公开(公告)号：US20150299262A1

公开(公告)日：2015-10-22

申请号：US14648834

申请日：2013-10-18

Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

Inventor： Motomu KANAI ,  Yohei SOMA ,  Tadamasa ARAI ,  Daisuke SASAKI ,  Yuki KOBAYASHI

IPC: C07K7/64

CPC classification number: C07K7/64 ,  A61K38/00 ,  C07K7/06

Abstract: Provided is a novel compound which has excellent inhibitory activity for Aβ aggregation, and which is useful as a drug.A cyclic peptide or a salt thereof, the cyclic peptide having an amino acid sequence represented by the following formula (1): X-Leu-Val-Y1—Y2  (1) (wherein X is Lys, Arg, His, Ala, Gly, Ser, or Thr; and Y1 and Y2, which are identical to or different from each other, each represent a group represented by the following formula (2): (wherein Ar1 represents an aromatic hydrocarbon group or an aromatic heterocyclic group (the aromatic hydrocarbon group or the aromatic heterocyclic group may have 1 to 5 substituents selected from the group consisting of an alkyl group, a cycloalkyl group, a haloalkyl group, a halogen atom, a hydroxy group, an alkoxy group, an aromatic hydrocarbon group, an aromatic heterocyclic group, and an amino group); R1 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a haloalkyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group (the aromatic hydrocarbon group or the aromatic heterocyclic group may have 1 to 5 substituents selected from the group consisting of an alkyl group, a cycloalkyl group, a haloalkyl group, a halogen atom, a hydroxy group, an alkoxy group, an aromatic hydrocarbon group, an aromatic heterocyclic group, and an amino group); and n is an integer from 0 to 2)), wherein the α-amino group at the amino terminus of the amino acid sequence is linked, via a peptide bond, to the carboxyl group at the carboxyl terminus of the amino acid sequence.

Abstract translation: 提供了对A＆Bgr具有优异抑制活性的新型化合物。 聚集，并且其作为药物是有用的。 环状肽或其盐具有下述式（1）表示的氨基酸序列的环状肽：X-Leu-Val-Y1-Y2（1）（式中，X为Lys，Arg，His，Ala，Gly ，Ser或Thr; Y1和Y2彼此相同或不同，分别表示由下式（2）表示的基团：（其中Ar1表示芳香族烃基或芳香族杂环基（芳香族） 烃基或芳族杂环基可以具有1〜5个选自烷基，环烷基，卤代烷基，卤素原子，羟基，烷氧基，芳香族烃基，芳香族烃基 杂环基和氨基）; R 1表示氢原子，烷基，环烷基，卤代烷基，芳香族烃基或芳香族杂环基（芳香族烃基或芳香族杂环基可以具有1个 至5个取代基 由烷基，环烷基，卤代烷基，卤素原子，羟基，烷氧基，芳香族烃基，芳香族杂环基和氨基组成的组构成）。 且n为0至2的整数）），其中氨基酸序列的氨基末端的α-氨基通过肽键连接到氨基酸序列的羧基末端的羧基。

公开(公告)号：US20160137706A1

公开(公告)日：2016-05-19

申请号：US14898409

申请日：2014-06-13

Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY

Inventor： Motomu KANAI ,  Yohei SOMA ,  Atsuhiko TANIGUCHI ,  Daisuke SASAKI

IPC: C07K14/47 ,  C07K1/113

CPC classification number: C07K14/4711 ,  A61K38/00 ,  C07K1/113

Abstract: The invention provides an Aβ peptide aggregation inhibitor, an Aβ peptide toxicity reducing agent, and a preventive and/or therapeutic agent for Alzheimer's disease. The oxidized Aβ peptide in which one or more amino acid residues of Aβ peptide have been oxidized (excluding an oxidized Aβ peptide in which only Met has been oxidized).

Abstract translation: 本发明提供了一种A＆bgr; 肽聚集抑制剂，A＆bgr; 肽毒性还原剂，以及阿尔茨海默病的预防和/或治疗剂。 氧化的A＆bgr 肽，其中A和Bgr的一个或多个氨基酸残基; 肽已被氧化（不包括氧化的A＆bgr肽，其中仅Met被氧化）。