IMIDAZOPYRAZINE OR IMIDAZODIAZEPINE DERIVATIVES, ACTIVE WITH RESPECT TO RECEPTOR CB2 Russian patent published in 2015 - IPC C07D471/04 A61K31/4985 A61P29/00 A61P3/04 A61P37/02 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to field of organic chemistry, namely to heterocyclic compound of general formula (I) or to its pharmaceutically acceptable salt, acid salt or stereoisomer, where Y: NR_a and N⁺R₁R₂X^-; Z: bond, -(CH₂)_p, -CHOH, -CH=CH-, -C≡C-, -CONH- and -CO-; R_b: C₁-C₈ alkyl, C₂-C₈ alkenyl, C₆-C₁₀ aryl, -NR₅R₆,: , and ; with each alkyl, alkenyl and aryl, representing R_b, possibly, contains 1-3 substituents, selected from C₁-C₄ alkyl, C₂-C₄ alkenyl, C₃-C₆ cycloalkyl, C₁-C₄ alkoxy, C₆-C₁₀ aryl, 5-, 6- and 7-membered heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, halogen, -OH, -NH₂, -CN and -NO₂; R_c: halogen, C₁-C₆ alkyl, C₂-C₆ alkenyl, C₂-C₆ alkinyl, C₃-C₁₀ cycloalkyl, C₃-C₈ cycloalkenyl, C₁-C₄ alkoxy, C₆-C₁₀ aryl, 5-, 6-, 7- and 8-membered monocyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, 9- and 10-membered bicyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; with C₁-C₆ alkyl, C₂-C₆ alkenyl C₂-C₆ alkinyl, C₃-C₁₀ cycloalkyl, C₃-C₈ cycloalkenyl, C₆-C₁₀aryl, 5-, 6-, 7-, 8-membered monocyclic heterocyclyl and 9- and 10-membered bicyclic heterocyclyl, representing R_c, possibly contain 1-5 substituents, selected from the group, consisting of C₁-C₄ alkyl, C₁-C₄ alkoxy, C₁-C₄ haloalkyl, C₁-C₄ haloalkoxy, C₃-C₆ cycloalkyl, C₄-C₈ cycloalkenyla, halogen, -OH, -NH₂, C₆-C₁₀ (A)(A')(A")(A'")aryl, (A)(A')(A")(A'")heterocyclyl, containing 1-3 heteroatom, selected from nitrogen, oxygen and sulphur, NR₁₄R₁₅, (CH₂)_pNR₁₄R₁₅, -CN, -NO₂, oxo, -COOR₁₄, SOR₁₄, SO₂R₁₄, SO₂NR₁₄R₁₅, NR₁₅SO₂R₁₆, COR₁₄, CONR₁₄R₁₅ and NR₁₅COR₁₆; with each (A), (A'), (A") and (A'")independently absent or representing C₁-C₄ alkyl, and each heterocyclyl (A)(A')(A")(A'")heterocyclyl is independently selected from the group, consisting of 5-, 6-, 7- and 8-membered monocyclic heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur, and 9- and 10-membered bicyclico heterocyclyl, containing 1-3 heteroatoms, selected from nitrogen, oxygen and sulphur; the remaining radicals have values given in i.1;and on condition that, if R_c represents heterocyclyl, said heterocyclyl is bound directly through carbon atom of heterocyclyl ring. Invention also relates to particular compounds and to pharmaceutical composition based on formula (I) compound.

EFFECT: obtained are novel imidazopyrazine and imidazodiazepine derivatives, useful for prevention or treatment of disease or condition, severity of which is reduced by receptors to cannabinoids.

21 cl, 5 dwg, 4 tbl, 71 ex