ETHYNYL COMPOUNDS

摘要

The present invention relates to ethynyl derivatives of formula I;;X, O, R1, R2, R3, R3′, R4, R4′, R5, R6, R6′, m, and n are as defined hereinor 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 can be used for the treatment of schizophrenia or cognitive disorders.

主权项

1. A compound of formulawherein
X is N or C—R, wherein R is hydrogen or halogen; is N or CH;
with the proviso that only one of G or X is nitrogen; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen; R2 is hydrogen, lower alkyl, hydroxy, lower alkoxy or C(O)O-benzyl; R3,R3′, R4, R4′, R6, and R6′ are each independently hydrogen or lower alkyl;
or R6 and R4 together with the carbon atom to which they are attached form a C4-6-cycloalkyl ring, when m is 0 and n is 1 or 2; R5 is hydrogen or lower alkyl; n is 0, 1 or 2; and m is 0 or 1; with the proviso that n and m are not simultaneously 0; or a pharmaceutically acceptable acid addition salt, a racemic mixture, its corresponding enantiomer, optical isomer, or stereoisomer thereof.