SUBSTITUTED DERIVATIVES OF 3-THIAZOLAMINEPROPIONIC ACID AND THEIR USE AS PHARMACEUTICALS Russian patent published in 2017 - IPC C07D277/56 C07D417/04 A61K31/426 A61K31/427 A61P9/00 A61P11/00 A61P13/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formulas Ia

and Ib

,

in any of its stereoisomeric form or its physiologically acceptable salt, where G R⁷¹-O-C(O)-; R1 represents hydrogen; R2 represents hydrogen; R¹⁰ represents R¹¹; R¹¹ represents Ar; R³⁰ is selected from the group including a (C₃-C₇)-cycloalkyl and R³²-C_uH_2u-, where u means an integer chosen from the series containing 0, 1, 2 and 3; R³² represents a phenyl, optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C₁-C₆)-alkyl, R³³ and (C₁-C_6)- alkyl-O-; R³³ is a phenyl optionally substituted by one substitute selected from a halogen; R⁴⁰ is selected from the group consisting of hydrogen and (C₁-C₄)-alkyl, or R³⁰ and R⁴⁰ together represent (CH₂)_x, where x is an integer selected from the group comprising 2, 3, 4 and 5; R⁵⁰ is hydrogen; R⁶⁰ is hydrogen; R⁷¹ is hydrogen; Ar, independently of each other Ar group, is selected from the group comprisng a phenyl and an aromatic 5-membered or 6-membered monocyclic heterocycle containing one or two heteroatoms selected from nitrogen and attached via a ring carbon atom, where the phenyl and the heterocycle all are optionally substituted by one or more identical or different substituents selected from the group comprising a halogen, a (C₁-C₆)-alkyl, (C₁-C₆) alkyl-O- and CF₃; where all the alkyl substituents, independently from each other and independently of any other substituents, are optionally substituted by one or more fluorine atoms. The invention also relates to obtaining the compound of formulas Ia and Ib, or a physiologically acceptable salt thereof, that is prepared by reacting a compound of formula IIa or IIb with the compound. The compound of formulas Ia and Ib or its physiologically acceptable salt is intended for use as a pharmaceutical agent having the inhibitory activity against cathepsin A.

EFFECT: substituted derivatives of the 3-thiazoleaminepropionic acid as protease inhibitors of cathepsin A.

7 cl, 1 tbl