5-(phenyl/pyridine-Etinil) -2-pyridine/2-pyridine-Carboxamida, MGLUR5 modulator; 5-Containing pharmaceutical ingredients; formulation process; compounds for the treatment of schizophrenia or cognitive disorders.
The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2′ are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2′ together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4′ are each independently hydrogen or lower alkyl, or R4 and R4′ together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; 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. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).COMPUESTOS DERIVADOS DE 5-(FENIL/PIRIDINIL-ETINIL)-2-PIRIDINA/2-PIRIMIDINA-CARBOXAMIDA, MODULADORES MGLUR5; COMPOSICIÓN FARMACÉUTICA QUE LOS COMPRENDE; PROCESO DE PREPARACIÓN DE ELLOS; Y SU USO EN EL TRATAMIENTO DE ESQUIZOFRENIA O ENFERMEDADES COGNITIVAS.