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DIAGNOSTIC IMAGING AGENT FOR OLIGOMERIC AMYLOID NEW

外国特許コード F210010576
整理番号 (S2020-0200-N0)
掲載日 2021年11月1日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2021JP007344
国際公開番号 WO 2021172515
国際出願日 令和3年2月26日(2021.2.26)
国際公開日 令和3年9月2日(2021.9.2)
優先権データ
  • 特願2020-033405 (2020.2.28) JP
発明の名称 (英語) DIAGNOSTIC IMAGING AGENT FOR OLIGOMERIC AMYLOID NEW
発明の概要(英語) Disclosed are a diagnostic imaging agent used for detecting oligomeric amyloid-β, with the active ingredient of the diagnostic imaging agent being a curcumin derivative that is present only in a keto form structure or a salt thereof; and a curcumin derivative represented by formula (IA): (in the formula, each R1 is independently a hydrogen atom, a fluorine atom, CH3-, CH2F-, CHF2-, CF3-, CH3O-, CH2FO-, CHF2O-, or CF3O-; each R2 is independently a hydrogen atom or a fluorine atom; A is alkyl, cyano, carboxy, alkoxycarbonyl, or R3-(CH2)m-; R3 is hydroxy, carboxy, cyano, alkylcarbonyloxy, alkoxycarbonyl, alkoxyalkoxy, hydroxyalkoxy, or CONR4R5; R4 and R5 are each independently a hydrogen atom or alkyl; and m is an integer of 1-5 (provided that when R1s are both CH3O- or CF3O-, and R2s are both a hydrogen atom, A must not be CH3-)) or a salt thereof.
従来技術、競合技術の概要(英語) BACKGROUND ART
The number of dementia patients in Japan is estimated to exceed 500 million and reaches 700 million in 2025, and resolution is an emergency and important problem. The most common of dementia is Alzheimer's disease (AD), and clinical symptoms of Alzheimer's disease are memory disorders, higher-order brain dysfunction (loss, loss, loss of absence, configuration loss), and the like. The symptoms are often common to other dementia diseases, and it is extremely difficult to definitively diagnose Alzheimer's disease using clinical symptoms alone.
Furthermore, in AD, the development of root therapeutic agents has failed in a manner. Alzheimer's disease brain has progressed 20~ 30 years prior to onset, and the importance of advanced medicine to diagnose and treat at the stage prior to onset has been pointed out.
Characteristic histopathology of Alzheimer's disease is geriatric plaques and neurofibrillary tangles. The main component of the former is amyloid beta protein with a beta sheet structure and that of the latter is hyperphosphorylated tau protein. It is known that in Alzheimer's disease, the pathological histological changes described above, such as accumulation of aggregated amyloid beta protein, begin in the brain far before clinical symptoms occur. Therefore, detection of aggregated amyloid β protein as a marker is one of early diagnosis methods for amyloid-accumulating diseases, particularly Alzheimer's disease.
At an early stage prior to the onset of AD, an oligomer of amyloid beta peptide (Aβ) plays an important role. The aggregates of Aβ become Aβ fibers (Aβ fibrils) via the Aβ oligomer. Because treatment after onset of AD is difficult, it is important to establish accurate diagnosis and develop therapies in the 40~ 50 s where toxic oligomers begin to accumulate.
From this perspective, in recent years, studies have been undertaken for radioactive contrast agents for positron tomography (PET) and single-photon tomography (SPECT) that selectively bind to amyloid beta protein in the brain. Classical compounds with high affinity for amyloid include Congo Red, thioflavin S and thioflavin T, which have been used for pathologically definitive diagnosis of Alzheimer's disease. Many of them pass through the blood-brain barrier and hardly migrate into the brain when administered intravenously.
Further, nuclear magnetic resonance imaging (MRI) is an example of a diagnostic method that does not use radionuclides. To date, the present inventors reported that senile spots were successfully imaged by fluorine nuclear magnetic resonance imaging (fluorine MR imaging) using a curcumin derivative (Patent Documents 1 and 2). In addition, Patent Document 3 reports a curcumin derivative that interacts with Aβ fibers and can be used to detect Aβ fibers.
However, to date, small molecule compounds that specifically bind to Aβ oligomers have not been reported.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • SHIGA UNIVERSITY OF MEDICAL SCIENCE
  • 発明者(英語)
  • TOOYAMA, Ikuo
  • TAGUCHI, Hiroyasu
  • YANAGISAWA, Daijiro
  • KATO, Tomoko
国際特許分類(IPC)
指定国 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 IT JO 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 ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN WS 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

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