Futurechem Co., Ltd

Korea Institute of Science and Technology

Sogang University Research Foundation

The Asan Foundation

Dae-Yoon Chi

Byoung-Se Lee

Ick-Chan Kwon

Kui-Won Choi

Kwang-Meyung Kim

Hee-Seup Kil

Sang-Yoon Kim

Chansoo Park

Hyun-Ju Sung

Dae-hyuk Moon

Ju-Hee Ryu

Beom-Suk Lee

So-Young Chu

Woojin Cho

Jong-Min Kim

Seung-Jin Lee

Heewon Kang

Jae-seung Kim

Jin-sook Ryu

Kyeong-Soon Park

Seung-Jae Myung

Seung-jun Oh

Seul-Ki Lee

In-Chan Youn

Hye-Rim Kwon

Min-Hyung Lee

Hyojin Cha

Kyunghun Kim

Jae-Hak Lee

Cheol-Soo Lee

Eun-Young Heo

Sirion Uthaiwan

Woon-Jung Jung

Yu-Jin Bae

The present invention relates to a solid precursor in the form of an organic salt, the solid precursor having a solid support, a method for manufacturing same, and an application thereof. The solid precursor of the present invention enables omission of the [F]fluoride refining process using additional cartridge, and the use of excessive phase-transfer catalyst, and can easily remove remaining substance after reaction through the solid support inside the precursor. The solid precursor of the present invention is very appropriate for an automated synthesis device as an all-in-one system that can carry out overall process of [F]fluorosis reaction, when used by charging in a cartridge.

Precursor compound connected to solid support for manufacturing 18F radiopharmaceutical, method for manufacturing same, and application thereof

The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducingF using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.

18F-labeled precursor of PET radioactive medical supplies, and preparation method thereof

The present invention relates to an anticancer prodrug consisting of peptide of acetyl-SEQ ID NO: 1-linker-anticancer drug. The anticancer prodrug effectively provides an anticancer drug unstable in acid or base, such as doxorubicin, in a form of prodrug. Thus, the anticancer prodrug exists as a non-toxic inactive form when administered into the body, but effectively releases the anticancer drug as an active ingredient in the target area in the presence of caspase activated by radiation or UV treatment after administered into the body. Accordingly, the anticancer drug exhibits selective anticancer effects on cancer cells, thereby maximizing the therapeutic effect and minimizing the side-effects of chemotherapy.

Anticancer prodrug activated by radiation or ultraviolet treatment and use thereof

The present invention relates to an anticancer prodrug consisting of peptide of acetyl-SEQ ID NO: 1-linker-anticancer drug. The anticancer prodrug effectively provides an anticancer drug unstable in acid and base, such as doxorubicin, in a form of prodrug. Thus, the anticancer prodrug exists as a non-toxic inactive form when administered into the body, but effectively releases the anticancer drug as an active ingredient in the target area in the presence of caspase activated by radiation or UV treatment after administered into the body. Accordingly, the anticancer drug exhibits selective anticancer effects on cancer cells, thereby maximizing the therapeutic effect and minimizing the side-effects of chemotherapy.

Anticancer prodrugs activated by radiation or ultraviolet treatment and use thereof

Method and apparatus for synthesizing an F-18 labeled radioactive pharmaceutical by labeling a precursor with an F-18 radioactive isotope, by reacting the labeled precursor to obtain a labeled pharmaceutical, by separating impurities from the labeled pharmaceutical to provide a purified labeled pharmaceutical, and by collecting the purified labeled pharmaceutical. The apparatus includes a labeling cartridge that contains the precursor, receives the isotope, and causes a labeling reaction to provide the labeled precursor; a synthesizing container that receives the labeled precursor, receives at least one reagent effective to hydrolyze the labeled precursor, and within which the labeled precursor undergoes a hydrolysis reaction to provide the labeled pharmaceutical; and a separation cartridge that receives the labeled pharmaceutical, and contains a polymer compound that separates impurities into polar compounds and nonpolar compounds to provide the purified labeled pharmaceutical. The labeling and separation cartridges may be contained in a removable cassette.

Apparatus and method for synthesizing F-18 labeled radioactive pharmaceuticals

The present invention relates to (3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or to the pharmaceutically acceptable salt thereof, to a method for preparing same, and to a pharmaceutical composition containing same as active ingredients for the diagnosis or treatment of neurodegenerative brain diseases. The aryl derivatives of the present invention are (3-fluoro-2-hydroxy)propyl-functionalized to increase the polarity thereof, and therefore the drugs containing the aryl derivatives can easily permeate into the cerebrovascular membrane, thus increasing the effectiveness of the drugs. As the aryl derivatives of the present invention strongly bind to &#x3b2;-amyloid, the aryl derivatives, when labeled with radioisotope, can be used as a diagnostic agent for non-invasively diagnosing early Alzheimer's disease. Further, the aryl derivatives of the present invention bind to low molecular &#x3b2;-amyloid peptide conjugates to inhibit the generation of malignant high molecular &#x3b2;-amyloid plaque, and thus can be effectively used as a therapeutic agent for neurodegenerative brain diseases such as Alzheimer's disease.

(3-fluoro-2-hydroxy)propyl-functionalized aryl derivatives or pharmaceutically acceptable salts thereof, method for preparing same, and pharmaceutical composition containing same as active ingredient for the diagnosis or treatment of neurodegenerative brain diseases

Disclosed are a nanoparticle sensor for measuring protease activity, for protease imaging, and a method for preparing the same. More specifically, the present invention relates to a nanoparticle sensor for measuring protease activity in which a fluorophore- and a quencher-conjugated peptide substrate is conjugated to a biocompatible polymer nanoparticle. The peptide substrate is specifically lysed by a protease. The sensor according to the present invention is capable of inhibiting emission of fluorescence with high extinctive activity of the quencher on a fluorescent material. But strong fluorescence is specifically emitted only if the peptide substrate is lysed by a specific protease. Therefore, the sensor is especially useful as a method for screening a novel drug such as a protease overexpression inhibitor, and early diagnosis of incurable diseases and various diseases such as autoimmune diseases including cancer, osteoarthritis, rheumatoid arthritis and dementia.

Nanoparticle sensor for measuring protease activity and method for manufacturing the same

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Seoul, South Korea

Dae-Yoon Chi