Anticonvulsant and central nervous system-depressing bis (fluorophenyl) alkylamides and their uses
申请人:NPS Pharmaceuticals, Inc.
公开号:US20030199589A1
公开(公告)日:2003-10-23
Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacologic half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.
已经合成了具有有益药理特性(例如,抗惊厥活性)的双(氟苯基)烷基酰胺类化合物,可用于治疗神经系统疾病或障碍,例如癫痫、抽搐和癫痫性疾病。本发明的优选化合物还会引起较少的镇静作用,并在癫痫动物模型中具有高的治疗和保护指数。这些化合物还具有长的药理学半衰期,在实际的临床治疗应用中,应该可以转化为一天一次的剂量,对于患有这些疾病和/或障碍的患者非常有益。这些化合物还可能在治疗中枢和外周神经系统的其他疾病和障碍,或受其影响的疾病和障碍方面具有进一步的临床实用性,包括但不限于痉挛、骨骼肌痉挛和疼痛、不宁腿综合症、焦虑和压力以及双相障碍。