公开(公告)号：EP3009446A4

公开(公告)日：2017-01-18

申请号：EP14810613

申请日：2014-06-13

申请人： JAPAN SCIENCE & TECH AGENCY

发明人： KANAI MOTOMU ,  SOMA YOHEI ,  TANIGUCHI ATSUHIKO ,  SASAKI DAISUKE

IPC分类号： C07K14/47 ,  A61K38/00 ,  A61K38/17 ,  A61K45/00 ,  A61P25/28 ,  C07K1/113

CPC分类号： C07K14/4711 ,  A61K38/00 ,  C07K1/113

摘要： The invention provides an A² peptide aggregation inhibitor, an A² peptide toxicity reducing agent, and a preventive and/or therapeutic agent for Alzheimer's disease. The oxidized A² peptide in which one or more amino acid residues of A² peptide have been oxidized (excluding an oxidized A² peptide in which only Met has been oxidized).

摘要翻译： 本发明提供了A 2肽聚集抑制剂，A 2肽毒性还原剂和阿尔茨海默病的预防和/或治疗剂。 A 2肽的一个或多个氨基酸残基被氧化的氧化的A 2肽（不包括其中仅Met被氧化的氧化的A 2肽）。

公开(公告)号：EP2940037A4

公开(公告)日：2016-08-03

申请号：EP13868231

申请日：2013-10-18

申请人： JAPAN SCIENCE & TECH AGENCY

发明人： KANAI MOTOMU ,  SOMA YOHEI ,  ARAI TADAMASA ,  SASAKI DAISUKE ,  KOBAYASHI YUKI

IPC分类号： C07K7/64 ,  A61K38/00 ,  A61P25/28

CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/06

摘要： Provided is a novel compound which has excellent inhibitory activity for A² 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): €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒX-Leu-Val-Y 1 -Y 2 €ƒ€ƒ€ƒ€ƒ€ƒ(1) (wherein X is Lys, Arg, His, Ala, Gly, Ser, or Thr; and Y 1 and Y 2 , which are identical to or different from each other, each represent a group represented by the following formula (2) : (wherein Ar 1 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); R 1 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 ±-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.

公开(公告)号：EP3170820A4

公开(公告)日：2017-12-06

申请号：EP15822530

申请日：2015-07-15

申请人： JAPAN SCIENCE & TECH AGENCY

发明人： KANAI MOTOMU ,  SOMA YOHEI ,  TANIGUCHI ATSUHIKO ,  SHIMIZU YUSUKE

IPC分类号： C07D417/04 ,  A61K31/4725 ,  A61K31/4745 ,  A61K38/00 ,  A61P3/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  C07D455/04 ,  C07K7/06 ,  C07K14/47

CPC分类号： C07D455/04 ,  A61K31/4725 ,  A61K31/4745 ,  A61K38/00 ,  C07D417/04 ,  C07K7/06 ,  C07K14/47

摘要： It is intended to provide: a compound useful as an amyloid oxidation catalyst which is applicable in vivo and is applicable not only to A² peptides but to other amyloids; and a prophylactic or therapeutic drug for an amyloid-related disease, comprising the same. The present invention provides a benzothiazole compound represented by the following formula (1) wherein X represents a halogen atom; R 1 represents an optionally substituted hydrocarbon group; R 2 represents a hydrogen atom or an optionally substituted hydrocarbon group; R 3 and R 4 are the same or different and each represent a hydrogen atom, an optionally substituted hydrocarbon group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; R 2 and R 4 optionally together form an alkylene group; and R 5 represents an anion.

公开(公告)号：EP3081556A4

公开(公告)日：2017-06-07

申请号：EP14870019

申请日：2014-12-09

申请人： JAPAN SCIENCE & TECH AGENCY

发明人： KANAI MOTOMU ,  SOMA YOHEI ,  ARAI TADAMASA ,  ARAYA TAKUSHI

IPC分类号： C07D213/81 ,  A61K31/44 ,  A61K31/505 ,  A61P25/28 ,  C07D239/30

CPC分类号： C07D213/81 ,  C07D239/30

摘要： Provided is a novel compound which has an excellent A² aggregation inhibitory effect and is useful as a pharmaceutical. An amide compound represented by the formula (1) or a salt thereof, wherein Z represents CH or N; A and B are the same or different and each represents -CH 2 -, -O-, -S-, or -NH-; R 1 and R 2 are the same or different and each represents a branched alkyl group, a branched alkenyl group, an optionally substituted aromatic hydrocarbon group, an optionally substituted aralkyl group, an optionally substituted cycloalkyl group, or an optionally substituted aromatic heterocyclic group; and R 3 represents a branched alkyl group, a branched alkenyl group, an optionally substituted cycloalkyl group, or an optionally substituted aralkyl group.

摘要翻译： 提供了具有优异的A 2聚集抑制效果并且可用作药物的新型化合物。 由式（1）表示的酰胺化合物或其盐，其中Z表示CH或N; A和B相同或不同，并且各自表示-CH 2 - ， - O - ， - S-或-NH-; R 1和R 2相同或不同，表示支链烷基，支链烯基，可以具有取代基的芳香族烃基，可以具有取代基的芳烷基，可以具有取代基的环烷基或可以具有取代基的芳香族杂环基。 并且R 3表示支链烷基，支链烯基，任选取代的环烷基或任选取代的芳烷基。