发明名称 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
摘要 The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). 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.
申请公布号 US2016115169(A1) 申请公布日期 2016.04.28
申请号 US201414896230 申请日期 2014.06.03
申请人 JANSSEN PHARMACEUTICA NV 发明人 Alonso-de Diego Sergio-Alvar;Cid-Núñez José Maria;Delgado-González Óscar;Decorte Annelies Marie Antonius;Van Gool Michiel Luc Maria;MacDonald Gregor James;Megens Antonius Adrianus Hendrikus Petrus;Trabanco-Suárez Andrés Avelino;García-Molina Arénzazu;Andrés-Gil José Ignacio
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of Formula (I) or a stereoisomeric form thereof, wherein R1 is phenyl or 2-pyridinyl, each optionally substituted with one or more substituents each independently selected from the group of halo, C1-4alkyl, mono- or poly-haloC1-4alkyl, —O—C1-4alkyl, —C1-4alkyl-O—C1-4alkyl, mono- or poly-haloC1-4alkyloxy, —C1-4alkyl-OH, C1-4alkylthio, mono- or poly-haloC1-4alkylthio, cyano, C3-7cycloalkyl optionally substituted with trifluoromethyl, and —SF5; or is R2 is selected from wherein R5 and R6 are each independently selected from the group of hydrogen, halo, cyano, C1-4alkyl, —C1-4alkyl-OH, C3-7cycloalkyl, mono- or poly-haloC1-4alkyl, —C1-4alkyl-O—C1-4alkyl, —O—C1-4alkyl, mono- or poly-haloC1-4alkyloxy, 1-acetylazetidin-3-yl, and NR′R″; wherein R′ is selected from hydrogen and C1-4alkyl; R″ is selected from hydrogen and C1-4alkyl; or R′ and R″ together with the Nitrogen atom to which they are attached form a heterocyclic group selected from the group of 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, and 4-morpholinyl; wherein each of the heterocyclic groups may be optionally substituted with a substituent selected from halo, hydroxyl, C1-4alkyl, mono- or poly-haloC1-4alkyl, and —(CO)C1-4alkyl; R3 is selected from hydrogen and C1-4alkyl; R4 is selected from the group of hydrogen, C1-4alkyl, mono- or poly-haloC1-4alkyl, —C1-4alkyl-O—C1-4alkyl, and —C1-4alkyl-OH; or a N-oxide, or a pharmaceutically acceptable salt or a solvate thereof.
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