DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES
|Posted date||Nov 5, 2018|
|International application number||2018JP008773|
|International publication number||WO 2018164184|
|Date of international filing||Mar 7, 2018|
|Date of international publication||Sep 13, 2018|
|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||
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||
（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
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。）
A 1及びA 2のいずれか一方が水素原子を示し、他方が
|IPC(International Patent Classification)||
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
Contact Information for " DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES "
- Shiga University of Medical Science Research Cooperation Division
- URL: http://www.shiga-med.ac.jp/
- Address: Setatsukinowa-cho Ootsu-city Shiga-pref Japan , 520-2192
- Phone: 81-77-548-2847
- Fax: 81-77-548-2086