INHIBITORS OF CATECHOL-O-METHYLTRANSFERASE AND THEREOF APPLICATION IN TREATMENT OF PSYCHIC DISORDERS Russian patent published in 2016 - IPC C07D239/54 C07D239/553 C07D239/62 C07D401/14 C07D401/04 A61K31/513 A61K31/515 A61P25/18 A61P25/24 A61P25/30 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel compounds of 4-pyrimidinone of structural formula I and II, which possess properties of catechol-O-methyltransferase (COMT) inhibitor. Compounds can be applied in treatment and prevention of neurological, psychic disorders and diseases, which COMT fragment is involved in, such as negative and positive symptoms of schizophrenia, depression, depressive phase of bipolar disorder, diseases, associated with DA deficiency, such as ADD/ADHD, and addiction, such as opiate, drug and tobacco-addiction, as well as against growth of weight/sense of hunger, associated with cessation of smoking of use of antipsychotics. In formula and compounds A represents hydrogen or C_1-6alkyl; X represents hydrogen or halogen; R¹ represents phenyl or heterocyclyl, selected from 6-membered unsaturated heterocyclyl with one nitrogen atom in cycle, where said phenyl and heterocyclyl is substituted with 1-3 groups R^a; R² represents C_1-6alkyl, N(CH₃)₂, (CH₂)_nC_5-10heterocyclyl, (CH₂)_nC_6-10aryl, where said aryl and heterocyclyl is optionally substituted with 1-2 groups R^a; R^a represents halogen, C₂-₄alkinyl, (CH₂)_nCF₃, CN, NHSO₂R², OR², (CH₂)_nC₅-₁₀heterocyclyl, containing 1-2 nitrogen atoms and possibly additionally oxygen or sulphur atom in ring, (CH₂)_nC₆aryl, O(CH₂)_nC₆aryl, where said aryl represents phenyl, where said alkinyl, heterocyclyl and aryl is optionally substituted with 1-3 groups R^b; R^b represents C_1-6alkyl, OC_1-6alkyl, halogen, CHF₂, OCHF₂, -O-, (CH₂)_nC₆aryl, (CH₂)_nC₅heterocyclyl, containing 3 heteroatoms in cycle, selected from nitrogen and oxygen, OR², (CH₂)_nCF₃, where said heterocycle is optionally substituted with 1 or several C_1-6alkyls; and n equals 0-1.

EFFECT: invention relates to pharmaceutical composition, containing claimed invention compounds and possibly additionally containing monoamine oxidase inhibitor (MAOI), selected from moclobemide.

16 cl, 1 tbl, 8 ex