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81.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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82.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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83.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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84.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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85.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：US07863296B2
公开(公告)日：2011-01-04
申请号：US11134769
申请日：2005-05-20
申请人： David M. Weiner , Robert E. Davis , Mark R. Brann , Anna-Maria Frost-Jensen, legal representative , Norman Nash
发明人： David M. Weiner , Robert E. Davis , Mark R. Brann , Norman Nash
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-insomnia agent. Disclosed herein are also methods of treating insomnia 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失眠剂的药物组合物。 本文公开的也是使用所公开的药物组合物治疗失眠的方法。
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86.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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87.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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88.发明申请Apparatus and method to transfer data from a tire pressure monitor tool to a remote output device such as a printer 有权将数据从轮胎压力监测工具传送到诸如打印机的远程输出装置的装置和方法公开(公告)号：US20080164988A1
公开(公告)日：2008-07-10
申请号：US11650513
申请日：2007-01-08
IPC分类号： B60C23/02
CPC分类号： B60C23/0408 , B60C23/0479
摘要： A tire pressure monitoring tool transmits a triggering signal to a tire sensor; receives a reporting signal from the tire sensor; extracts data from the reporting signal; stores the extracted data; and transmits the stored data to an external device. The transmitted stored data is in a predetermined order, and in a text format.
摘要翻译： 轮胎压力监测工具将触发信号传送到轮胎传感器; 从轮胎传感器接收报告信号; 从报告信号中提取数据; 存储提取的数据; 并将存储的数据发送到外部设备。 所发送的存储数据是以预定的顺序和文本格式。
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89.发明授权公开(公告)号：US06664793B1
公开(公告)日：2003-12-16
申请号：US10087281
申请日：2002-03-01
申请人： Allen R. Sampson , Robert E. Davis
发明人： Allen R. Sampson , Robert E. Davis
IPC分类号： G01N2702
CPC分类号： G01N27/221 , G01N27/228
摘要： An apparatus and method for obtaining a measurement of various qualities of an electrochemical cell. The apparatus includes first and second electrodes and an excitation source for providing a time varying excitation voltage to the first electrode. The excitation voltage is switched between two voltage levels with the first and second voltages alternately applied to the first electrode for predetermined times. An external capacitance is connected between the second electrode and ground. The apparatus is capable of determining the time related rates at which electrical charge is transferred from the first electrode to charge the external capacitance. These rates, here termed Transient Immitivity Response (TIR), may be provided as a digital or analog output.
摘要翻译： 一种用于获得电化学电池的各种质量的测量的装置和方法。 该装置包括第一和第二电极以及用于向第一电极提供时变激励电压的激励源。 激励电压在两个电压电平之间切换，其中第一和第二电压交替施加到第一电极预定次数。 外部电容连接在第二电极和地之间。 该装置能够确定从第一电极传送电荷以对外部电容充电的时间相关速率。 这些速率，这里称为瞬态映射反应（TIR），可以作为数字或模拟输出。
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公开(公告)号：US06544745B2
公开(公告)日：2003-04-08
申请号：US09893055
申请日：2001-06-27
IPC分类号： C12P1934
CPC分类号： C07D219/08 , A61K38/00 , C07K14/4711 , C07K14/4713 , C12N9/0053 , C12Q1/6806 , C12Q1/6883 , C12Q2600/156 , C12Q2527/101
摘要： The present invention relates to genetic mutations in mitochondrial genes that segregate with diabetes mellitus. The invention provides methods for detecting such mutations, as a diagnostic for diabetes mellitus, either before or after the onset of clinical symptoms. Examples of specific mutations in the ATP synthase 8/6 sequence and tRNALys sequence are given. The invention also provides treatments for dysfunctions due to genes for mitochondrial functions that segregate with diabetes mellitus. Cybrid cell lines are described which are useful as model systems for the study of the mitochondrial metabolic disorders that are associated with diabetes mellitus, and for identifying therapeutic compounds and treatments for this disease.
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