AZAINDOL DERIVATIVES AS FACTOR Xa INHIBITORS Russian patent published in 2008 - IPC C07D471/04 A61K31/437 A61P7/02 

FIELD: chemistry.

SUBSTANCE: invention concerns compounds of the formula I and their pharmaceutically acceptable salts as factor Xa inhibitors, medicine based on them, as well as a method of their obtaining and application. In the general formula I R⁰ is monocyclical or bicyclical 6-9-membered heterocyclyl selected out of the group of benzothiophenyl, pyridyl or monocyclical 5-membered heterocyclyl containing 1, 2 heteroatoms selected out of nitrogen or oxygen, where the mentioned heterocyclyl is monosubstituted by R8 and additionally substituted by monocyclical 5-membered heterocyclyl containing 1 heteroatom of sulfur, where heterocyclyl is monosubstituted by R8; R8 is a halogen or substructure , which is 6-membered partially unsaturated or aromatic cyclical group in the formula I, containing 1 nitrogen heteroatom, and which is substituted by 1 R23 group or oxogroup under a condition that the mentioned cyclical group is not a phenyl residuum; Q is a direct link, -(C₀-C₂)-alkylene-C(O)-NR¹⁰-, -(C₁-C₆)-alkylene; -R¹ is a hydrogen atom; R² is a direct link, V is a 6-membered cyclical residuum with 1 heteroatom selected out of nitrogen, where the mentioned cyclical residuum is unsubstituted, bicyclical 12-membered heterocyclyl with 1-2 heteroatom selected out of nitrogen, where the mentioned cyclical residuum is unsubstituted; G is a direct link; M a hydrogen atom, -(C₁-C₈)-alkyl where alkyl is unsubstituted; R3 is a hydrogen atom; R23 is a hydrogen atom, -(C₀-C₄)-alkylene -O-R19 (where R19 is a) hydrogen atom, b) -(C₁-C₄)-alkyl where alkyl is unsubstituted or monosubstituted by R13), -(C₀-C₄)-alkylene-C(O)-R¹¹, -(C₀-C₄)-alkylene-C(O)-O-R¹¹; R11 and R12 can both or individually be hydrogen atom, -(C₁-C₆)-alkyl: -O-R¹⁷ or R13 is -C(O)-O-R¹⁰; R¹⁰ and R²⁰ are hydrogen atoms or -(C₁-C₆)-alkyl independently from each other, R17 is -(C₁-C₆)-alkyl; and its pharmaceutically acceptable salts.

EFFECT: possible application in effecting blood coagulation, inflammation reaction or fibrinolysis, or in treatment and prophylactics of diseases caused by Xa factor, eg cardiovascular disorders, thromboembolic diseases or restenosis.

11 cl, 1 tbl, 15 ex