1295501-83-5Relevant academic research and scientific papers
POSITIVE ALLOSTERIC MODULATORS (PAM)
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Page/Page column 41, (2011/05/11)
The present invention relates to phenylethynyl derivatives of formula (I) wherein R1 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; R2 is hydrogen, lower alkyl, =O, lower alkoxy, phenyl, hydroxy or lower alkyl substituted by hydroxy; X is N, CF or CH; L is -NR3-, -NHC(R3)2-, -O-, -OC(R3)2-, -CR4R4'-; R3 is hydrogen or lower alkyl; R4/R4' are independently from each other hydrogen or lower alkyl; cyc is cycloalkyl or heterocycloalkyl, or is a non-aromatic bicycle selected from 7-oxa- bicyclo[2.2.1]hept-1-yl or bicyclo[2.2.1]hept-1-yl; n is 1, 2 or 3; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
POSITIVE ALLOSTERIC MODULATORS (PAM)
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Page/Page column 20, (2011/05/05)
The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4′, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
