POSITIVE ALLOSTERIC MODULATORS (PAM) Russian patent published in 2015 - IPC C07D213/74 C07D239/34 C07D239/42 C07D401/06 C07D405/12 C07D413/06 C07D493/08 A61K31/44 A61K31/4427 A61K31/505 A61K31/506 A61P25/18 A61P25/28 

Abstract RU 2561920 C2

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

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RU 2 561 920 C2

Authors

Grin Ljuk

Guba Vol'Fgang

Eshke Georg

Zholidon Siniz

Lindemann Lotar

Richchi Antonio

Rjukher Daniehl'

Shtadler Khajnts

Viejra Ehrik

Dates

2015-09-10Published

2010-10-25Filed