公开(公告)号：US20080269251A1

公开(公告)日：2008-10-30

申请号：US12091181

申请日：2006-12-18

申请人： Jose Ignacio Andre-Gil ,  Manuel Jesus Alcazar-Vaca ,  Maria Lourdes De La Morena ,  Sonio Martinez Gonzalez ,  Julen Oyarzabal Santanarina ,  Joaquin Pastor-Fernandez ,  Juan Antonio Vega Ramiro ,  Wilhelmus Helena Ignatius Maria Drinkenburg

发明人： Jose Ignacio Andre-Gil ,  Manuel Jesus Alcazar-Vaca ,  Maria Lourdes De La Morena ,  Sonio Martinez Gonzalez ,  Julen Oyarzabal Santanarina ,  Joaquin Pastor-Fernandez ,  Juan Antonio Vega Ramiro ,  Wilhelmus Helena Ignatius Maria Drinkenburg

IPC分类号： A61K31/497 ,  C07D403/06 ,  A61P25/24 ,  A61P25/18 ,  A61P25/04 ,  A61P25/28 ,  A61P25/00

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

摘要： The present invention concerns substituted pyrazinone derivatives according to the general Formula (I) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein the variables are defined in Claim 1, having selective α2C-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine. The compounds according to the invention are useful for the prevention and/or treatment of central nervous system disorders, mood disorders, anxiety disorders, stress-related disorders associated with depression and/or anxiety, cognitive disorders, personality disorders, schizoaffective disorders, Parkinson's disease, dementia of the Alzheimer's type, chronic pain conditions, neurodegenerative diseases, addiction disorders, mood disorders and sexual dysfunction.

摘要翻译： 本发明涉及根据通式（I）的取代的吡嗪酮衍生物，其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式或其季铵盐，其中变量定义于 权利要求1，具有选择性α2-2肾上腺素能受体拮抗剂活性。 它还涉及它们的制备，包含它们的组合物及其作为药物的用途。 根据本发明的化合物可用于预防和/或治疗中枢神经系统疾病，情绪障碍，焦虑障碍，与抑郁和/或焦虑相关的压力相关疾病，认知障碍，人格障碍，分裂情感障碍，帕金森病 ，阿尔茨海默病的痴呆，慢性疼痛病症，神经变性疾病，成瘾症，情绪障碍和性功能障碍。