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1.发明授权Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production 有权使用小分子放射性配体发现淀粉样蛋白-β肽生产的抑制剂公开(公告)号：US06331408B1
公开(公告)日：2001-12-18
申请号：US09438901
申请日：1999-11-12
IPC分类号： C12Q137
CPC分类号： G01N33/6896 , G01N2333/4709 , G01N2500/02 , G01N2500/20 , G01N2800/2821 , Y10S435/968
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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2.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：US07153491B2
公开(公告)日：2006-12-26
申请号：US10734031
申请日：2003-12-11
IPC分类号： A61K49/00
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 Aβ 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：US07304056B2
公开(公告)日：2007-12-04
申请号：US11493156
申请日：2006-07-26
IPC分类号： C07D243/12 , A61K31/55 , A61P25/28
CPC分类号： C07D223/12 , C07D243/24 , C07D401/06 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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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4.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：US07342008B2
公开(公告)日：2008-03-11
申请号：US11522699
申请日：2006-09-18
IPC分类号： C07D243/12 , A61K31/55 , A61P25/28
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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公开(公告)号：US07304055B2
公开(公告)日：2007-12-04
申请号：US11492593
申请日：2006-07-25
IPC分类号： C07D243/24 , A61K31/55 , A61P25/28
CPC分类号： C07D223/12 , C07D243/24 , C07D401/06 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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.
摘要翻译： 本发明涉及具有药物和生物影响性质的新型内酰胺，其药物组合物和使用方法。 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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公开(公告)号：US07101870B2
公开(公告)日：2006-09-05
申请号：US11175644
申请日：2005-07-06
IPC分类号： C07D223/20 , A61K31/55 , A61P25/28
CPC分类号： C07D401/06 , C07D223/12 , C07D243/24 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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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公开(公告)号：US07507815B2
公开(公告)日：2009-03-24
申请号：US11950399
申请日：2007-12-04
IPC分类号： C07D243/24
CPC分类号： C07D401/06 , C07D223/12 , C07D243/24 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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.
摘要翻译： 本发明涉及具有药物和生物影响性质的新型内酰胺，其药物组合物和使用方法。 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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公开(公告)号：US06794381B1
公开(公告)日：2004-09-21
申请号：US09506360
申请日：2000-02-17
IPC分类号： C07D22300
CPC分类号： C07D401/06 , C07D223/12 , C07D243/24 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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 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.
摘要翻译： 本发明涉及具有药物和生物影响性质的新型内酰胺，其药物组合物和使用方法。 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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9.发明申请SUCCINOYLAMINO LACTAMS AS INHIBITORS OF A-BETA PROTEIN PRODUCTION 失效作为A-beta蛋白质生产的抑制剂的SUCCINOYLAMINO LACTAMS公开(公告)号：US20080293692A1
公开(公告)日：2008-11-27
申请号：US11950399
申请日：2007-12-04
IPC分类号： A61K31/55 , C07D223/10 , C07D401/06 , A61P25/00 , A61K31/551 , C07D243/12
CPC分类号： C07D401/06 , C07D223/12 , C07D243/24 , C07D401/10 , C07D405/12
摘要： This invention relates to novel lactams 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.
摘要翻译： 本发明涉及具有药物和生物影响性质的新型内酰胺，其药物组合物和使用方法。 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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10.发明授权Hydroxyalkanoylaminolactams and related structures as inhibitors of aβ protein production 失效羟基烷酰氨基内酰胺和相关结构作为abeta蛋白生产的抑制剂公开(公告)号：US07423033B2
公开(公告)日：2008-09-09
申请号：US12024812
申请日：2008-02-01
IPC分类号： C07D243/24 , A61K31/395
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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