公开(公告)号：EP2137193A2

公开(公告)日：2009-12-30

申请号：EP08731502.4

申请日：2008-03-06

申请人： Sanofi-Aventis

发明人： CAO, Bin ,  GURUNIAN, Vieroslava ,  KONGSAMUT, Sathapana ,  KOSLEY, Jr., Raymond, W. ,  SHER, Rosy ,  HARTUNG, Ryan E.

IPC分类号： C07D498/04 ,  A61P25/24 ,  A61K31/519 ,  A61P25/06 ,  A61P25/18 ,  A61P29/00

CPC分类号： C07D498/04

摘要： The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.

摘要翻译： 本发明涉及一系列取代的二氢和四氢恶唑啉嘧啶酮，具体地涉及一系列2-取代-2,3-二氢 - 恶唑并[3,2-a]嘧啶-7-酮和2-取代-2,2-二氢吡喃并[ （I）的3,5,6-四氢恶唑并[3,2-a]嘧啶-7-酮：其中p，n，X，Y，R1，R2，R3，R4，R5，R6， R 7和R 8如本文所定义。 本发明还涉及制备这些化合物包括新型中间体的方法。 本发明的化合物是代谢型谷氨酸受体（mGluR），特别是mGluR2受体的调节剂。 因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性神经变性疾病，精神病，惊厥，焦虑， 抑郁，偏头痛，疼痛，睡眠障碍和呕吐。