公开(公告)号：US20130137727A1

公开(公告)日：2013-05-30

申请号：US13750778

申请日：2013-01-25

申请人： David M. WEINER ,  Robert E. DAVIS ,  Mark R. BRANN ,  Carl-Magnus A. ANDERSSON ,  Allan K. ULDAN

发明人： David M. WEINER ,  Robert E. DAVIS ,  Mark R. BRANN ,  Carl-Magnus A. ANDERSSON ,  Allan K. ULDAN

IPC分类号： A61K31/4468 ,  A61K45/06

CPC分类号： A61K31/4468 ,  A61K9/20 ,  A61K31/194 ,  A61K45/06 ,  C07C59/255 ,  C07D211/58 ,  A61K2300/00

摘要： Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.