NEW BICYCLIC COMPOUNDS OF THIOPHENYLAMIDE Russian patent published in 2018 - IPC C07D333/66 C07D409/04 C07D409/14 C07D413/04 C07D413/14 C07D417/04 C07D495/04 A61K31/381 A61P3/10 

FIELD: pharmacology.

SUBSTANCE: invention relates to a compound of the formula (I), where R¹ and R² together form -CR¹⁴=CR¹⁵-CR¹⁶=CR¹⁷-, -CR¹⁴R¹⁵-O-(CR¹⁶R¹⁷)_m-CR¹⁸R¹⁹-, -CR¹⁴R¹⁵-(CR¹⁶R¹⁷)_m-O-CR¹⁸R¹⁹-, -O-CR¹⁴R¹⁵-(CR¹⁶R¹⁷)_m-CR¹⁸R¹⁹-, -CR¹⁴R¹⁵-NR²²-CR¹⁶R¹⁷-CR¹⁸R¹⁹-, -CR¹⁴R¹⁵-S(O)₂-CR¹⁶R¹⁷-CR¹⁸R¹⁹-, -CR¹⁴R¹⁵-CR²⁰R²¹- or -CR¹⁴R¹⁵-CR¹⁶R¹⁷- (CR¹⁸R¹⁹)_p-CR²⁰R²¹-; R³ is phenyl or substituted 5-6 membered heteroaryl with one to three ring heteroatoms selected from N, O and S, wherein the substituted heteroaryl is substituted by R²³; R⁴ is H; R⁵ and R⁶ are independently selected from H and alkyl; R⁷ is H or alkyl; A is NR⁸ or CR⁹R¹⁰; E is NR¹¹ or CR¹²R¹³; R⁹, R¹⁰, R¹² and R¹³ are independently selected from H, a halogen atom and alkyl; or R⁸ and R¹² together with the nitrogen and carbon atoms to which they are attached, form a substituted 4-6 membered heterocycloalkyl with one nitrogen atom as a ring heteroatom, wherein the substituted heterocycloalkyl is substituted by R²⁶; or R⁹ and R¹¹ together with the nitrogen and carbon atoms to which they are attached, form a substituted 5-membered heterocycloalkyl with one nitrogen atom as a ring heteroatom; or R⁹ and R¹² together with the carbon atoms to which they are attached, form a substituted 3-8 membered saturated or unsaturated cycloalkyl, substituted phenyl, substituted 6-membered heterocycloalkyl with one oxygen atom as a ring heteroatom or substituted 5-6 membered heteroaryl with one to two nitrogen atoms as ring heteroatoms, wherein the substituted cycloalkyl, substituted phenyl, substituted heterocycloalkyl and substituted heteroaryl are substituted by R²⁶ and can be further substituted by R²⁷, where in case when R⁹ and R¹² together with the carbon atoms to which they are attached, form substituted phenyl or substituted heteroaryl, R¹⁰ and R¹³ are absent; or R¹⁰ and R¹³ together with the carbon atoms to which they are attached form a double bond; R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²³, R²⁴, R²⁵, R²⁶ and R²⁷ are independently selected from H, hydroxy, halogen, alkyl, cycloalkyl, haloalkyl, alkoxy, alkoxyalkyl and alkoxycarbonyl; or R¹⁶ and R¹⁷ together with the carbon atoms to which they are attached, form a cycloalkyl or a 4-membered heterocycloalkyl with one oxygen atom as a ring heteroatom; or R¹⁴ and R²⁰ together with the carbon atoms to which they are attached, form -CH₂-; R²² is alkoxycarbonyl; m is zero or 1; n is zero or 1; p is zero, 1 or 2; or its pharmaceutically acceptable salts and its use as inhibitors of the fatty acid binding protein FABR.

EFFECT: improved compounds properties.

27 cl, 258 ex