COUMARONE DERIVATIVES ELICITING COMT-INHIBITING ACTIVITY Russian patent published in 2006 - IPC C07D311/42 C07D405/04 C07D215/20 A61K31/352 A61P25/06 

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to novel coumarone derivatives of the general formula (1): wherein two OH-substitutes in phenyl moiety are in ortho-position with respect to one to another; R₁ is in ortho-position with respect to one hydroxyl group; X means oxygen atom (O); R₁ represents -NO₂; R₂ represents hydrogen atom or (C₁-C₆)-alkyl; R₃ means -(Y)_n-(B)_m-COOH or -(Y)_n-(B)_m-R₈ wherein m = 0 or 1; n = 0; Y represents -CO-; B represents (C₁-C₆)-alkylene; R₈ represents phenyl or 5- or 6-membered heterocycle with one-four heteroatoms chosen from nitrogen atom (N) wherein indicated phenyl is substituted optionally with one substitute chosen from halogen atom, -NO₂ or (C₁-C₆)-alkyl; or R₂ and R₃ form in common -(CH₂)_r- wherein r = 3, 4 or 5; R₄ and R₅ form in common -O; R₆ means hydrogen atom (H), or to their pharmaceutically acceptable salts or pharmaceutically acceptable esters that are inhibitors of enzyme - catechol O-methyltransferase (COMT). Invention provides preparing novel coumarone derivatives possessing the valuable biologically active effect.

EFFECT: valuable biochemical property of derivatives.

9 cl, 1 tbl, 13 ex