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    • 2. 发明申请
    • BENZODIAZEPINE DERIVATIVES, COMPOSITIONS, AND METHODS FOR TREATING COGNITIVE IMPAIRMENT
    • 苯并噻吩衍生物,组合物和治疗认知障碍的方法
    • WO2016205739A1
    • 2016-12-22
    • PCT/US2016/038224
    • 2016-06-17
    • MEKONNEN, BelewBUTERA, John, A.HUANG, Jianxing
    • MEKONNEN, BelewBUTERA, John, A.HUANG, Jianxing
    • C07D487/14A61K31/5513A61P25/00
    • A61K31/551A61K31/13A61K31/27A61K31/445A61K31/496A61K31/55A61K45/06C07D487/14A61K2300/00
    • This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a α5- containing GABA A receptor agonist ( e.g. , a α5-containing GABA A receptor positive allosteric modulator) as described herein in treating cognitive impairment associated with central nervous system (CNS) disorders in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age- Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer' s Disease(AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson' s disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction.
    • 本发明涉及苯并二氮杂衍生物,包含治疗有效量的那些苯并二氮杂衍生物的组合物和使用这些衍生物或组合物治疗与中枢神经系统(CNS)病症相关的认知障碍的方法。 特别地,本发明涉及在本文所述的含有α5的GABA A受体激动剂(例如,含有α5的GABA A受体阳性变构调节剂)用于治疗有需要的受试者中与中枢神经系统(CNS)紊乱相关的认知障碍 或其风险包括但不限于具有年龄相关认知障碍或轻度认知障碍(MCI),遗忘MCI(aMCI),年龄相关记忆障碍(AAMI),年龄相关认知衰退(ARCD) ),痴呆,阿尔茨海默病(AD),前驱性AD,创伤后应激障碍(PTSD),精神分裂症,双相情感障碍,肌萎缩性侧索硬化(ALS),癌症治疗相关认知障碍,精神发育迟滞,帕金森病 (PD),自闭症谱系障碍,脆性X病症,Rett综合征,强迫行为和物质成瘾。