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DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES

Foreign code F180009568
File No. (S2017-0497-N0)
Posted date Nov 5, 2018
Country WIPO
International application number 2018JP008773
International publication number WO 2018164184
Date of international filing Mar 7, 2018
Date of international publication Sep 13, 2018
Priority data
  • P2017-046350 (Mar 10, 2017) JP
Title DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES
Abstract Disclosed is a compound selected from among aniline derivatives represented by formula (1) and naphthalene derivatives represented by formula (2), or a salt thereof. (In the formulae, each of R1 and R2 independently represents a hydrogen atom or an alkyl group; and one of A1 and A2 represents a hydrogen atom, while the other represents a fluorine atom-substituted or unsubstituted alkoxy group or a group represented by formula (AA). In formula (AA), R3 represents a fluorine atom-substituted or unsubstituted ethylene group; R4 represents a fluorine atom-substituted or unsubstituted ethyl group; and n represents an integer of 1-10. In cases where n represents an integer of 2 or more, the R3 moieties may be the same as or different from each other.)
Outline of related art and contending technology BACKGROUND ART
Alzheimer's disease, progressive occurring aged from the pre-characterized disease and dementia, currently, national 460 number of patients is called as a million or more.In the future, along with the aging of the population to ensure that the number is expected to increase.Advances the study of Alzheimer's disease, the underlying therapeutic drug development has been promoted.Using these novel agents in order to perform the treatment of Alzheimer, early and accurate diagnosis of Alzheimer's disease in a noninvasive method is essential.
Clinical symptoms of Alzheimer's disease, memory impairment, higher order brain dysfunction (aphasia, row deletion, the deletion is confirmed, the deletion line configuration) or the like.Other disease symptoms of dementia often seen in common, not only the clinical symptoms of Alzheimer's disease is a definitive diagnosis extremely difficult.
On the other hand, the feature of Alzheimer's disease as the pathological tissue finding, senile plaques and neurofibrillary change. Β-sheet structure is a major component of the former amyloid β protein and taking, in the latter it is phosphorylated tau proteins in excess.Clinical symptoms in Alzheimer's disease from the front side and develop, amyloid aggregated β protein in the brain of the pathological tissue changes such as the accumulation of the beginning is known.
From such a viewpoint, in recent years, β-amyloid proteins in the brain to selectively couple (PET) and single photon emission computed tomography positron emission tomography (SPECT) studies for radioactive contrast agent has been promoted.However, they are, 11C, 13N, 15O, 18F in order to use radionuclides such as side effects caused by the radiation damage and there is a concern, it is necessary to be provided with a facility near the cyclotron, is very expensive and the cost of the reagent in question.Therefore, a diagnosis method that does not use radioactive nuclide has been desired.
A radionuclide is not used as one of the diagnostic methods of nuclear magnetic resonance imaging (MRI) is a method.To this, fluorine nuclear magnetic resonance imaging (MR imaging fluorine) using the image of the senile plaques is successful, the present inventors et al. and have been reported from the group of the Tsukuba (JP-1-5, non-patent document 1).
Abnormal deposition of the protein with a disease which is referred to as the (tauopathy) ETLHI.Hyperphosphorylated tau protein is the accumulation, the accumulation of amyloid β protein delay than is believed to arise, the accumulation of amyloid β protein neurofibrillary tangles as compared with the closely related to the severity of the disease are considered.
Therefore, for a SPECT and PET binding protein with a radioactive contrast agent and research, such as the contrast agent, for example, have been reported in JP-6-9.A radionuclide such a problem as described above is present, up to now using MRI imaging of neurofibrillary tangles successful has not been reported.
Scope of claims (In Japanese)請求の範囲
[請求項1]
 式(1)で表されるアニリン誘導体及び式(2)で表されるナフタレン誘導体から選択される化合物又はその塩。
[化1]
[化2]
(式中、R 1及びR 2はそれぞれ独立に水素原子又はアルキルを示す。
A 1及びA 2のいずれか一方は水素原子を示し、他方はフッ素原子置換又は未置換のアルコキシ又は
[化3]
を示す。ここで、R 3はフッ素原子置換又は未置換のエチレン基を示し、R 4はフッ素原子置換又は未置換のエチルを示し、nは1~10の整数を示す。nが2以上の整数を示す場合、R 3は同一であっても、異なっていてもよい。)
[請求項2]
 A 1及びA 2のいずれか一方が水素原子を示し、他方が
[化4]
を示し、nが5~8の整数を示す、請求項1に記載の化合物又はその塩。
[請求項3]
 標識化された請求項1に記載の化合物又はその塩。
[請求項4]
 前記標識が放射性核種である、請求項3に記載の化合物又はその塩。
[請求項5]
 請求項1若しくは2に記載の化合物又はその塩を有効成分とするタウオパチーのMRI用画像診断薬。
[請求項6]
 請求項1、3若しくは4に記載の化合物又はその塩を有効成分とするタウオパチーのポジトロン断層撮影法(PET)用画像診断薬。
[請求項7]
 前記タウオパチーがアルツハイマー病、進行性核上性麻痺、大脳皮質変性症、前頭側頭型認知症又はピック病である、請求項5又は6に記載の画像診断薬。
[請求項8]
 請求項5~7のいずれか一項に記載の画像診断薬を投与する工程を含む、タウオバチーの診断方法。
[請求項9]
 請求項1~4のいずれか一項に記載の化合物又はその塩を有効成分とするタウオパチー診断用の体外診断薬。
[請求項10]
 前記タウオパチーがアルツハイマー病、進行性核上性麻痺、大脳皮質変性症、前頭側頭型認知症又はピック病である、請求項9に記載の体外診断薬。
[請求項11]
 請求項9又は10に記載の体外診断薬を用いて試料中のタウ蛋白を検出する工程を含む、タウオバチーの診断方法。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NATIONAL UNIVERSITY CORPORATION SHIGA UNIVERSITY OF MEDICAL SCIENCE
  • OTSUKA PHARMACEUTICAL CO., LTD.
  • Inventor
  • TOOYAMA, Ikuo
  • YANAGISAWA, Daijiro
  • TAGUCHI, Hiroyasu
  • SOGABE, Takayuki
  • SHIRAI, Nobuaki
  • HIRAO, Koichi
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 JO 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

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