyl, haloC_1-8alkylaminocarbonyl; halophenylC_1-8alkylaminocarbonyl, phenyl-C_3-8-cycloalkylaminocarbonyl, haloC_1-8alkylphenylC_1-8alkylaminocarbonyl, halophenylC_3-8 cycloalkylaminocarbonyl, halophenylC_3-8cycloalkylC_1-8alkylaminocarbonyl; R⁸ means H, C_1-8alkyl, haloC_1-8alkyl, halogen or hydroxyl; or R⁷ and R⁸ together with a carbon atom they are attached to, form C_3-8cycloalkyl or substituted pyrrolidine, wherein substituted pyrrolidine represents pyrrolidine, N-substituted haloC_1-8alkyl or formyl; R⁹ means H, C_1-8alkyl, haloC_1-8alkyl, halogen or nitro; or R⁸ and R⁹ together with a carbon atom they are attached to, form C_3-8cycloalkyl; or its pharmaceutically acceptable salt

EFFECT: compounds inhibit the enzyme catepsin that enables using them in pharmaceutical compositions.

27 cl, 8 dwg, 1 tbl, 88 ex