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1.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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2.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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3.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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4.发明授权Clinical indications for genotyping polymorphic variants of G-protein coupled receptors 有权G蛋白偶联受体基因分型多态性变体的临床适应症公开(公告)号：US07348140B1
公开(公告)日：2008-03-25
申请号：US10206858
申请日：2002-07-25
申请人： David M. Weiner , Mark R. Brann , Ethan S. Burstein , Jakob L. Hansen , Fabrice Piu , Andria Lee
发明人： David M. Weiner , Mark R. Brann , Ethan S. Burstein , Jakob L. Hansen , Fabrice Piu , Andria Lee
CPC分类号： C12Q1/6883 , C12Q2600/106 , C12Q2600/156 , G01N33/94 , Y10T436/143333
摘要： The invention provides compositions and methods for screening individuals for the presence of G-protein coupled receptor (GPCR) variants. The compositions and methods are useful for determining clinical outcome of drug therapy or for tailoring drug therapy for the individual based upon the presence or absence of one or more GPCR variants in the subject.
摘要翻译： 本发明提供用于筛选个体存在G蛋白偶联受体（GPCR）变体的组合物和方法。 基于受试者中一种或多种GPCR变体的存在或不存在，组合物和方法可用于确定药物治疗的临床结果或为个体定制药物治疗。
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5.发明申请公开(公告)号：US20130137727A1
公开(公告)日：2013-05-30
申请号：US13750778
申请日：2013-01-25
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.
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6.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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7.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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8.发明申请SELECTIVE SEROTONIN 2A/2C RECEPTOR INVERSE AGONISTS AS THERAPEUTICS FOR NEURODEGENERATIVE DISEASES 有权选择性丝氨酸蛋白酶2A / 2C受体反转激动剂作为神经病变性疾病的治疗剂公开(公告)号：US20110257229A1
公开(公告)日：2011-10-20
申请号：US13169893
申请日：2011-06-27
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。
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9.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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10.发明授权Selective serotonin receptor inverse agonists as therapeutics for disease 有权选择性5-羟色胺受体反向激动剂作为疾病的治疗剂公开(公告)号：US07875632B2
公开(公告)日：2011-01-25
申请号：US12378385
申请日：2009-02-11
申请人： David M. Weiner , Robert E. Davis , Mark R. Brann
发明人： David M. Weiner , Robert E. Davis , Mark R. Brann
IPC分类号： A61K31/445 , A61P25/00
CPC分类号： A61K31/138 , A61K9/0019 , A61K31/445 , A61K31/4468 , A61K45/06 , A61K2300/00
摘要： Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions.
摘要翻译： 本文公开了包含反式5-羟色胺受体激动剂或5-羟色胺受体拮抗剂和抗精神病药物的药物组合物。 本文公开的是使用所公开的药物组合物治疗精神病的方法。
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