3 - cyano - 4 - (piridiniloxi - phenyl) - pyridin - 2 - One Derivatives, a preparation method thereof, which includes a Pharmaceutical Composition and its use in preparation of a Medicament for the treatment of a disease mediated by a positive allosteric Modulator or by an agonist ortosterico MGL

摘要

Compounds, in particular, pyridinone derivatives including any of its forms estereoquu00edmicamente isomeras, or a Salt or a solvate acceptable for pharmaceutical use of these compounds.These compounds are alostu00e9ricospositivos modulators of metabotropic glutamate receptor subtype 2 (u00f4mglur2u00f6) useful for the Treatment or prevention of Neurological and Psychiatric Disorders associated with glutamate dysfunction and diseases in which participates elsubtipo m GluR2 of metabotropic receptors.In particular, these diseases are disorders of the central nervous system selected from the group of anxiety, Schizophrenia, migrana, depression, and Epilepsy.Also provided are composicionesfarmacu00e9uticas and a process for the preparation of said compounds and to the use of these compounds in the preparation of a Medicament for the Prevention and Treatment of such diseases in which participamglur2.Claim 1: a compound of the formula (1), including any of its forms estereoquu00edmicamente isomeras, where R1 is alkyl or alkyl of C1 - C4 - 6 3 substituted cycloalkyl C3 - 7; R2 is Hydrogen or Halo is piridinilosustituido; with one or two substituents.Where each Substituent is selected independently of Halo or c1-4 alkyl; n is an integer value 1 or 2; or an acceptable Salt or a solvate of the compound for pharmaceutical use, IF R2 is provided; 2 - fluoride, then is not 3 - pyridinyl substituted with one or two substituents. Where each Substituent is selected independently or c1-4 alkyl, Halo.Claim 37: a process for the preparation of a Compuestocomo claimed in claim 1, characterized by the reaction of an intermediate of formula (2), where y represents a group suitable for PD mediated coupling with boronic acids or boronic esters, with a Intermediary of formula (3), where R3 and R4 represents Hydrogen or alkyl of C1 - 4Or where R3 and R4 can be taken together to form the ch2ch2 Bivalent radical of Formula - - - ch2ch2ch2 - or - C (CH3) 2C (CH3) 2 - in an appropriate Solvent Inert to the Reaction, the presence of a suitable base and a suitable catalyst in thermal conditions, where R1, R2 a and N are defined as in L To claim 1; or, if desired,The additional conversion of the compounds of formula (1) together, siguiendotransformaciones known in the Art, and also, if desired, the conversion of the compounds of formula (1) in an Acid Addition Salt of non-toxic therapeutically Active, by Treatment with an Acid Laconversion; or, Conversely, the way of adding acid salt in the base Open,By Treatment with Alkali; or, if desired, the preparation of their estereoquu00edmicamente isomeras forms.