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1. 发明授权

US07803774B2 Modulators of β-amyloid peptide aggregation 失效
标题翻译： β-淀粉样肽聚集的调节剂
公开(公告)号：US07803774B2
公开(公告)日：2010-09-28
申请号：US10989763
申请日：2004-11-15
申请人： Mark A. Findeis , Kathryn Phillips , Gary L. Olsen , Christopher Self
发明人： Mark A. Findeis , Kathryn Phillips , Gary L. Olsen , Christopher Self
IPC分类号： A61K38/00 , A61K49/00
CPC分类号： C07K14/4711 , A61K38/00
摘要： Compounds that modulate natural β amyloid peptide aggregation are provided. The modulators of the invention comprise a peptide, preferably based on a β amyloid peptide, that is comprised entirely of D-amino acids. Preferably, the peptide comprises 3-5 D-amino acid residues and includes at least two D-amino acid residues independently selected from the group consisting of D-leucine, D-phenylalanine and D-valine. In a particularly preferred embodiment, the peptide is a retro-inverso isomer of a β amyloid peptide, preferably a retro-inverso isomer of Aβ17-21. In certain embodiments, the peptide is modified at the amino-terminus, the carboxy-terminus, or both. Preferred amino-terminal modifying groups alkyl groups. Preferred carboxy-terminal modifying groups include an amide group, an acetate group, an alkyl amide group, an aryl amide group or a hydroxy group. Pharmaceutical compositions comprising the compounds of the invention, and diagnostic and treatment methods for amyloidogenic diseases using the compounds of the invention, are also disclosed.
摘要翻译：调节天然化合物的化合物提供淀粉样肽聚集。本发明的调节剂包含肽，优选基于淀粉样肽，其完全由D-氨基酸组成。优选地，肽包含3-5个D-氨基酸残基，并且包括独立地选自D-亮氨酸，D-苯丙氨酸和D-缬氨酸的至少两个D-氨基酸残基。在一个特别优选的实施方案中，该肽是一种反式异构体，淀粉样蛋白肽，优选A-Bgr; 17-21的逆反异构体。在某些实施方案中，肽在氨基末端，羧基末端或两者都被修饰。优选的氨基末端修饰基团是烷基。优选的羧基末端修饰基团包括酰胺基，乙酸基，烷基酰胺基，芳基酰胺基或羟基。还公开了包含本发明化合物的药物组合物，以及使用本发明化合物的淀粉样变性疾病的诊断和治疗方法。

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