On December 11, 2014, Van Gool, Michiel Luc Maria; Alonso-De Diego, Sergio-Alvar; Cid-Nunez, Jose Maria; Delgado-Gonzalez, Oscar; Decorte, Annelies Marie Antonius; Macdonald, Gregor James; Megens, Antonius Adrianus Hendrikus Petrus; Trabanco-Suarez, Andres Avelino; Garcia-Molina, Aranzazu; Andres-Gil, Jose Ignacio published a patent.Category: pyridine-derivatives The title of the patent was Preparation of 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mGluR2 receptors. And the patent contained the following:
Title compounds I [R1 = substituted Ph or 2-pyridinyl; R2 = substituted pyridinyl; R3 = H or alkyl; R4 = H, alkyl, mono- or polyhalo-alkyl, alkyl-O-alkyl or alkyl-OH], or a N-oxide, or a pharmaceutically acceptable salt or a solvate, are prepared as neg. allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (mGluR2). Thus, e.g., II was prepared by reaction of (7S)-methyl-3-(2-methylpyridin-4-yl)-6,7-dihydro-5H-pyrazolo[1,5-a]pyrazin-4-one with 4-bromobenzotrifluoride. Compound II showed pIC50 value of 8.05 against hmGluR2 in GTPγS binding assay. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders. The experimental process involved the reaction of 4-Bromo-2-isopropylpyridine(cas: 908267-63-0).Category: pyridine-derivatives
The Article related to dihydropyrazolopyrazine preparation neg allosteric mglur2 receptors cns disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyridine-derivatives