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1.发明申请公开(公告)号：US20100227886A1
公开(公告)日：2010-09-09
申请号：US12759664
申请日：2010-04-13
IPC分类号： A61K31/4468 , A61P25/18
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.
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2.发明申请Selective Serotonin 2A/2C Receptor Inverse Agonists as Therapeutics for Neurodegenerative Diseases 有权选择性5-羟色胺2A / 2C受体反向激动剂作为治疗神经退行性疾病公开(公告)号：US20100227885A1
公开(公告)日：2010-09-09
申请号：US12759662
申请日：2010-04-13
IPC分类号： A61K31/4468 , A61P25/28
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。
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3.发明授权公开(公告)号：US08377959B2
公开(公告)日：2013-02-19
申请号：US13539011
申请日：2012-06-29
IPC分类号： A61K31/47 , A61K31/445
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.
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4.发明授权Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases 有权选择性5-羟色胺2A / 2C受体反向激动剂作为神经变性疾病的治疗剂公开(公告)号：US08227487B2
公开(公告)日：2012-07-24
申请号：US13169893
申请日：2011-06-27
IPC分类号： A61K31/47 , A61K31/445
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。
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5.发明授权Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases 有权选择性5-羟色胺2A / 2C受体反向激动剂作为神经变性疾病的治疗剂公开(公告)号：US07994193B2
公开(公告)日：2011-08-09
申请号：US12759662
申请日：2010-04-13
IPC分类号： A61K31/47 , A61K31/445
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。
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6.发明授权Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases 有权选择性5-羟色胺2A / 2C受体反向激动剂作为神经变性疾病的治疗剂公开(公告)号：US07732462B2
公开(公告)日：2010-06-08
申请号：US11416527
申请日：2006-05-03
IPC分类号： A61K31/47 , A61K31/445
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。
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7.发明授权公开(公告)号：US07659285B2
公开(公告)日：2010-02-09
申请号：US11416855
申请日：2006-05-03
IPC分类号： A61K31/47 , A61K31/445
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.
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8.发明授权公开(公告)号：US08008323B2
公开(公告)日：2011-08-30
申请号：US12759664
申请日：2010-04-13
IPC分类号： A61K31/47 , A61K31/445
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.
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9.发明授权公开(公告)号：US07713995B2
公开(公告)日：2010-05-11
申请号：US11416594
申请日：2006-05-03
申请人： David M. Weiner , Robert E. Davis , Mark R. Brann , Norman Nash , Carl-Magnus A. Andersson , Allan K. Uldam
发明人： David M. Weiner , Robert E. Davis , Mark R. Brann , Norman Nash , Carl-Magnus A. Andersson , Allan K. Uldam
IPC分类号： A61K31/47
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.
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10.发明授权Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases 有权选择性5-羟色胺2A / 2C受体反向激动剂作为神经变性疾病的治疗剂公开(公告)号：US07601740B2
公开(公告)日：2009-10-13
申请号：US10759561
申请日：2004-01-15
IPC分类号： A61K31/47 , A61K31/445 , C07D211/56
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。
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