CAO, BIN,曹斌,GURUNIAN, VIEROSLVA,葛伦尼,葛倫尼,KONGSAMUT, SATHAPANA,孔萨姆,孔薩姆,KOSLEY, JR., RAYMOND W.,柯斯莱,柯斯萊,SHER, ROSY,薛罗斯,薛羅斯,HARTUNG, RYAN E.,哈莱恩,哈萊恩
申请号：
TW097107968
公开号：
TWI417296B
申请日:
2008.03.07
申请国别(地区):
TW
年份:
2013
代理人:
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, R7and R8are 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.本發明關於一系列經取代的二氫及四氫唑并嘧啶酮類，明確地說，係關於具式(I)之一系列的2－經取代的－2,3－二氫－唑并[3,2－a]嘧啶－7－酮類及2－經取代的－2,3,5,6－四氫－唑并[3,2－a]嘧啶－7－酮類：其中p、n、X、Y、R1、R2、R3、R4、R5、R6、R7及R8具有在此被定義之含義；本發明也關於製備這些化合物以及新穎中間物之方法，本發明的化合物為代謝性穀胺酸受體類(metabotropic glutamate receptors，mGluR)，特別是mGluR2受體之調節物，因此，本發明的化合物可作為有用的藥劑，尤其是用於治療及/或預防各種的中樞神經系統(CNS)疾病類，包括，但不限於急性及慢性之神經退化症、精神病、抽搐、焦慮、憂鬱、偏頭痛、疼痛、睡眠障礙及嘔吐。
