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公开(公告)号：US07288523B2
公开(公告)日：2007-10-30
申请号：US10721774
申请日：2003-11-26
IPC分类号： A61K38/08
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0808 , C07K5/0815 , C07K5/0819 , C07K5/101 , C07K5/1019 , C07K5/1021 , C07K5/1024 , C07K14/4711 , G01N33/6896 , G01N2800/2821
摘要： The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid β peptide, as model substances for synthesis of amyloid β peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1-A′-Y′-Leu-X′-Z′-B′-R2 in which X′ means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid β peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Y′ means any amino acid; Z′ means any non-acidic amino acid; A′ means a direct bond or an α-amino acid bonded at the carboxyl terminal of the α-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the α-carboxy group; B′ means a direct bond or an α-amino acid bonded at the α-nitrogen or a di-, tri, tetra- or pentapeptide bonded at the α-nitrogen of the N-terminal α-amino acid; R1 is H or —CO—R3 bonded at the α-amino group of A′; R2 is H, —OR4 or NR5R6, all bonded to the α-carboxyl group of the α-carboxyterminal of B′; R3 and R4 are straight or branched carbon chain of 1-4 carbon atoms; R5 and R6 are independently H, alkyl, cycloalyl, aryl or substituted aryl or together are —(CH2)n— where n is 4-5; and R1 and R2 together can form a hydrocarbon ring or heterocyclic ring; all α-amino acids being either D- or L-isomers.
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公开(公告)号：US06331440B1
公开(公告)日：2001-12-18
申请号：US09095106
申请日：1998-06-10
IPC分类号： G01N33566
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0808 , C07K5/0815 , C07K5/0819 , C07K5/101 , C07K5/1019 , C07K5/1021 , C07K5/1024 , C07K14/4711 , G01N33/6896 , G01N2800/2821
摘要： The invention relates to compounds of formula (I) or (II), which are of interest especially for inhibition of polymerization of amyloid &bgr; peptide, as model substances for synthesis of amyloid &bgr; peptide-ligands, as tools for the identification of other organic compounds with similar functional properties and/or as ligands for detection of amyloid deposits using e.g., positron emission tomography (PET). Formula (II) is: R1—A′—Y′—Leu—X′—Z′—B′—R2 in which X′ means any group or amino acid imparting to the compound according to formula (I) the ability to bind to the KLVFF-sequence in amyloid &bgr; peptide, or two amino acids imparting the same ability, but with the proviso that one is not proline; Y′ means any amino acid; Z′ means any non-acidic amino acid; A′ means a direct bond or an &agr;-amino acid bonded at the carboxyl terminal of the &agr;-carboxy group or a di-, tri-, tetra- or pentapeptide bonded at the carboxyl terminal of the &agr;-carboxy group; B′ means a direct bond or an &agr;-amino acid bonded at the &agr;-nitrogen or a di-, tri-, tetra- or pentapeptide bonded at the &agr;-nitrogen of the N-terminal &agr;-amino acid; R1 is H or —CO—R3 bonded at the &agr;-amino group of A′; R2 is H, —OR4 or NR5R6, all bonded to the &agr;-carboxyl group of the &agr;-carboxyterminal of B′; R3 and R4 are straight or branched carbon chain of 1-4 carbon atoms; R5 and R6 are independently H, alkyl, cycloalkyl, aryl or substituted aryl or together are —(CH2)n— where n is 4-5; and R1 and R2 together can form a hydrocarbon ring of heterocyclic ring; all &agr;-amino acids being either D- or L-isomers.
摘要翻译： 本发明涉及式（I）或（II）的化合物，其特别用于抑制淀粉样蛋白β肽的聚合作为淀粉样蛋白β肽配体的合成的模型物质，作为鉴定其它有机化合物的工具 具有类似的功能性质和/或用于使用例如正电子发射断层摄影（PET）检测淀粉样蛋白沉积物的配体。 式（II）是：R1-A'-Y'-Leu-X'-Z'-B'-R2，其中X'表示赋予根据式（I）的化合物的任何基团或氨基酸， 到淀粉样蛋白β肽中的KLVFF序列或赋予相同能力的两个氨基酸，但条件是一个不是脯氨酸; Y'表示任何氨基酸; Z'表示任何非酸性氨基酸; A'是指在α-羧基的羧基末端键合的直接键或α-氨基酸，或在α-羧基的羧基末端键合的二，三，四或五肽; B'是指在α-氮键合键或在N-末端α-氨基酸的α-氮键合的二 - ，三 - ，四 - 或五肽的直接键或α-氨基酸; R1是在A'的α-氨基键合的H或-CO-R3; R2是H，-OR4或NR5R6，均与B'的α-羧基末端的α-羧基键合; R3和R4是1-4个碳原子的直链或支链碳链; R 5和R 6独立地为H，烷基，环烷基，芳基或取代的芳基，或一起为 - （CH 2）n - ，其中n为4-5; R1和R2一起可以形成杂环的烃环; 所有α-氨基酸都是D-或L-异构体。
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公开(公告)号：US20130280732A1
公开(公告)日：2013-10-24
申请号：US13997854
申请日：2011-12-28
IPC分类号： G01N33/68
CPC分类号： G01N33/6896 , C07K16/18 , G01N2800/2821
摘要： The present invention provides an agent for determining Alzheimer's disease, comprising an anti-S38AA antibody, a method of determining Alzheimer's disease in a test animal, comprising detecting an S38AA fragment in a sample collected from said animal, and a method of screening for a substance that treats or prevents Alzheimer's disease, comprising contacting a test substance with a cell permitting measurement of production of a S38AA fragment, measuring the production amount of the S38AA fragment in the cell, and comparing the production amount with that of the S38AA fragment in a control cell free of contact with the test substance, and selecting a test substance that down-regulates the production amount of the S38AA fragment as a substance capable of treating or preventing Alzheimer's disease, based on the comparison results.
摘要翻译： 本发明提供了一种用于测定阿尔茨海默病的药剂，其包含抗S38AA抗体，测试动物中测定阿尔茨海默病的方法，包括检测从所述动物收集的样品中的S38AA片段，以及筛选物质的方法 治疗或预防阿尔茨海默病，包括使测试物质与允许测量S38AA片段生产的细胞接触，测量细胞中S38AA片段的产生量，并将生产量与对照组中的S38AA片段的产量进行比较 基于比较结果，选择与测试物质接触的细胞，并且根据比较结果选择下调S38AA片段的产生量的测试物质作为能够治疗或预防阿尔茨海默氏病的物质。
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公开(公告)号：US10393757B2
公开(公告)日：2019-08-27
申请号：US13997854
申请日：2011-12-28
IPC分类号： G01N33/53 , G01N33/566 , A01N37/18 , G01N33/68 , C07K16/18
摘要： The present invention provides an agent for determining Alzheimer's disease, comprising an anti-S38AA antibody, a method of determining Alzheimer's disease in a test animal, comprising detecting an S38AA fragment in a sample collected from said animal, and a method of screening for a substance that treats or prevents Alzheimer's disease, comprising contacting a test substance with a cell permitting measurement of production of a S38AA fragment, measuring the production amount of the S38AA fragment in the cell, and comparing the production amount with that of the S38AA fragment in a control cell free of contact with the test substance, and selecting a test substance that down-regulates the production amount of the S38AA fragment as a substance capable of treating or preventing Alzheimer's disease, based on the comparison results.
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