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公开(公告)号：US07276495B2
公开(公告)日：2007-10-02
申请号：US11005573
申请日：2004-12-06
申请人： Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
发明人： Qi Han , Hong Liu , Richard E. Olson , Michael G. Yang
IPC分类号： C07D487/00 , A61K31/55 , A61P25/28
CPC分类号： C07D401/04 , C07D223/12 , C07D223/18 , C07D243/12 , C07D243/24 , C07D403/02
摘要： This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
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22.发明申请Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs 有权氮杂双环胺氧化物作为α-7烟碱乙酰胆碱受体配体药物公开(公告)号：US20120108596A1
公开(公告)日：2012-05-03
申请号：US13097153
申请日：2011-04-29
申请人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
发明人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
IPC分类号： A61K31/4725 , A61P25/18 , A61P25/28 , A61K31/439 , A61K31/498 , A61K31/506 , A61K31/444 , A61K31/497 , C07D498/20 , C07D519/00
CPC分类号： C07D498/10
摘要： The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是用于烟碱型α7受体的配体，激动剂和部分激动剂的前药，并且可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。
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23.发明申请公开(公告)号：US20100099684A1
公开(公告)日：2010-04-22
申请号：US12607354
申请日：2009-10-28
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/499 , C07D239/12 , C07D241/36 , C07D401/14 , A61K31/498 , A61K31/444 , A61P25/28
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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24.发明申请Novel Alpha-(N-Sulfonamido)Acetamide Compound as an Inhibitor of Beta Amyloid Peptide Production 有权新型α-（N-磺酰氨基）乙酰胺化合物作为β淀粉样蛋白肽生产抑制剂公开(公告)号：US20090111858A1
公开(公告)日：2009-04-30
申请号：US12249180
申请日：2008-10-10
IPC分类号： A61K31/4245 , C07D271/06 , A61P25/28
CPC分类号： C07C311/19 , C07C237/06 , C07C253/30 , C07D271/06 , Y02P20/582 , C07C255/50
摘要： The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.
摘要翻译： 本发明提供了一种新的α-（N-亚磺酰氨基）乙酰胺化合物，其药物组合物，其制备方法和治疗阿尔茨海默病和与β-淀粉样肽相关的其它病症的方法。
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25.发明申请HYDROXYALKANOYLAMINOLACTAMS AND RELATED STRUCTURES AS INHIBITORS OF A BETA PROTEIN PRODUCTION 审中-公开作为蛋白质生产的抑制剂的羟基甘氨酰胺和相关结构公开(公告)号：US20090111793A1
公开(公告)日：2009-04-30
申请号：US12207355
申请日：2008-09-09
申请人： Richard E. Olson , Hong Liu , Lorin A. Thompson
发明人： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC分类号： A61K31/55 , C07D223/18 , A61P25/28 , A61P25/00
CPC分类号： C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
摘要： This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译： 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。
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26.发明申请公开(公告)号：US20080207602A1
公开(公告)日：2008-08-28
申请号：US12061227
申请日：2008-04-02
申请人： Richard E. Olson
发明人： Richard E. Olson
IPC分类号： A61K31/5513 , C07D243/14 , A61P25/00
CPC分类号： C07D223/16 , C07D243/12 , C07D243/14 , C07D243/24 , C07D401/04
摘要： This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译： 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。
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27.发明申请HYDROXYALKANOYLAMINOLACTAMS AND RELATED STRUCTURES AS INHIBITORS OF A BETA PROTEIN PRODUCTION 失效作为蛋白质生产的抑制剂的羟基甘氨酰胺和相关结构公开(公告)号：US20080132482A1
公开(公告)日：2008-06-05
申请号：US12024812
申请日：2008-02-01
申请人： Richard E. Olson , Hong Liu , Lorin A. Thompson
发明人： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC分类号： A61K31/55 , C07D243/14 , C07D267/02 , C07D281/02 , A61K31/5513
CPC分类号： C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
摘要： This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译： 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。
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28.发明授权Lactams substituted by cyclic succinates as inhibitors of Aβ protein production 有权由环状琥珀酸酯取代的内酰胺作为Abeta蛋白质生产的抑制剂公开(公告)号：US07354914B2
公开(公告)日：2008-04-08
申请号：US10998894
申请日：2004-11-29
申请人： Richard E. Olson
发明人： Richard E. Olson
IPC分类号： C07D267/02 , C07D281/02 , C07D291/02 , A61K31/55 , A61P25/28
CPC分类号： C07D223/16 , C07D223/12 , C07D223/18 , C07D243/12 , C07D243/14 , C07D243/24 , C07D243/26
摘要： This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.
摘要翻译： 本发明涉及具有式（I）的新型内酰胺：其药物组合物及其使用方法。 这些新化合物抑制淀粉样蛋白前体蛋白的加工，更具体地，抑制Aβ肽的产生，从而起到防止淀粉样蛋白质神经沉积的形成的作用。 更具体地，本发明涉及治疗与β-淀粉样蛋白产生相关的神经系统疾病，例如阿尔茨海默病和唐氏综合征。
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29.发明授权Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging 有权使用小分子放射性配体发现淀粉样蛋白β肽生产抑制剂和诊断成像公开(公告)号：US06737038B1
公开(公告)日：2004-05-18
申请号：US09573789
申请日：2000-05-17
IPC分类号： A61K4900
CPC分类号： G01N33/6896 , G01N2333/4709 , G01N2500/02 , G01N2500/20 , G01N2800/2821
摘要： This invention relates to a novel method of screening for inhibitors of beta-amyloid production, and thereby identifying such inhibitors as therapeutics for neurological and other disorders involving APP processing and beta-amyloid production. This invention also relates to identifying macromolecules involved in APP processing and beta-amyloid production. Furthermore, inhibitors identified by the screening method of the present invention are useful in the treatment of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A&bgr; peptides.
摘要翻译： 本发明涉及一种筛选β-淀粉样蛋白生成抑制剂的新方法，从而鉴定了诸如涉及APP加工和β-淀粉样蛋白生成的神经学和其它病症治疗剂的抑制剂。 本发明还涉及鉴定参与APP处理和β-淀粉样蛋白生成的大分子。 此外，通过本发明的筛选方法鉴定的抑制剂可用于治疗神经障碍，例如阿尔茨海默氏病，其涉及升高的Aβ肽水平。
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公开(公告)号：US06348504B1
公开(公告)日：2002-02-19
申请号：US09282037
申请日：1999-03-30
IPC分类号： A61K3133
CPC分类号： C07C311/19 , A61K31/18 , A61K31/195 , C07C257/18 , C07C271/22
摘要： This invention relates generally to oxime ethers which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
摘要翻译： 本发明一般涉及可用作血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂的肟醚，含有这些化合物的药物组合物，制备这些化合物的方法，以及使用这些化合物抑制血小板聚集的方法， 作为血栓溶解剂，和/或用于治疗血栓栓塞障碍。
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