METABOLICALLY STABLE CYP-EICOSANOID ANALOGUES FOR THE TREATMENT OF CARDIOLOGICAL DISEASES Russian patent published in 2021 - IPC C07C275/20 C07D309/14 C07D249/08 C07D257/04 C07D263/48 C07D295/192 C07D307/68 C07C311/17 C07C311/51 C07C233/56 A61K31/16 A61K31/395 A61K31/17 A61K31/18 A61K31/34 A61K31/35 A61P9/00 

FIELD: medicine.

SUBSTANCE: invention relates to a compound of the general formula P-E-I or its pharmaceutically acceptable salts, which are metabolically stable analogues of bioactive lipid mediators obtained from polyunsaturated omega-3 fatty acids (n-3 PUFA), pharmaceutical compositions based on them, their application, and a method for the treatment of cardiovascular diseases using them. In the general formula P-E-I, P is -(CH₂)_n-O-(CH₂)_k-X, n is an integer from 3 to 8; and k is 0, 1 or 2; X is CH₂OH, CH₂OAc, CH(O) or a group selected from

and ; R² is -NHR³; -NR²⁰R²¹; -OR²²; -(OCH₂-CH₂)_i-R²³; -C₃-C₁₀-heterocyclyl containing one oxygen atom; R³ is (SO₂R³⁰); C₆-aryl group optionally substituted with -O-CH₃ or COOH, heteroaryl group containing 3 carbon atoms and two heteroatoms, which are O and N; or 6-element heterocycloalkyl containing 1 heteroatom, which is O; R³⁰ is C₁-C₆ alkyl or C₆-aryl group; each of R²⁰ and R²¹ is independently H, C₁-C₆alkyl group that can be substituted with one or more hydroxyl groups; C₃-C₆cycloalkyl group, or together form 5-6-element heterocycloalkyl containing 1 or 2 heteroatoms selected from O and N; R²² is H or C₁-C₆alkyl group; R²³ is -OH; i is an integer from 1 to 10; R⁵ is H; fluorine or chlorine atom; -CF₃; -C(=O)OR⁵¹; -NHC(=O)R⁵²; -C(=O)NR⁵³R⁵⁴; or -S(O₂)OH; R⁵¹ is H or C₁-C₆alkyl group; each of R⁵², R⁵³ and R⁵⁴ is independently C₁-C₆alkyl group; R⁹ is C₁-C₆alkyl or C₆-aryl; g is 1 or 2; X¹ is an oxygen atom; a sulfur atom or NH; E is a group represented by the general formula (III) or (IV), and ring A in the formula (III) is 6-element carbocyclic ring containing at least one double bound, including 6-element aromatic carbocyclic ring; and each of L and T is independently a ring atom, L and T are adjacent to each other; each of R¹² and R¹³ is independently H, a fluorine atom or hydroxyl; I is -(CH₂)_m-Y, m is an integer from 3 to 6 provided that m is an integer from 3 to 5, when E is a group of the general formula (III); Y is a group selected from

each of R⁴⁰, R⁴¹, R⁴³ and R⁴⁴ is independently H or -C₁-C₆alkyl; each of R⁴² or R⁴⁵ is independently -C₁-C₃alkyl.

EFFECT: obtaining compositions for the treatment of cardiovascular diseases.

17 cl, 9 dwg, 3 tbl, 12 ex