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DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES NEW

外国特許コード F180009568
整理番号 (S2017-0497-N0)
掲載日 2018年11月5日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2018JP008773
国際公開番号 WO 2018164184
国際出願日 平成30年3月7日(2018.3.7)
国際公開日 平成30年9月13日(2018.9.13)
優先権データ
  • 特願2017-046350 (2017.3.10) JP
発明の名称 (英語) DIAGNOSTIC IMAGING AGENT AND EXTRACORPOREAL DIAGNOSTIC AGENT FOR INTRACTABLE NEUROLOGICAL DISEASES NEW
発明の概要(英語) 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.)
従来技術、競合技術の概要(英語) 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.
  • 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
  • NATIONAL UNIVERSITY CORPORATION SHIGA UNIVERSITY OF MEDICAL SCIENCE
  • OTSUKA PHARMACEUTICAL CO., LTD.
  • 発明者(英語)
  • Nobuaki Shirai
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 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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