FIELD: medicine, pharmaceutics.
SUBSTANCE: claimed invention relates to novel derivatives of phenylethinyl of formula (I) or to their pharmaceutically acceptable acid addition salts, possibly, in the form of a racemic mixture, or an enantiomer, that corresponds to it, and/or an optic isomer, and/or a stereoisomer. The compounds possess properties of positive allosteric modulators (PAM) of metabotropic glutamate receptors of subtype 5 (mGluR5) and can be used in the treatment of schizophrenia or cognitive disorders. In formula (I)
R1 represents hydrogen, halogen, lower alkyl or a lower alkyl, substituted with halogen; R2 represents hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl, substituted with hydroxyl; X represents N, CF or CH; L represents -NR3-, -NHC(R3)2-, -O-, -OC(R3)2-, -CR4R4'-; R3 represents hydrogen or lower alkyl, R4/R4' independently on each other represent hydrogen or lower alkyl; cyc represents cycloalkyl or heterocycloalkyl, or represents a non-aromatic bicycle, selected from 7-oxa-bicyclo [2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n represents 1, 3 or 3.
EFFECT: obtaining novel phenylethinyl derivatives.
23 cl, 1 tbl, 44 ex
Title | Year | Author | Number |
---|---|---|---|
ARYLETHINYL DERIVATIVES | 2011 |
|
RU2573560C2 |
ETHINYL DERIVATIVES | 2010 |
|
RU2553461C2 |
OXAZOLINE DERIVATIVES FOR TREATING CNS DISORDERS | 2010 |
|
RU2569887C2 |
DIHYDROOXAZOLE-2-AMINE DERIVATIVES | 2011 |
|
RU2587512C2 |
NITROGEN-CONTAINING HETEROARYL DERIVATIVES | 2011 |
|
RU2559895C2 |
4,5-DIHYDRO-OXAZOL-2-YL DERIVATIVES | 2009 |
|
RU2513086C2 |
N-PHENYL-2-PYRIMIDINE DERIVATIVES | 2003 |
|
RU2370493C2 |
DERIVATIVES OF N-(IMIDAZOPYRIMIDIN-7-YL)-HETEROARYLAMIDES AND THEREOF APPLICATION AS PDE10A INHIBITORS | 2011 |
|
RU2562066C2 |
2-OXA-5-AZABICYCLO[2.2.1]HEPTANE-3-YL DERIVATIVES | 2015 |
|
RU2697651C2 |
2-AMINO-PYRIMIDINE DERIVATIVES AS JNK INHIBITORS | 2011 |
|
RU2572247C2 |
Authors
Dates
2015-09-10—Published
2010-10-25—Filed