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1.发明申请Methods for preventing and treating obesity in patients with mc4 receptor mutations 审中-公开mc4受体突变患者预防和治疗肥胖的方法公开(公告)号：US20060183789A1
公开(公告)日：2006-08-17
申请号：US10527675
申请日：2003-09-23
IPC分类号： C12Q1/68 , A61K31/405
CPC分类号： C12Q1/6883 , A61K31/00 , A61K45/06 , C12Q2600/156
摘要： Methods are provided for treating health conditions associated with altered MC4 receptor activity with melanin concentrating hormone receptor antagonists. Such compounds may be used, for example, to treat or prevent obesity and/or overeating, and to reduce body mass index, in patients carrying one or more MC4 receptor mutations.
摘要翻译： 提供了用于治疗与由黑色素浓缩激素受体拮抗剂改变的MC4受体活性相关的健康状况的方法。 在携带一种或多种MC4受体突变的患者中，这样的化合物可用于例如治疗或预防肥胖和/或暴饮暴食并降低体重指数。
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2.发明授权Methods for screening GABA-modulatory compounds for specified pharmacological activities 失效筛选用于规定药理活性的GABA调节化合物的方法公开(公告)号：US06737242B1
公开(公告)日：2004-05-18
申请号：US09565524
申请日：2000-05-05
申请人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： G01N33567
CPC分类号： G01N33/9426 , G01N2333/70571 , G01N2500/00
摘要： Methods are provided that are useful in assaying compounds for cognitive enhancing properties, anxiolytic properties, hypnotic properties, or antidepressant properties. These methods involve determining the in vitro efficacy and EC50 of the compounds at defined series of cloned GABAA subtype receptors composed of specific variants of &agr;,&bgr;, and &ggr; subunits in order to develop and an activity profile for each compound. Optionally, the binding affinities of the compounds at GABAA receptors are also determined. As an additional step the in vivo effects of the compounds may be tested in animal models.
摘要翻译： 提供了可用于测定化合物的认知增强性质，抗焦虑性质，催眠性质或抗抑郁药性质的方法。 这些方法涉及确定化合物在由α，β和γ亚基的特异性变体组成的克隆的GABAA亚型受体的体外功效和EC 50，以便开发每种化合物的活性谱。 任选地，还测定了化合物在GABA A受体上的结合亲和力。 作为附加步骤，可以在动物模型中测试化合物的体内作用。
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公开(公告)号：US20080044353A1
公开(公告)日：2008-02-21
申请号：US11547292
申请日：2005-03-28
IPC分类号： A61K31/496 , A61P1/00 , G01N33/15
CPC分类号： A61K45/06 , A61K31/454 , A61K31/5377 , A61K2300/00
摘要： Compositions and methods are provided for weight management. The compositions generally comprise a MCHR antagonist, either in combination with a CB1 antagonist or formulated for coadministration with a CB1 antagonist. Certain methods involve coadministering a MCHR antagonist and a CB1 antagonist to a patient.
摘要翻译： 提供组合和方法用于体重管理。 组合物通常包含MCHR拮抗剂，与CB1拮抗剂组合或配制用于与CB1拮抗剂共同给药。 某些方法涉及向患者共同施用MCHR拮抗剂和CB1拮抗剂。
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4.发明申请Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders 审中-公开组合使用乙酰胆碱酯酶抑制剂和GABAa反向激动剂治疗认知障碍公开(公告)号：US20050009861A1
公开(公告)日：2005-01-13
申请号：US10912993
申请日：2004-08-06
IPC分类号： A61K31/13 , A61K31/195 , A61K31/4375 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/55 , A61K31/66 , A61K45/06 , A61P9/10 , A61P17/02 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61K31/4745
CPC分类号： A61K31/55 , A61K31/00 , A61K31/13 , A61K31/195 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/66 , A61K45/06 , A61K31/435 , A61K31/40 , A61K31/27 , A61K31/125 , A61K2300/00
摘要： This invention provides a composition for treating a cognitive disorder, which comprises an acetylcholinesterase inhibitor, and a GABAA inverse agonist selected from a compound of the formula where X and Y are as defined herein.
摘要翻译： 本发明提供用于治疗认知障碍的组合物，其包含乙酰胆碱酯酶抑制剂和选自下式的化合物的GABA A反向激动剂，其中X和Y如本文所定义。
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5.发明授权Methods for screening GABA-modulatory compounds for specified pharmacological activities 失效筛选用于规定药理活性的GABA调节化合物的方法公开(公告)号：US07060451B2
公开(公告)日：2006-06-13
申请号：US10045396
申请日：2001-11-09
申请人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： G01N33/567 , C07K1/00 , C07H21/04 , C12N1/20 , C12P21/02
CPC分类号： G01N33/9426 , G01N2333/70571 , G01N2500/00
摘要： Methods are provided that are useful in assaying compounds for cognitive enhancing properties, anxiolytic properties, hypnotic properties, or antidepressant properties. These methods involve determining the in vitro efficacy and EC50 of the compounds at defined series of cloned GABAA subtype receptors composed of specific variants of α, β, and γ subunits in order to develop and an activity profile for each compound. Optionally, the binding affinities of the compounds at GABAA receptors are also determined. As an additional step the in vivo effects of the compounds may be tested in animal models.
摘要翻译： 提供了可用于测定化合物的认知增强性质，抗焦虑性质，催眠性质或抗抑郁药性质的方法。 这些方法包括确定在由α，β和γ亚基的特异性变体组成的限定的克隆的GABA亚型亚型受体系列中的化合物的体外功效和EC 50 为每个化合物开发和活动资料。 任选地，还测定了化合物在GABA A A受体上的结合亲和力。 作为附加步骤，可以在动物模型中测试化合物的体内作用。
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