CONDENSED HETEROCYCLIC DERIVATIVES AS S1P MODULATORS Russian patent published in 2016 - IPC C07D487/04 C07D471/04 C07D491/04 C07D495/04 C07D498/04 C07D513/04 A61K31/4355 A61K31/4365 A61K31/437 A61K31/407 A61K31/55 A61P25/00 A61P25/28 A61P25/18 

FIELD: chemistry.

SUBSTANCE: invention relates to condensed heterocyclic derivative of formula (I), selected from structures A, B, C, D and E, where R1 is selected from (1-4C)alkyl; (3-6C)cycloalkyl; indanyl, optionally substituted with halogen; phenyl, optionally substituted with one-three substituents, independently selected from halogen, cyano, (1-4C)alkyl, optionally substituted with one or several fluorine atoms, (1-4C)alkoxy, optionally substituted with one or several fluorine atoms; pyridyl, optionally substituted with one halogen atom; Z represents linker group -W-(C_n-alkylene)-T-, where W is bound with R1 and is selected from bond, -O-, -S-, -SO₂-, -NH-,-CH=CH-, -C≡C- and trans-cyclopropylene; n represents integer number from 0 to 2, T is bound with phenylene fragment and is selected from bond, -O-, -S-, -SO₂-, -NH-, -CO-, -C=C-, -C≡C- and trans-cyclopropylene; R2 represents H or one or two substituents, independently selected from halogen, (1-4C)alkyl, optionally substituted with one-three halogen atoms, or (104C)alkoxy; X is selected from C or N; if X represents C, R3 is selected from H and (1-4C)alkyl, in other case R3 is absent; Y is selected from NH, O and S; R4 represents (1-4C)alkylene-R5 where one or several carbon atoms in alkylene group can be independently substituted with one or two halogen atoms or (CH₂)₂, with formation of cyclopropyl part, R5 represents -COOH. The invention also relates to pharmaceutically acceptable salts of formula (I) compounds, pharmaceutical composition, containing formula (I) compounds, and application of formula (I) compounds for medication manufacturing.

EFFECT: formula compounds, demonstrating properties of receptor S1P agonists.

24 cl, 1 dwg, 1 tbl