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公开(公告)号：US20170197956A1
公开(公告)日：2017-07-13
申请号：US15326320
申请日：2015-07-15
发明人： Motomu KANAI , Yohei SOMA , Atsuhiko TANIGUCHI , Yusuke SHIMIZU
IPC分类号： C07D455/04 , C07D417/04
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 Aβ 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; R1 represents an optionally substituted hydrocarbon group; R2 represents a hydrogen atom or an optionally substituted hydrocarbon group; R3 and R4 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; R2 and R4 optionally together form an alkylene group; and R5 represents an anion.
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公开(公告)号：US20190100537A1
公开(公告)日：2019-04-04
申请号：US16087017
申请日：2017-03-21
发明人： Motomu KANAI , Yohei SOMA , Jizhi NI , Atsuhiko TANIGUCHI
摘要： Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to Aβ peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same. A curcumin-boron complex represented by the following formula (1): wherein X1 and X2 are identical or different, and each represent a halogenoalkyl group or a halogen atom; X3 represents a bromine atom, an iodine atom, or a selenium atom; R1 and R2 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R3 and R4 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R1 and R3 or R2 and R4 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; R5 and R6 are identical or different, and each represent a hydrogen atom or an optionally substituted alkyl group; R7 and R8 are identical or different, and each represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R5 and R7 or R6 and R8 are optionally taken together to form an optionally substituted alkylene group or alkenylene group; and m and n each represent an integer of 1 to 3, or a salt thereof.
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公开(公告)号：US20160137706A1
公开(公告)日：2016-05-19
申请号：US14898409
申请日：2014-06-13
发明人： Motomu KANAI , Yohei SOMA , Atsuhiko TANIGUCHI , Daisuke SASAKI
CPC分类号： C07K14/4711 , A61K38/00 , C07K1/113
摘要： 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).
摘要翻译： 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）。
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公开(公告)号：US20180042948A1
公开(公告)日：2018-02-15
申请号：US15555721
申请日：2016-03-04
发明人： Motomu KANAI , Yohei SOMA , Yusuke SHIMIZU , Atsuhiko TANIGUCHI , Kounosuke OISAKI , Yoichiro KUNINOBU
IPC分类号： A61K31/69 , A61K31/4725 , C07F5/02 , C07D215/06 , C07D207/46 , C07D207/456 , A61K31/4025 , C07D401/14
CPC分类号： A61K31/69 , A61K31/4025 , A61K31/4725 , A61K41/00 , C07D207/44 , C07D207/456 , C07D207/46 , C07D215/06 , C07D401/14 , C07D455/04 , C07F5/02
摘要： Provided are a compound which is useful as an in vivo applicable, amyloid-oxygenating catalyst selective for amyloid and applicable not only to an Aβ peptide but also to other amyloids and a drug containing the compound for preventing and/or treating amyloid-related-diseases.Disclosed is a boron-dipyrrin complex represented by the following formula (1) wherein X1 and X2 are the same or different and each represent a halogenoalkyl group or a halogen atom; R1 represents a hydrogen atom, an alkyl group, or a group represented by formula (b); R2 and R6 are the same or different and each represent a hydrogen atom or a halogen atom; R3, R4, R5, and R7 are the same or different and each represent a hydrogen atom, a halogen atom, or an alkyl group; R8 represents a hydrogen atom or —(CH2)l—(Y)m—(CH2)n—Z wherein Y represents —CO—, —CONH—, or a triazole ring, Z represents a carboxyl group, a sulfonic acid group, or a —CO-peptide residue, l and n each represent an integer of 1 to 6, and m represents 0 or 1; R9 and R10 are the same or different and each represent a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; and R8 and R10 together optionally form an alkylene group.
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