AMINO-SUBSTITUTED 3-HETEROAROYLAMINO-PROPIONIC ACID DERIVATIVES AND USE THEREOF AS PHARMACEUTICAL AGENTS Russian patent published in 2016 - IPC C07D231/38 C07D401/04 C07D401/12 C07D403/04 C07D403/06 C07D405/12 C07D417/04 C07D487/04 A61K31/415 A61K31/4439 A61K31/4152 A61P9/00 A61P11/00 A61P13/12 A61P25/28 A61P37/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I in form of any of its stereoisomeric forms, or its physiologically acceptable salt, where A denotes C(R¹); D denotes N(R²); E denotes N; G denotes R⁷¹-O-C(O)-; R¹ is selected from a group consisting of hydrogen and NC-; R² denotes Ar-C_sH_2s-, where s denotes an integer 0 or R² and R¹¹ together denote -C(R¹⁸)=C(R¹⁹)-; R¹⁰ is selected from a group consisting of R¹¹, R¹²-N(R¹³)-C(O)- and R¹⁴-C(O)- and (C₁-C₄)-alkyl-S(O)_m-; R¹¹ is selected from a group, consisting of hydrogen and R¹⁴ or R¹⁰ and¹¹ form Het²; R¹² and R¹³ are independently selected from a group, consisting of hydrogen and Ar; R³⁰ is selected from a group, consisting of R³¹, (C₃-C₇)-cycloalkyl, R³²-C_uH_2u-, where u denotes an integer selected from a group consisting of 0, 2 and 3; R⁴⁰ is selected from a group consisting of hydrogen and (C₁-C-₄)-alkyl; R⁵⁰ denotes hydrogen; R⁶⁰ denotes hydrogen or R³⁰ and R⁵⁰ together denote (CH₂)_z, optionally substituted with one or more identical or different (C₁-C₄)-alkyl substitutes, where z denotes an integer selected from a group consisting of 3, 4 and 5; R⁷¹ denotes hydrogen; Ar, independently from each other group Ar, is selected from a group consisting of phenyl and aromatic 5-member or 6-member monocyclic heterocycle, which comprises one cyclic heteroatom selected from a group, consisting of nitrogen, oxygen, and is bonded to other part of molecules through a cyclic carbon atom, where phenyl is optionally substituted with one or more identical or different substitutes, selected from a group consisting of halogen, (C₁-C₆)-alkyl; Het² denotes a saturated 5-6-member monocyclic heterocycle, which includes cyclic nitrogen atom, through which Het² is bonded to other part of molecule, and optionally one additional cyclic heteroatom, selected from sulphur, optionally substituted with one or more substitutes, selected from oxo; m independently from each other m denotes 2. Invention also relates to a method of producing a compound of formula I or a physiologically acceptable salt thereof, which includes reacting a compound of formula II with a compound of formula III, where groups A, D, E, G, R¹⁰, R¹¹, R³⁰, R⁴⁰, R⁵⁰ and R⁶⁰, in compounds of formulae II and III, are defined as groups in compounds of formula I, and, furthermore, there may be functional groups, which can be in protected form or in form of precursor groups, and group J, which is part of compound of formula II, denotes HO-, (C₁-C-₄)-alkyl-O- or halogen. Compound of formula I or physiologically acceptable salt thereof are intended for use as a pharmaceutical agent for inhibiting of protease of cathepsin A.

EFFECT: technical result is amino-substituted 3-heteroaroylamino-propionic acid derivatives as cathepsin A inhibitor.

8 cl, 1 tbl