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 C1-6alkyl; 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 Ra; R2 represents C1-6alkyl, N(CH3)2, (CH2)nC5-10heterocyclyl, (CH2)nC6-10aryl, where said aryl and heterocyclyl is optionally substituted with 1-2 groups Ra; Ra 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 Rb; Rb represents C1-6alkyl, OC1-6alkyl, 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 C1-6alkyls; 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
Title | Year | Author | Number |
---|---|---|---|
CATECHOL-O-METHYL TRANSFERASE INHIBITORS AND USE THEREOF IN TREATING PSYCHOTIC DISORDERS | 2011 |
|
RU2586974C2 |
CATECHOL-O-METHYLTRANSFERASE INHIBITORS AND THEREOF APPLICATION FOR TREATMENT OF PSYCHOTIC DISORDERS | 2011 |
|
RU2563634C2 |
TRKA KINASE INHIBITORS, COMPOSITIONS BASED THEREON AND METHODS | 2015 |
|
RU2672583C2 |
DERIVATIVES OF BENZIMIDAZOL, COMPOSITIONS CONTAINING THEM, OBTAINING AND APPLICATION | 2004 |
|
RU2346938C2 |
BORONIC ACID DERIVATIVES AND THEIR THERAPEUTIC USE | 2017 |
|
RU2773346C2 |
IMIDAZOPYRIDINE COMPOUNDS AS PAD INHIBITORS | 2018 |
|
RU2782743C2 |
COMPOSITIONS AND METHODS FOR JAK PATH INHIBITION | 2011 |
|
RU2672100C2 |
N-(PYRID-4-YL) AMIDES AND N-(PYRIMIDIN-4-YL) AMIDES AND THEIR PHARMACEUTICAL AND COSMETIC APPLICATION | 2012 |
|
RU2625789C2 |
HETEROCYCLIC ANALOGUES OF PYRIMIDINES AS JAK INHIBITORS | 2012 |
|
RU2564419C1 |
N-7 SUBSTITUTED PURINES AND PYRAZOLOPYRIMIDINES, COMPOSITIONS THEREOF AND METHODS FOR USE | 2010 |
|
RU2515541C2 |
Authors
Dates
2016-01-20—Published
2011-02-28—Filed