Atomic Energy Council-institute of Nuclear Energy Research

Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan

Show-Wen Liu

Cheng-Fang Hsu

Yu Lung Chang

Cheng-Hsien Lin

Tsyh-Lang Lin

Chih-Yuan Lin

Tsung-Hsien Chiang

Kuei-Lin Lu

Yueh-Feng Deng

Ming-Che Tsai

Da-Ming Wang

Ching-Yun Li

Sheng-Lun Lin

Wuu-Jyh Lin

Jenn-Tzong Chen

Lie-Hang Shen

Chyng-Yann Shiue

Shu-Hung Lin

Shiou-Shiow Farn

Yu-Lung Wu

I-Chung Tang

Kwei-Luen Hsu

Te-Sheng Liang

Chang-Mau Sheng

Ching-Jun Liou

Haw-Jan Chen

Sheng-Po Huang

A [F-18]FEONM precursor is synthesized. 2-bromoethanol is added to further connect an atom of oxygen at an N terminal of the precursor. Four atoms of carbon can be further connected. Thus, better fat-solubility is obtained along with the increase in carbon. Positioning in brain imaging becomes better.

Method of fabricating [F-18]FEONM precursor

A precursor for labeling therapeutic agents for liver cancer and a method for manufacturing the same are revealed. The chemical structure of the precursor has a ligand linked to complex compounds of radioisotopes. Moreover, the chemical structure of the precursor further includes a specific functional group soluble in Lipiodol or having properties of Lipiodol. Thus the radioisotopes attached to the precursor are allowed to retain in hepatic tissues of patients with liver cancer for internal radiation therapy of liver cancer.

Precursor for labeling therapeutic agent for liver cancer and method for manufacturing the same

A bifunctional compound and a method for manufacturing the same are revealed. The structural formula of the compound includes two main functional groups. One functional group is a diamide dithiolate (NS) ligand able to bind with radioisotopes. The other functional group is polybasic carboxylic acid that binds to biochemical substances. Based on properties of the above two functional groups, the compound of the present invention can be used for preparation of radiopharmaceuticals such as radiotracter for disease diagnosis or radioactive therapeutic agent for disease treatment.

Bifunctional compound and method for manufacturing the same

A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (NS) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while NSligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.

Precursor used for labeling hepatorcyte receptor and containing trisaccharide and diamide demercaptide ligand, method for preparing the same, radiotracer and pharmaceutical composition of the same

A radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same are revealed. The radiotracer precursor, DANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus DANI can be used to produce radiotracers stayed in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

Radiotracer precursor for imaging of hypoxic tissue, radiotracer, and method for preparing the same

The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus BANI can be used to produce radiotracers retained in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

Radiotracer precursor BANI for imaging of hypoxic tissue, radiotracer, and method for preparing the same

A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (BuSn) that is easy to be replaced. Thus a dopamine receptor radiotracerI-IBZM can be produced at high yield rate by a substitution reaction of the precursor. At the same time, both the method for preparing the precursor SnBZM and a method for preparing a reference standard IBZM are simplified. Moreover, stability of each product is improved.

Radiotracer precursor and method for preparing the same

A bifunctional compound with a monosaccharide and a NSligand, and more particularly, a bifunctional compound with a NSligand and aminohexylacetyl galactosamine (ah-GalNAc) is provided. A method for preparing the bifunctional compound with a monosaccharide and a NSligand is also provided, including activating a carboxyl group in an organic ligand, reacting the activated carboxyl group with a galactopyranoside through amidation, and then hydrolyzing. The bifunctional compound of the present invention is widely useful in nuclear medicine for preparation of liver imaging agents for assisting in correct diagnosis of diseases.

Bifunctional compound with monosaccharide and N2S2 ligand, and preparation and use thereof

HLMN series compounds used as radioactive agents for treatment of liver cancer and a manufacturing method thereof are revealed. 2-thioethylamine hydrochloride is reacted with triphenylmethanol for protection of thiol to obtain 2-[(triphenylmethyl)thio]ethylamine. Then obtain N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide by a transamidation reaction between 2-[(triphenylmethyl)thio]ethylamine and chloroactyl chloride. Next produce a amine-amide-thiol ligand-N-[2-((triphenylmethyl)thio)ethyl][2-((triphenylmethyl)thio)ethylamino]acetamide by a substitution reaction of N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide and 2-[(triphenylmethyl)thio]ethylamine. After respective reaction with 1-bromotetradecane, 1-bromohexadecane and ethyl 16-bromohexadecanoate, HLMN series compounds are obtained. These amine-amide-dithiols quadridentate ligands can react with MO(M=Tc or Re) to produce electrically neutral complexes. The complexes have high lipophilicity, allowing them soluble in lipiodol to be applied to radiation therapy for liver cancer.

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A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [Iodine](R)&#x2014;N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([I]MIPP) with a leaving group BuSn.

Method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, and use therof

A method for preparing a precursor of radioactive 3-iodobenzylguanidine- N,N'-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N&#x2032;-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N&#x2032;-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*l]MIBG.

Method for preparing precursor of radioactive 3-iodobenzylguanidine

A radioactive mixture and a manufacturing method thereof are disclosed. The radioactive mixture (Re-MN/Lipiodol mixture) is formed by chelating reaction of MN series compounds that are amine-amide-disulfide amine quadric-dentate chelate ligands with TcO/or ReO, and then dissolved in Lipiodol. Moreover, theTc/orRe of the TcO/or ReOavoids bone marrow injuries caused by freeY. By the feature of the Lipiodol that stays in liver tumors for a long period, the radioactive mixture is applied to treat liver cancers by injection so that injuries caused by surgical operations can be prevented.Re-MN/Lipiodol is used for liver cancer, breast cancer or other solid tumors treatment. Re-188 MN or Re-188 MN/Lipiodol can be mixed with anticancer drugs, hydrogel, liposome, micelle or other nano-particles to form the multifunctional therapeutic modality.

Radioactive mixture and manufacturing method thereof

A bifunctional compound containing an amino group and diaminedithiol ligand and a manufacturing method thereof are revealed, the bifunctional compound includes at least one amino group and a diaminedithiol (NS) ligand. The amino groups is for reacting with compounds containing carboxylic acids or halogens while the NSligand binds with technetium or rhenium so as to form an anion complex. The thiol group in the NSligand is protected by a protecting group for prevention of oxidation and easy storage. This protecting group is released easily during complex reactions. Due to the bifunctional property, the compound is applied to preparation of radiopharmaceuticals such as imaging agents and targeted agents.

Bifunctional compound containing amino group and diaminedithiol ligand and manufacturing method thereof

A compound containing carboxylate ester and N2S2 ligand bi-functional groups and a manufacturing method thereof are disclosed. The S in the N2S2 ligand of the compound containing carboxylate ester and N2S2 ligand bi-functional groups includes a protective group so as to avoid to be oxidized and easy storage. In a complex reaction, the protective group is automatically released As to the active carboxylate ester, it is for reacting with compounds having amino groups such as amines, amino acids, peptides, or protein etc while the N2S2 ligand is for bonding with technetium or rhenium so as to form neutral complex. The compound containing carboxylate ester and N2S2 ligand bi-functional groups is applied to radiopharmaceuticals such as contrast agents for tissues and target agents.

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Show-Wen Liu