Institute of Nuclear Energy Research

Tty Biopharm Company, Limited

Institute of Nuclear Energy Research Rocaec

Institute of Nuclear Energy Research, Taiwan

Shyh-Yi Chyi

Te-Wei Lee

Shiang-Rong Chang

Lie-Hang Shen

Zei-Tsan Tsai

Tian-Fu Huang

Chih-Hsien Chang

Shui-Tein Chen

Ying-Kai Fu

Chun-Ying Huang

Gann Ting

Shu-Ling Chen

Henton Huang

Te-Jung Chen

Kwo-Ping Chang

Hui-Lan Wu

Ming-Der Yu

Wei-Lian Chen

Yin-Mao Hsu

Chang-Mau Shing

Kung-Tsung Wang

Wei-Chuan Hsu

Kuo-Hsien Fan

Charng-Feng Kao

Ming-Shiuan Wu

Yao-Tsung Hsieh

This invention provides a process for producing a radioactive arsenic-containing compound, comprising the steps of: (i) subjecting an arsenic-containing compound to a neutron irradiation treatment, said arsenic-containing compound being selected from a group consisting of AsO, AsS, AsS, and a combination thereof, such that the arsenic element contained in the arsenic-containing compound is converted to a radioactive arsenic isotope; and (ii) recovering the resultant product from step (i). This invention also provides a pharmaceutical composition comprising a therapeutically effective amount of the radioactive arsenic-containing compound and a pharmaceutically acceptable carrier. The pharmaceutical composition can be used in the treatment of tumors/cancers such as hematological malignancies and solid tumors.

Radioactive arsenic-containing compounds and their uses in the treatment of tumors

This invention relates a process for preparing octreotide and derivatives thereof. The starting material, Thr(ol)(tBu)-2-chlorotrityl resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin or D-Phe-Cys(Trt)-Tyr(tBu)-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)(tBu)-2-chlorotrityl resin was obtained. Cleavage of the peptide from the resin was achieved by strong acid solution. The cleaved peptide reacted with charcoal to give disulfide-containing peptide of

Process for preparing octreotide and derivatives thereof

This invention is a novel synthesis of BCA-peptides (BCA: bifunctional chelating agents). In this method, the starting material--Fmoc-Thr(ol)-Terephthal-Acetal-Amide Resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)-Terephtha l-Acetal-Amide Resin was obtained. This compound reacted with iodine to give disulfide-containing peptide resin of ##STR1## Cleavage of the peptide from the resin was achieved by TFA. The cleavaged peptide was protected by the reaction of octreotide with di-t-butyldicarbonate. BCA was coupled to the selectively protected octreotide. This product was obtained by reaction of protected BCA-peptides with TFA. The final product was labeled by radioisotope .sup.111 InCl.sub.3 for tumor imaging radiopharmaceuticals.

Method for synthesis of bifunctional chelating agents-peptides

Novel tumor imaging agents in which the dimercaptosuccinic acid was dissolved in phosphate buffer and labelled with radioisotope gallium. The product of gallium dimercaptosuccinate has been characterized by a variety of experiments including serum stability, biodistribution and imaging experiment. As the results, the compound of gallium dimercaptosuccinate has been confirmed as a novel radiopharmaceutical for tumor imaging agent.

Gallium dimercaptosuccinate as a novel tumor imaging agent

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Taoyuan, Taiwan

Shyh-Yi Chyi