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PHOSPHONIUM COMPOUND AND PRODUCTION METHOD THEREFOR

外国特許コード F160008915
整理番号 S2016-0741-N0
掲載日 2016年12月22日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2015JP059857
国際公開番号 WO 2016072104
国際出願日 平成27年3月30日(2015.3.30)
国際公開日 平成28年5月12日(2016.5.12)
優先権データ
  • 特願2014-224986 (2014.11.5) JP
発明の名称 (英語) PHOSPHONIUM COMPOUND AND PRODUCTION METHOD THEREFOR
発明の概要(英語) The present invention provides a phosphonium compound indicated by formula (II). Also provided is a production method for a quaternary phosphonium compound labelled with positron emitting radionuclides, that includes a step in which: an electrophile indicated by formula (I) X1-CH2-A1 is reacted with a triphenylphosphine having at least one substituent labelled with positron emitting radionuclides on a benzene ring; and a quaternary phosphonium salt is obtained.
従来技術、競合技術の概要(英語) BACKGROUND ART
Between the inside and outside the inner mitochondrial membrane and a proton concentration gradient, the inner mitochondrial membrane by a concentration gradient of from - 180mV to - 140mV of the membrane potential is generated. Non-localized fat-soluble cation positive charge within the molecule (Delocalized Liphphilic Cations, DLCs) resonance stabilization by delocalization has a structure that allows molecules, the lipid bilayer of the cell membrane has a fat-soluble can easily pass through, the electrochemical potential of mitochondrial membrane potential using, to the mitochondrion of the in vivo are integrated has the property (non-patent document 1 and 2).
Is labeled with a radionuclide DLCs, myocardial blood flow imaging, , brown adipose tissue in applications such as imaging active (Brown Adipose Tissue, BAT) usage of has been studied and, in particular myocardial blood flow imaging has been many reports.
Current, ischemic heart disease and the most common cause of death in the world, according to a survey of the World Health Organization for the year 2011 are 700 million people died. In Japan is ischemic heart disease, malignant neoplasm and then a second cause of death and the 2 - position. Ischemic heart disease such as myocardial infarction or angina pectoris is a generic term, the progress of arteriosclerosis of the coronary artery and the main causes, effective for the treatment is important in the early detection of myocardial ischemia. Therefore, leads to the early detection of ischemic heart disease in the development of a highly accurate diagnosis is one of important problems in the modern medicine can be considered to be 1.
Ischemic heart disease general assay, electrocardiography, ultrasound examination, blood test, in addition to cardiac catheter inspection or the like, in the nuclear medical examination using PET or SPECT imaging and myocardial blood flow. In the case of a myocardial ischemic condition is mild, the patient is a calm state at the time of the entire myocardial blood flow but kept, load is exerted on the cardiac muscles in motion such as the myocardium may more oxygen, the need for nutrients, circulation resulting in increased blood flow. Resulting in increased blood flow in normal tissues is on the other hand, after the site of the stenosis in the arterioles, dilates the blood vessels in the at rest substantially to the maximum blood flow were maintained, coronary blood flow is not increased. When the load is in the imaging of the myocardium therefore, appear as an image loss of radioactivity is the site of the stenosis. Based on this principle, by patient movement or adenosine agent such as a load is applied to the myocardium, resting myocardial blood flow by comparing the image of the diagnosis is performed.
The current clinical practice,201 TlTlClor99m Tclabeled99m TcSestamibi(MIBI) 、99m TcTetrofosminSPECT such as as an imaging agent for myocardial blood flow agent is mainly used. However, a radiation standardized SPECT attenuation correction techniques may be not, large fat in the chest or the patient by the female patient adversely affect or attenuated, are not suitable for a quantitative measurement such as limitations, with high spatial resolution and sensitivity are expected to be used PET.
Apoptosis or programmed cell death, the cell specific protease (caspase) which is executed via the activation of. Is the activation of caspases, cytochrome c release from mitochondria is responsible, in its free of the mitochondrial changes in membrane potential can happen in parallel have been reported. Mitochondria play an important role in the control of apoptosis (non-patent document 3) responsible for.
Brown adipose tissue is responsible for storing energy due to the consumption of energy in white adipose unlike to produce heat from, and has been a therapeutic target for treatment of obesity of. Brown fat, maintenance of body temperature in the cold environment, intake of high fat diet is to produce heat, this heat production and enriched in brown fat cells is carried out in the mitochondria.
As an agent for PET is,15 OH2 Oor13 NNH3 、82 RbRbClis reported. However,15 O2 is minute,13 N10 min is short half - lives,15 OH2 Oor13 NNH3 cyclotron held the use of limited clinical facilities. In addition,82 Rbis82 Srmanufactured from the generator, the generator is expensive and thus limited the use of a high throughput. Therefore, these nuclides (110 min) compared to having a prolonged half-life18 Fof labeled PET imaging agents are under research and development has been actively conducted in recent years (Patent Document 1-3, and non-patent document 5-11).
  • 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
  • TOHOKU UNIVERSITY
  • 発明者(英語)
  • FURUMOTO, Shozo
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 DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR 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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