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.

公开(公告)号：US20110257229A1

公开(公告)日：2011-10-20

申请号：US13169893

申请日：2011-06-27

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

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

IPC分类号： A61K31/4468 ,  A61P25/18 ,  A61K31/4515

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.

摘要翻译： 与式（I）化合物（一种新型和选择性的5HT2A / 2C受体反向激动剂）的行为药理学数据证明了在精神病和运动障碍模型中的体内功效。 这包括逆转MK-801诱导的运动行为的活动，表明该化合物可能是MPTP灵长类运动障碍模型中有效的抗精神病药和活性，表明作为抗运动障碍剂的功效。 这些数据支持5HT2A / 2C受体反向激动作用可能赋予人类抗精神病和抗运动障碍功效的假说，并表明使用式（I）化合物和相关药物作为帕金森病，相关人类神经变性疾病的新疗法， 和精神病。