[EN] TRIAZOLOPHTHALAZINE / QUINOLINE / ISOQUINOLINE DERIVATIVES WHICH ARE LIGANDS FOR GABA-A RECEPTORS CONTAINING THE ALPHA 5 SUBTYPE<br/>[FR] DERIVES DE TRIAZOLOPHTHALAZINE/QUINOLINE/ISOQUINOLINE QUI SONT DES LIGANDS POUR DES RECEPTEURS GABA-A CONTENANT LE SOUS-TYPE ALPHA 5
申请人:MERCK SHARP & DOHME
公开号:WO2002081474A1
公开(公告)日:2002-10-17
The present invention provides a compound of formula (I): in which R1 is an aromatic or heteroaromatic ring, M is a bond, -CH¿2?-, -O- or -S-, R?2, R3 and R4¿ are as defined herein, and X, Y and Z generally define a 1,2,4-triazolo[3,4-a]phthalazine, 1,2,3-triazolo[1,5-a]quinoline or 1,2,4-triazolo[3,4-a]isoquinoline core, as a ligand for GABA-A receptors containing the alpha 5 subtype and which is preferably an inverse agonist thereat and is thus useful for enhancing cognition in conditions such as Alzheimer's disease, compositions containing it, its use in therapy, use of it for making medicaments and methods of treatment using it.