COMPOUNDS THAT INHIBIT RELEASING INFLAMMATORY CYTOKINES Russian patent published in 2006 - IPC C07D487/04 A61K31/506 A61P29/00 

FIELD: organic chemistry, biochemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a compound and to all its enantiomeric and diastereomeric forms and pharmaceutically acceptable salts that are able to prevent extracellular release of inflammatory cytokines. Proposed compounds have the formula (I): wherein R represents: (a) -OR³ or (b) -NR^4aR^4b; R³ represents unsubstituted or substituted phenyl wherein substitutes are: (i) halogen atom; (ii) (C₁-C₆)-alkyl; (iii) trifluoromethyl; (iv) trichloromethyl; (v) tribromomethyl; (vi) cyano-group, and (vii) (C₁-C₆)-alkoxy-group; each R^4a and R^b represents independently: (a) hydrogen atom or (b) -[C(R^5aR^5b)]_xR⁶ wherein index x = 0-5; each R^5a and R^5b represents independently hydrogen atom, linear or branched (C₁-C₄)-alkyl, (C₃-C₇)-cyclic alkyl; R⁶ represents -OR⁷ or (C₁-C₄)-alkyl; R⁷ represents hydrogen atom or (C₁-C₄)-alkyl; R¹ represents halogen-substituted phenyl; each among links R^2a and R^2b is chosen independently from the groups consisting of: (a) hydrogen atom; (b) -O(CH₂)_jR⁸; (c) -(CH₂)_jCO₂R¹⁰; (d) -(CH₂)_jCON(R¹⁰)₂; (e) a double bond when R^2a and one R^2b are chosen with formation of a double bond; (f) a ring when one R^2a and one R^2b are chosen with formation a ring and indicated ring is chosen from the group consisting of: (i) benzene and (ii) dioxalane; each R⁸ and R¹⁰ represents independently hydrogen atom or (C₁-C₄)-alkyl; j represents index from 0 to 5; m represents index from 1 to 3; n represents index from 1 to 3, and m + n = 4. Also, invention relates to a pharmaceutical composition based on abovementioned compounds that inhibits extracellular release of inflammatory cytokines, and a method for regulation of extracellular release of inflammatory cytokines.

EFFECT: valuable medicinal properties of compounds.

10 cl, 9 tbl, 11 ex