公开(公告)号：US20100029620A1

公开(公告)日：2010-02-04

申请号：US11722380

申请日：2005-12-20

申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Joaquin Pastor-Fernández ,  Xavier Jean,Michel Langlois ,  Julen Oyarzabal-Santamarina ,  Juan Antonio Vega-Ramiro

发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Joaquin Pastor-Fernández ,  Xavier Jean,Michel Langlois ,  Julen Oyarzabal-Santamarina ,  Juan Antonio Vega-Ramiro

IPC分类号： A61K31/496 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/10 ,  C07D401/04 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/551 ,  A61P25/22 ,  A61P25/24 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16

CPC分类号： C07D257/04 ,  C07D233/70 ,  C07D249/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/14

摘要： The present invention concerns substituted triazolone, tetrazolone and imidazolone 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的取代的三唑酮，四唑酮和咪唑啉酮衍生物，其中 变量在权利要求1中定义，具有选择性α2C-肾上腺素受体拮抗剂活性。 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。

公开(公告)号：US20100105694A1

公开(公告)日：2010-04-29

申请号：US12445243

申请日：2007-10-10

申请人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernández ,  Juan Antonio Vega-Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

发明人： José Ignacio Andrés-Gil ,  Manuel Jesús Alcázar-Vaca ,  Maria Lourdes Linares De La Morena ,  Sonia Martinez Gonzalez ,  Julen Oyarzabal Santamarina ,  Joaquin Pastor-Fernández ,  Juan Antonio Vega-Ramiro ,  Francisca Delgado-Jiménez ,  Wilhelmus Helena Ignatius Maria Drinkenburg

IPC分类号： A61K31/497 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  A61P25/00 ,  A61P25/28

CPC分类号： C07D401/12 ,  C07D241/20

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 2C-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，具有选择性的2C-肾上腺素受体拮抗剂活性。 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。