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CURCUMIN-BORON COMPLEX AND PHARMACEUTICAL CONTAINING SAME

Foreign code F170009274
File No. E112P09WO
Posted date Oct 31, 2017
Country WIPO
International application number 2017JP011232
International publication number WO 2017164172
Date of international filing Mar 21, 2017
Date of international publication Sep 28, 2017
Priority data
  • P2016-056615 (Mar 22, 2016) JP
Title CURCUMIN-BORON COMPLEX AND PHARMACEUTICAL CONTAINING SAME
Abstract Provided are a compound that is bioapplicable and amyloid-selective, and is useful as an amyloid oxidation catalyst applicable not only to aβ peptides but to other amyloids as well, and a preventive/therapeutic agent for amyloid-related diseases using the same. A curcumin-boron complex represented by general formula (1) (wherein: X1 and X2 are identical or different, and represent a halogenoalkyl group or an halogen atom; X3 represents a bromine atom, an iodine atom, or a selenium atom; R1 and R2 are identical or different, and represent a hydrogen atom or an optionally substituted alkyl group; R3 and R4 are identical or different, and represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R1 and R3 or R2 and R4 together may form an optionally substituted alkylene group or alkenylene group; R5 and R6 are identical or different, and represent a hydrogen atom or an optionally substituted alkyl group; R7 and R8 are identical or different, and represent a hydrogen atom, a halogen atom, an alkoxy group, or an optionally substituted alkyl group, or R5 and R7 or R6 and R8 together may form an optionally substituted alkylene group or alkenylene group; and m and n represent integers from 1 to 3), or a salt thereof.
Outline of related art and contending technology BACKGROUND ART
Usually, by folding of the protein, to form a specific native are responsible for vital functions, on the other hand misfolding can be aggregated into β-sheet structure rich fibers sometimes (amyloid-). In the course of the production of the amyloid aggregates (oligomers, proto-fibrillar, fibers) known to cause various functions and disorders (such conditions include 'amyloid' collectively referred to as a), of one or more 20 of the amyloid protein have been identified as the causative agent. Amyloid such as, for example, β amyloid Alzheimer's disease, tau protein, Parkinson's disease α-synuclein, amylin diabetes, systemic - cis transthyretin, such as Huntington's disease Huntingtin is known.
These pathogenic amyloid development of therapeutics targeting strategy include, for example Alzheimer's disease amyloid amyloid β with respect to (abbreviated as A β), precursor protein from an inhibitor of an enzyme that A β, accelerator A β-degrading enzyme, immunotherapy, or the like of the aggregation-inhibiting A β is known. On the other hand, with respect to A β, oxygenation of the body A β peptide Met (A β peptide Met residues and a sulfur atom oxygenized (O) oxygen ligand) a small amount remains within the living body, and the oxygenation Met A β body is unlikely to be agglomerates as compared to the peptide have been reported (non-patent document 1-3). From such a viewpoint, the present inventors, represented by the formula flavin binding site A β using photocatalyst A β peptide A β peptide oxygenized and oxygenation was obtained, the oxygenized body A β A β peptide is reported to suppress the flocculation of (non-patent document 4).
Scope of claims (In Japanese)[請求項1]
次の一般式(1)
[化1]
(式中、X1及びX2は、同一又は異なって、ハロゲノアルキル基又はハロゲン原子を示し;
X3は、臭素原子、ヨウ素原子又はセレン原子を示し;
R1及びR2は、同一又は異なって、水素原子又は置換基を有していてもよいアルキル基を示し;
R3及びR4は、同一又は異なって、水素原子、ハロゲン原子、アルコキシ基又は置換基を有していてもよいアルキル基を示すか、R1とR3、又はR2とR4が一緒になって、置換基を有していてもよいアルキレン基又はアルケニレン基を形成してもよく;
R5及びR6は、同一又は異なって、水素原子又は置換基を有していてもよいアルキル基を示し;
R7及びR8は、同一又は異なって、水素原子、ハロゲン原子、アルコキシ基又は置換基を有していてもよいアルキル基を示すか、R5とR7、又はR6とR8が一緒になって、置換基を有していてもよいアルキレン基又はアルケニレン基を形成してもよく;
m及びnは、1~3の整数を示す)
で表されるクルクミンホウ素錯体又はその塩。
[請求項2]
X1がハロゲノアルキル基であり、X2がハロゲン原子である請求項1記載のクルクミンホウ素錯体又はその塩。
[請求項3]
m及びnが1である請求項1又は2記載のクルクミンホウ素錯体又はその塩。
[請求項4]
R1、R2、R3、R4、R5、R6、R7及びR8が示す置換基を有していてもよいアルキル基が、カルボキシ基、スルホン酸基、ヒドロキシ基、アミノ基、-CO-、-CONH-及びトリアゾール基から選ばれる1種以上の置換基を有していてもよいアルキル基である請求項1~3のいずれか1項に記載のクルクミンホウ素錯体又はその塩。
[請求項5]
R1とR3、R2とR4、R5とR7、又はR6とR8が一緒になって形成されるアルキレン基又はアルケニレン基の炭素数が2又は3である請求項1~4のいずれか1項に記載のクルクミンホウ素錯体又はその塩。
[請求項6]
請求項1~5のいずれか1項に記載のクルクミンホウ素錯体又はその塩を有効成分とする医薬。
[請求項7]
病原性アミロイドが関連する疾患の予防又は治療薬である請求項6記載の医薬。
[請求項8]
請求項1~5のいずれか1項に記載のクルクミンホウ素錯体又はその塩及び薬学的に許容される担体を含有する医薬組成物。
[請求項9]
病原性アミロイドが関与する疾患の予防又は治療薬製造のための請求項1~5のいずれか1項に記載のクルクミンホウ素錯体又はその塩の使用。
[請求項10]
病原性アミロイドが関与する疾患を予防又は治療するための、請求項1~5のいずれか1項に記載のクルクミンホウ素錯体又はその塩。
[請求項11]
請求項1~5のいずれか1項に記載のクルクミンホウ素錯体又はその塩の有効量を投与することを特徴とする病原性アミロイドが関連する疾患を予防又は治療する方法。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
  • Inventor
  • KANAI, Motomu
  • SOMA, Yohei
  • NI, Jizhi
  • TANIGUCHI, Atsuhiko
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG
Reference ( R and D project ) ERATO KANAI Life Science Catalysis AREA
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