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DIAGNOSTIC IMAGING AGENT FOR OLIGOMERIC AMYLOID

Foreign code F210010576
File No. (S2020-0200-N0)
Posted date 2021年11月1日
Country 世界知的所有権機関(WIPO)
International application number 2021JP007344
International publication number WO 2021172515
Date of international filing 令和3年2月26日(2021.2.26)
Date of international publication 令和3年9月2日(2021.9.2)
Priority data
  • 特願2020-033405 (2020.2.28) JP
Title DIAGNOSTIC IMAGING AGENT FOR OLIGOMERIC AMYLOID
Abstract 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.
Outline of related art and contending technology 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.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • SHIGA UNIVERSITY OF MEDICAL SCIENCE
  • Inventor
  • TOOYAMA, Ikuo
  • TAGUCHI, Hiroyasu
  • YANAGISAWA, Daijiro
  • KATO, Tomoko
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 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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