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1.发明授权Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging 失效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：US06878363B2
公开(公告)日：2005-04-12
申请号：US09859261
申请日：2001-05-17
Applicant: Robert Zaczek , Richard E. Olson , Dietmar A. Seiffert , Lorin A. Thompson
Inventor： Robert Zaczek , Richard E. Olson , Dietmar A. Seiffert , Lorin A. Thompson
CPC classification number: A61K51/0468
Abstract: A method of using radiolabelled and/or radiopharmaceutical small molecule inhibitors of beta-amyloid peptide production for the diagnosis of neurological and other disorders involving APP processing and beta-amyloid production. Radiolabelled small molecule inhibitors identified by the methods of the present invention would be useful in the diagnosis of neurological disorders, such as Alzheimer's disease, which involve elevated levels of Aβ peptides.
Abstract translation: 使用放射性标记和/或放射性药物小分子抑制剂β-淀粉样蛋白肽生产的方法用于诊断涉及APP加工和β-淀粉样蛋白生成的神经和其他疾病。 通过本发明方法鉴定的放射性标记的小分子抑制剂可用于诊断涉及升高水平的Aβ肽的神经障碍，例如阿尔茨海默氏病。
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公开(公告)号：US06495540B2
公开(公告)日：2002-12-17
申请号：US09817957
申请日：2001-03-27
Applicant: Lorin A. Thompson
Inventor： Lorin A. Thompson
IPC: A61K3155
CPC classification number: C07D223/12 , A61K31/55
Abstract: 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 A&bgr;-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 &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
Abstract translation: 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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3.发明授权Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production 有权羟基烷酰氨基内酰胺和相关结构作为Abeta蛋白质生产的抑制剂公开(公告)号：US07112583B2
公开(公告)日：2006-09-26
申请号：US11024377
申请日：2004-12-28
Applicant: Richard E. Olson , Hong Liu , Lorin A. Thompson
Inventor： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC: C07D243/12 , A61K31/55 , A61P25/28
CPC classification number: C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
Abstract: 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.
Abstract translation: 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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Patent Agency Ranking
公开(公告)号：US20080153868A1
公开(公告)日：2008-06-26
申请号：US11951516
申请日：2007-12-06
Applicant: Lorin A. Thompson , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
Inventor： Lorin A. Thompson , Kenneth M. Boy , Jianliang Shi , John E. Macor , Andrew C. Good , Lawrence R. Marcin
IPC: A61K31/437 , C07D217/00 , A61K31/47 , A61P25/00 , A61P25/28 , C07D221/02
CPC classification number: C07K5/06139 , C07D471/04
Abstract: There is provided a series of tetrahydroisoquinoline diaminopropane compounds of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R, R8 and R9 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
Abstract translation: 提供一系列式（I）的四氢异喹啉二氨基丙烷化合物或立体异构体; 或其药学上可接受的盐，其中R 8 R 8和R 9如本文所定义，其药物组合物和使用方法。 这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
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5.发明授权Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production 有权羟基烷酰氨基内酰胺和相关结构作为Abeta蛋白质生产的抑制剂公开(公告)号：US06960576B2
公开(公告)日：2005-11-01
申请号：US10287117
申请日：2002-11-04
Applicant: Richard E. Olson , Hong Liu , Lorin A. Thompson
Inventor： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC: C07D223/18 , C07D243/08 , C07D243/14 , C07D243/24 , C07D401/04 , C07D243/00 , A61K31/55 , C07D223/12 , C07D487/00
CPC classification number: C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
Abstract: 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.
Abstract translation: 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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6.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
Applicant: Richard E. Olson , Hong Liu , Lorin A. Thompson
Inventor： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC: A61K31/55 , C07D223/18 , A61P25/28 , A61P25/00
CPC classification number: C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
Abstract: 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.
Abstract translation: 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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7.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
Applicant: Richard E. Olson , Hong Liu , Lorin A. Thompson
Inventor： Richard E. Olson , Hong Liu , Lorin A. Thompson
IPC: A61K31/55 , C07D243/14 , C07D267/02 , C07D281/02 , A61K31/5513
CPC classification number: C07D223/18 , C07D223/10 , C07D223/12 , C07D223/16 , C07D243/08 , C07D243/14 , C07D243/24 , C07D243/26 , C07D401/04
Abstract: 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.
Abstract translation: 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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8.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
Applicant: Robert Zaczek , Richard E. Olson , Dietmar A. Seiffert , Lorin A. Thompson
Inventor： Robert Zaczek , Richard E. Olson , Dietmar A. Seiffert , Lorin A. Thompson
IPC: A61K4900
CPC classification number: G01N33/6896 , G01N2333/4709 , G01N2500/02 , G01N2500/20 , G01N2800/2821
Abstract: 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.
Abstract translation: 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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