申请人:CoCensys, Inc.
公开号:US05891871A1
公开(公告)日:1999-04-06
The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers. The invention also is directed to the process for the preparation of the substituted 2,3-benzodiazepin-4-ones.
本发明涉及取代的2,3-苯二氮平-4-酮,其为AMPA受体的拮抗剂或正向调节剂,并且用于治疗、预防或改善与中风、全局和局部缺血、中枢神经系统创伤、低血糖和手术相关的神经元丧失,以及治疗或改善包括阿尔茨海默病、肌萎缩侧索硬化症、亨廷顿病、帕金森病和唐氏综合症在内的神经退行性疾病,治疗、预防或改善兴奋性氨基酸过度刺激的不良后果,治疗或改善焦虑、精神病、惊厥、慢性疼痛、青光眼、巨细胞病毒性视网膜炎、尿失禁、肌肉痉挛和诱导麻醉,以及用于治疗或改善兴奋性氨基酸缺乏的不良后果,如精神分裂症、阿尔茨海默病和营养不良和神经发育不良,以及作为认知增强剂。本发明还涉及制备取代的2,3-苯二氮平-4-酮的方法。