| 摘要 |
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 formulaandcompounds A represents hydrogen or Calkyl; X represents hydrogen or halogen; Rrepresents 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; Rrepresents Calkyl, N(CH), (CH)Cheterocyclyl, (CH)Caryl, where said aryl and heterocyclyl is optionally substituted with 1-2 groups R; Rrepresents halogen, C-alkinyl, (CH)CF, CN, NHSOR, OR, (CH)C-heterocyclyl, containing 1-2 nitrogen atoms and possibly additionally oxygen or sulphur atom in ring, (CH)Caryl, O(CH)Caryl, where said aryl represents phenyl, where said alkinyl, heterocyclyl and aryl is optionally substituted with 1-3 groups R; Rrepresents Calkyl, OCalkyl, halogen, CHF, OCHF, -O-, (CH)Caryl, (CH)Cheterocyclyl, containing 3 heteroatoms in cycle, selected from nitrogen and oxygen, OR, (CH)CF, where said heterocycle is optionally substituted with 1 or several Calkyls; 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 |
