NON-ANNELATED TYOPHENYLAMIDS AS INHIBITORS OF FATTY ACIDS FABP 4 AND / OR 5 BINDING PROTEINS Russian patent published in 2018 - IPC C07D413/14 C07D417/14 C07D417/04 C07D333/36 C07D409/14 C07D413/04 A61K31/381 A61K31/426 A61K31/433 A61P3/10 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of (I)

where R¹ and R² formula independently selected from H, alkyl, haloalkyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkyl, cycloalkylalkyl, halocycloalkyl, halocycloalkylalkyl, substituted aryl, substituted arylalkyl, substituted heterocycloalkyl, substituted heterocycloalkylalkyl, substituted heteroaryl, substituted heteroarylalkyl, substituted aminocarbonyl, alkoxycarbonyl, haloalkoxycarbonyl and carboxy, wherein the substituted aryl, substituted arylalkyl, substituted heterocycloalkyl, substituted heterocycloalkylalkyl, substituted heteroaryl and substituted heteroarylalkyl are substituted with R¹⁴, R¹⁵ and R¹⁶, and wherein the substituted aminocarbonyl on the nitrogen atom is substituted with from one to two substituents independently selected from H, alkyl, cycloalkyl, haloalkyl, alkylcycloalkyl, cycloalkylalkyl, alkylcycloalkylalkyl, hydroxyalkyl and alkoxyalkyl; R³ is pyrrolidinyl, substituted [1,2,4]-oxadiazolyl, oxazolyl, substituted thiazolyl, substituted [1,2,4]thiadiazol-5-yl or pyrimidinyl, wherein the substituted with [1,2,4] thiadiazol-5-yl substituted [1,2,4]-oxadiazolyl and substituted thiazolyl are substituted with R¹⁷; R⁴ is H or alkyl; R⁵ and R⁶ are independently selected from H, alkyl and cycloalkyl; R⁷ is H, alkyl or cycloalkyl; A represents NR⁸ or CR⁹R¹⁰; E is CR¹²R¹³; R⁸ is selected from H, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, cycloalkylalkyl or halocycloalkylalkyl; R⁹ and R¹² together with the carbon atoms to which they are attached, form a substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl or substituted heteroaryl, wherein the substituted cycloalkyl, substituted cycloalkenyl, substituted aryl, substituted heterocycloalkyl, and substituted heteroaryl are substituted with R²⁰ and can be further substituted with R²¹, where in the case when R⁹ and R¹² together with the carbon atoms to which they are attached, form a substituted aryl or substituted heteroaryl, R¹⁰ and R¹³ are absent; R¹⁰ and R¹³ together with the carbon atoms to which they are attached form a double bond; R¹⁴, R¹⁵, R¹⁶, R¹⁷, R²⁰ and R²¹ are independently selected from H, hydroxy, oxo, halogen atom, alkyl, haloalkyl, cycloalkyl, haloalkoxyalkyl, alkoxy, halogenalkoxy, alkoxyalkyl, haloalkoxyalkyl, alkoxycarbonyl, carboxy and an amino group on the nitrogen atom substituted with from one to two substituents independently selected from H, alkyl, cycloalkyl, haloalkyl, alkylcycloalkyl, cycloalkylalkyl, alkylcycloalkylalkyl, hydroxyalkyl and alkoxyalkyl; n is zero, inhibiting activity of fatty acids FABP4 and / or FABP5 binding proteins.

EFFECT: proposed are non-annelated thiophenylamides as inhibitors of proteins.

12 cl, 12 tbl, 10 ex