OXYGEN-SUBSTITUTED DERIVATIVES OF 3-HETEROAROYLAMINOPROPIONIC ACIDS AND THEIR APPLICATION AS PHARMACEUTICAL SUBSTANCES Russian patent published in 2015 - IPC C07D231/20 C07D231/22 C07D401/04 C07D401/12 C07D403/12 C07D405/12 C07D413/12 C07D417/12 A61K31/415 A61P9/00 A61P11/00 A61P13/12 A61P25/28 A61P29/00 A61P37/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to formula compounds and their pharmaceutically acceptable salts, where A represents C(R¹); D represents N(R²); E represents N; G are selected from group, consisting of R⁷¹-O-C(O)- and R⁷²-N(R⁷³)-C(O)-; R¹ are selected from hydrogen, halogen and (C₁-C₆)-alkyl; R² are selected from (C₁-C₇)-alkyl, (C₃-C₇) cycloalkyl-C_sH_2s- and Ar-C_sH_2s-, where s equals 0, 1, 2 and 3; R¹⁰ are selected from R¹¹-O-, R¹²-N(R¹³)-C(O)-O- and Het²-C(O)-O-; R¹¹ are selected from hydrogen, R¹⁴, (C₃-C₇)-cycloalkyl and Ar; R¹² and R¹³ independently on each other are selected from hydrogen, R¹⁵ and Ar; R¹⁴ represents (C₁-C₁₀)-alkyl, which is optionally substituted with 1-3 similar or different substituents, selected from halogen, HO-, R¹⁶-O-, oxo, (C₃-C₇)-cycloalkyl, optionally substituted with 1-3 fluorine atoms, Ar, Het¹, Het³, di((C₁-C₄)-alkyl)N-C(O)- and Het¹-C(O)-; R¹⁵ represents (C₁-C₆)-alkyl; R¹⁶ represents (C₁-C₆)-alkyl, which is optionally substituted with (C₁-C₄)-alkyl-O-; R³⁰ is selected from group, consisting of R³¹, R³²-C_uH_2u- and Het³-C_uH_2u-, where u equals 0; R³¹, R³² and R³³ are such as given in invention formula; R⁴⁰ represents hydrogen; R³⁰ and R⁴⁰ together represent (CH₂)_x, x equals 2, 3, 4 or 5; R⁵⁰ is selected from group, consisting of hydrogen and HO-; R⁶⁰ represents hydrogen; R⁷¹, R⁷² and R⁷³ are such as given in invention formula; Ar is selected from group, consisting of phenyl and aromatic 6-membered monocyclic heterocycle, which includes one nitrogen atom, with phenyl and heterocycle being optionally substituted with 1-3 similar or different substituents, selected from halogen (C₁-C₆)-alkyl, optionally substituted with 1-3 fluorine atoms, (C₁-C₆)-alkyl-O-, (C₁-C₆)-alkyl-S(O)_m-, H₂N-S(O)₂- and NC-; Het¹, Het², Het³ and Het⁴ are such as given in invention formula; m equals 0, 1 and 2. Invention also relates to method of obtaining formula I compounds, pharmaceutical composition and application.

EFFECT: formula I compounds, possessing properties of cathepsin A protease.

2 cl, 2 tbl, 762 ex