XIA FACTOR INHIBITORS Russian patent published in 2020 - IPC C07D401/02 C07D401/14 C07D413/14 C07D471/08 C07D487/04 C07D487/08 C07D513/08 A61K31/4427 A61P7/02 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula I having the properties of a coagulation factor inhibitor XIa, a pharmaceutical composition based thereon, a method of inhibiting and preventing the formation of a blood thrombosis, method of treating and using for treating venous thromboembolism and pulmonary embolism, deep vein thrombosis, thrombotic stroke. In general formula I is phenyl or 5–10-member heteroaryl with 1–2 nitrogen atoms, which is optionally substituted with one or two groups independently selected from a group, consisting of halogen, oxo, cyano, R⁶, OR⁶, C(O)OR⁶, NR⁶R⁷, NHC(O)O-C_1-3 alkyl-OR⁷; is phenyl or 5–6 membered heteroaryl with 1–2 nitrogen atoms, which is optionally substituted with one or two groups independently selected from a group consisting of halogen, oxide, cyclopropyl, R⁶; W is N or N⁺O^-; YX is -CHC(O)OR⁷-NR⁶-, -CR⁶R⁷-C(O)NR⁶-, -CHC(O)R⁷-NR⁶-; Z is C_3-4 alkylene; R¹ is phenyl, optionally substituted with one to four substitutes, independently selected from a group consisting of halogen, cyano, R⁶, OR⁶, C(O)R⁶, NR⁶R⁷, and 5-member heteroaryl with 2–4 heteroatoms selected from nitrogen and oxygen (which is optionally substituted with halogen, cyano, cyclopropyl, C(O)OH, or R⁶); R² denotes hydrogen or OR⁶; R³ denotes hydrogen; each R⁴ independently represents C_1-6 alkyl; R⁵ denotes hydrogen, halogen or C_1-6 alkyl; or one of R⁴ and R⁵ can be taken together with atoms between them to form 3–6-member alkyl ring; each R⁶ independently represents hydrogen or C_1-6 alkyl, which is optionally substituted with one to three groups independently selected from a group consisting of halogen; each R⁷ independently represents hydrogen, C_1-6 alkyl, 6-member heteroaryl with 1 to 2 nitrogen atoms or 5-member heterocyclyl with 1 nitrogen atom, wherein said alkyl group is optionally substituted with one to three groups independently selected from a group consisting of halogen; R^a is hydrogen or hydroxy; n is an integer from zero to one.

EFFECT: inhibitors of factor XIa are offered.

15 cl, 172 ex