BENZENE DERIVATIVE OR SALT THEREOF Russian patent published in 2010 - IPC C07D211/74 C07D401/14 C07D405/14 C07D409/14 C07D413/14 C07D417/14 A61K31/4545 A61K31/553 A61P7/02 A61P9/10 A61P9/14 

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzene derivatives of general formula (I) or salts thereof: [Chem. 12]

(Symbols in the given formula have the following values X¹:-NR¹²-C(=O)- or -C(=O)-NR¹²-, X² : -NR¹³ -C(=O)-, Ring A is a 6-member ring, if necessary having 1 or 2 double bonds and if necessary having 1-3 heteroatoms selected from N, O, Ring B is a benzene ring or a 6-member heteroaryl ring having 1-3 heteroatoms selected from N, R is a hydrogen atom or a residue of β-D- glucopyranoside uronic acid; R¹-R⁸ are identical or different and each denotes a hydrogen atom, a halogen atom, -O-(lower alkyl), R⁹-R¹¹ are identical or different and each denotes a hydrogen atom, lower alkyl, -O-(lower alkyl), -(CH₂)_n-N(lower alkyl)₂, -(CH₂)_n-NH(lower alkyl), -(CH₂)n-N(lower alkyl) (if necessary substituted with -C=O; a 6-member heterocycle having 1-3 heteroatoms selected from N, S, O) -(CH₂)_n-(C=O)-N(lower alkyl)₂, -(CH₂)_n-(C-O)-N(lower alkyl) (if necessary substituted with -C=O, alkyl, a 6-member heterocycle having 1-3 heteroatoms selected from N) -(CH₂)_n- if necessary substituted with alkyl, -COCH₃, -SO₂CH₃, -COOCH₃, -C=O, CF₃, -OCH₃, OH, halogen; 5-7-member heterocycle having 1-3 heteroatoms selected from N, S, O), -(CH₂)_n-O- (if necessary substituted with alkyl; 6-member heterocycle having 1-3 heteroatoms selected from N), n is an integer from 0 to 3, R¹² and R¹³ denote a hydrogen atom, provided that in R¹-R¹¹, when two lower alkyls are bonded to a nitrogen atom, they can together form a 3-8-member nitrogen-containing heterocycle.) The invention also relates to benzene derivatives of general formula (II), to a pharmaceutical composition, as well as to use of the said compounds.

EFFECT: obtaining novel biologically active compounds which are active as inhibitors of activated blood-coagulation factor X.

16 cl, 365 ex, 42 tbl