NOVEL THIOPHENE DERIVATIVES AS S1P1/EDG1 RECEPTOR AGONISTS Russian patent published in 2011 - IPC C07D333/22 C07D413/04 A61K31/381 A61K31/4245 A61P37/06 

FIELD: chemistry.

SUBSTANCE: invention relates to thiophene derivatives of formula (I) where A denotes *-CO-CN=CH-, *-CO-CH₂CH₂-, or where the sign * indicates the thiophene bonding site in formula (I), R¹ denotes hydrogen or methyl, R² denotes n-propyl or isobutyl, R³ denotes hydrogen, methyl, ethyl, n-propyl, isopropyl or isobutyl, R⁴ denotes hydrogen or methoxy, R⁵ denotes hydrogen, C₁-C₄alkyl, C₁-C₄alkoxy or hydrogen, R⁶ denotes -(CH₂)_k-(CHR⁶⁵)_p-CHR⁶⁶-CONR⁶¹R⁶² hydroxy, hydroxy(C₂-C₄)alkoxy, di(hydroxy(C₁-C₄)alkyl)(C₁-C₄)alkoxy, 2,3-dihydroxypropoxy, -OCH₂-(CH₂)_m-NHCOR⁶⁴, -OCH₂-CH(OH)-CH₂-NR⁶¹R⁶², -OCH₂- CH(OH)-CH₂-NHCOR⁶⁴ or -OCH₂-CH(OH)-CH₂-NHSO₂R⁶³, R⁶¹ denotes hydrogen, 2-hydroxyethyl, 2-hydroxy-1-hydroxymethylethyl, carboxymethyl or C₁-C₄alkylcarboxymethyl, R⁶² denotes hydrogen, R⁶³ denotes methyl or ethyl, R⁶⁴ denotes hydroxymethyl, methyl aminomethyl or 2-methyl aminoethyl, R⁶⁵ denotes hydrogen, R⁶⁶ denotes hydrogen, m equals 1 or 2, k equals 0, p equals 1, R⁶⁷ denotes hydrogen, C₁-C₄alkyl or halogen, and to a salt thereof. The invention also relates to a pharmaceutical composition for preventing or treating diseases or disorders associated with an activated immune system based on said compounds.

EFFECT: obtaining novel compounds and a pharmaceutical composition based on said compounds, which can be used in medicine as immunodepressants.

31 cl, 2 tbl, 114 ex