ARYLETHINYL DERIVATIVES Russian patent published in 2016 - IPC C07D401/04 C07D401/14 C07D403/04 C07D413/04 C07D413/14 C07D498/04 A61K31/506 A61P25/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new ethinyl derivative of formula I in the form of a racemic mixture or respective enanthiomer and/or optic isomer and/or stereoisomer or to a pharmaceutically acceptable salt of the above compounds formed by acid addition. The compounds are allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5) and can find application in treating diseases mediated by mGluR5 action, wherein a disease is schizophrenia, cognitive disorders, fragile X syndrome or autism. In formula I

,

U is N or C(R⁵); V is CH or N; W is CH or N; provided only one of the groups U, V or W is a nitrogen atom, R⁵ is hydrogen, methyl or halogen; Y is -N(R⁶)-, -O-, -C(R^7')(R⁷)-, -CH₂O- or -CH₂S(O)₂-; R⁶ is hydrogen or lower alkyl, whereas R⁷/R^7' independently represent hydrogen, hydroxy group, lower alkyl or lower alkoxy group; R¹ is phenyl or 5-6-merous heteroaryl containing 1-2 heteroatoms specified in nitrogen atoms, which can contain one or two substitutes specified in halogen or lower alkyl; R²/R^2' independently represent hydrogen, lower alkyl, hydroxy group, lower alkoxy group, C₃-C₆-cycloalkyl, CH₂-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C₃-C₆-cycloalkyl, or a ring containing -CH₂OCH₂-; m is equal to 0, 1 or 2; if m is equal to 1, R³/R^3' independently represent hydrogen, lower alkyl, CH₂-lower alkoxy group, or together with a carbon atom, to which they are attached, can form C₃-C₆-cycloalkyl; or R³ and R² together with a carbon atom, to which they are attached, can form C_3-6-cycloalkyl or a ring containing -(CH₂)₂OCH₂-; n is equal to 0 or 1; if n is equal to 1, R⁴/R^4' independently represent hydrogen, lower alkyl, CH₂-lower alkoxy group or together with a carbon atom, to which they are attached, can form C₃-C₆-cycloalkyl; R⁴ and R² together with a carbon atom, to which they are attached, can form C_3-6-cycloalkyl; or if n is equal to 0, and Y is -N(R⁶)-, then R⁶ and R² together with a carbon atom and a nitrogen atom, to which they are attached, can form C_3-6-cycloalkyl; if n and m are equal to 0, then R² and R⁷ with a carbon atom, to which they are attached, can form C_3-6-cycloalkyl.

EFFECT: producing the compounds mediated by mGluR5 action.

28 cl, 1 tbl, 174 ex