DERIVATIVES OF BENZIMIDAZOL INHIBITING FACTOR Xa Russian patent published in 2009 - IPC C07D413/14 C07D401/14 C07D417/14 C07D471/04 C07D401/12 C07D451/06 C07D413/12 C07D409/14 C07D473/08 C07D495/04 A61K31/4184 A61P7/02 

FIELD: chemistry.

SUBSTANCE: invention concerns compounds of the formula I , where R⁰ is 1) monocyclic 6-14-member aryl, where aryl is independently mono-, di- or trisubstituted by R⁸, 2) heterocyclyl out of group of benzothiazolyl, indazolyl, pyridyl, where the said heterocyclyl is independently non-substituted or mono-, di- or trisubstituted by R⁸, and other radicals referred to in point 1 of the claim; R⁸ is halogen; on condition that R⁸ is at least one halogen atom if R⁰ is monocyclic 6-14-member aryl; substructure in the formula I is 4-8-member saturated, partly non-saturated or aromatic cyclic group including 0, 1 heteroatom selected out of nitrogen or sulfur, and is non-substituted or substituted 1, 2, 3 times by R³; Q is -(C₀-C₂)alkylene-C(O)NR¹⁰-, methylene; R¹ is hydrogen atom, -(C₁-C₄)alkyl, where alkyl is non-substituted or substituted one to three times by R¹³; R² is a direct link; R¹-N-R²-V can form 4-8-member cyclic group selected out of piperazine or piperidine group; R¹⁴ is halogen, =O, -(C₁-C₈)alkyl, -CN; V is 1) 6-14-member aryl, where aryl is independently non-substituted or mono-, di- or trisubstituted by R¹⁴, and other radicals referred to in point 1 of the claim; G is direct link, -(CH₂)_m-NR¹⁰, where m is 0 and R¹⁰ is hydrogen, -(CH₂)_m-C(O)-(CH₂)_n-, where m is 0 or 1, and n is 0, -(CH₂)_m-C(O)-NR¹⁰-(CH₂)_n-, where m is 0 or 1, and n is 0, 1 or 2, -(CH₂)_m-, where m is 1; M is 1) hydrogen atom, 2) 6-14-member aryl, and other radicals referred to in point 1 of the claim; R³ is 1) hydrogen atom, 2) halogen atom, 3) -(C₁-C₄)alkyl, where alkyl is non-substituted, and other radicals referred to in point 1 of the claim; R¹¹ and R¹² are independently the same or different and are 1) hyfrogen atom, 2) -(C₁-C₆)alkyl, where alkyl is non-substituted or monosubstituted by R¹³, and other radicals referred to in point 1 of the claim; or R¹¹ and R¹² can form 4-8-member monocyclic heterocyclic ring together with nitrogen atoms to which they are linked, and beside the nitrogen atom the ring can include one or two similar or different ring heteroatoms selected out of oxygen, sulfur and nitrogen; where the said heterocyclic ring is independently non-substituted or mono-, disubstituted by R¹³; R¹³ is halogen, =O, -OH, -CF₃, -(C₃-C₈)cycloalkyl, -(C₀-C₃)alkylene-O-R¹⁰; R¹⁰ is hydrogen, -(C₁-C₆)alkyl; R¹⁵ and R¹⁶ are independently hydrogen, -(C₁-C₆)alkyl; R¹⁷ is -(C₁-C₆)alkyl, -(C₃-C₈)cycloalkyl; in all stereoisomer forms and their mixes at any ratio, and physiologically tolerable salts. Compounds of the formula I are reversible inhibitors of enzyme factor Xa (FXa) and/or factor VIIa (FVIIa) of blood clotting, and can be generally applied in states accompanied by undesirable factor Xa and/or factor VIla activity, or supposing factor Xa and/or factor VIla inhibition for treatment or prevention. In addition, invention concerns methods of obtaining compounds of the formula I, their application as agents in pharmaceutical compositions.

EFFECT: obtaining compounds applicable as agents in pharmaceutical compositions.

19 cl, 1 tbl, 169 ex