BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS Russian patent published in 2015 - IPC C07F5/02 A61K31/69 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to compound of formula: or its pharmaceutically acceptable salts. Values of radicals are as follows: R^a represents member, selected from CN, C(O)NR¹R², C(O)OR³; R¹ and R² represent H, R³ represents H or unsaturated C₁-C₁₀ alkyl; X represents member, selected from N, CH and CR^b, R^b represents member, selected from halogen, substituted or non-substituted C₁-C₁₀ alkyl, C(O)OR⁴, OR⁴, NR⁴R⁵, where R⁴ and R⁵represent members, independently selected from H, substituted or non-substituted C₁-C₁₀ alkyl, substituted or non-substituted C₁-C₁₀ heteroalkyl, containing at least 1 heteroatom, where heteroatom represents O or N, and heteroatom can take any internal position in heteroalkyl group or take the position, through which alkyl group is bound to the remaining part of molecule, non-substituted C₃-C₁₀ cycloalkyl, pyridyl, substituted with CN group, or independently represents ; and , where alkyl and heteroalkyl substituents are independently selected from the group, including: -R', =O, -CO₂R', -OR', -OC(O)R', -NR"C(O)R', -NR'R", -CONR'R", pyridyl, halogen, , 4-methylpiperazinyl, 4-methylpiperidinyl, in quantity from 0 to 3; and where R' and R" are independently selected from the group, including hydrogen, non-substituted phenyl, non-substituted C₁-C₁₀ alkyl, C₁-C₁₀ alkoxy, on condition that R⁴ and R⁵, together with atoms to which they are bound, are optionally combined with formation of 4-8-membered non-substituted heterocycloalkyl ring, containing 1-2 heteroatoms, selected from N and O. Also claimed are pharmaceutical compositions, method of treating state, mediated by phosphodiesterase (FDE), a method of FDE inhibition.

EFFECT: invention makes it possible to obtain compounds, capable of inhibiting phosphodiesterase.

134 cl, 141 dwg, 2 tbl, 29 ex