1a, 5a-TETRAHYDRO-S-THIACYCLOPROPA[a]PENTALENES: TRICYCLIC DERIVATIVES OF THIOPHENE AS S1P1/EDG1 RECEPTOR AGONISTS Russian patent published in 2010 - IPC C07D333/78 C07D409/12 A61K31/38 A61K31/4436 A61P37/00 

FIELD: chemistry.

SUBSTANCE: described are novel thiophene derivatives of formula (1) and pharmaceutically acceptable salts thereof, where A is -CH₂CH₂-, -NH-CH₂-, -CH₂-O or -CH₂NH-, R¹ is hydrogen or alkyl, when X is C-R4, R¹ additionally represents halogen, and when A is -CH₂-CH₂- or -CH₂NH, R¹ additionally represents alkoxy, R² is hydrogen, alkoxy, fluoralkoxy, hydroxyalkoxy, hydroxyalkyl, di-(hydroxy)alkoxy, pyridinyl-3-methoxy, pyridinyl-4-methoxy, R³ is hydrogen, alkyl, trifluoromethyl, and when X is C-R⁴, R³ additionally represents halogen, and when A is -CH₂-CH₂-, R³ additionally represents alkoxy, X is N or C-R⁴, R⁴ is hydrogen, alkyl, alkoxy or halogen, R⁵ is methyl or ethyl. Also described are isomers of the said compounds, an initial compound for synthesis of formula (1) compound, which has agonistic effect on S1P1/EDG1 receptors, as well as a pharmaceutical composition based on formula (1) compound and use of formula (1) compound.

EFFECT: obtaining a pharmaceutical composition for preventing or treating diseases or disorders associated with activated immune system.

19 cl, 2 tbl, 167 ex