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

Institute of Nuclear Energy Research

Han-Chih Chang

Ming-Hsin Li

Chyng-Yann Shiue

Chun-Fang Feng

Han-Hsiang Chu

Method provided for labeling a nuclear medicine for imaging tracing, comprising a labeling precursor of the HDAC inhibitor BNL-26 (C22H23N3O) and the derivatives that are separated into two classes. The first class comprises a BNL-26 (C22H23N3O) and derivatives BNL-26a (C21H21N3O), BNL-26b (C22H22N2O), and other compounds of the labeling precursors which are categorized into two parts, the first part includes BNL-26-CH2CH2OTs (C31H33N3O4S), BNL-26a-CH2CH2OTs (C30H31N3O4S), and BNL-26b-CH2CH2OTs (C31H32N2O4S), which provides labeling precursor through &#x2014;CH2CH2OTs structure, and the second part includes pre-BNL-26 (C28H34N3O3B), pre-BNL-26a (C27H32N3O3B), pre-BNL-26b (C28H33N2O3B), which provides labeling precursor through 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl structure. The second class includes BNL-26 (C22H23N3O) indole/indoline, which provides a series of derivative labeling precursors derived from a secondary amide bond.

Precursor of a histone deacetylase inhibitor PET imaging compound for tracking cerebral neurodegenerative and tumor diseases

The present invention relates to a group of compounds for nuclear medicine imaging through F-18 labeled histone acetylation inhibitors (HDACi) of indole or indoline benzoyl amine and its derivatives, and provides a series of nuclear medicine imaging agents that bind with HDAC overexpression in vivo for diagnosis of malignant tumors discovered in the nuclear medicine imaging tracing.

Compound and analogues for tracing histone acetylation inhibitors PET imaging for diagnosis and treatment of tumors

A method of synthesizing a compound of imaging agent with HDAC (histone deacetylase) inhibitor consists of two parts, the first part of the method is to provide the inhibitor of HDAC with a compound of imaging agent that includes HDAC inhibitor BNL-26 (CHNO) and its analogs to be labeled with radionuclide F-18, producing a series of new nuclear medicine tracers: BNL-26-CHCH18F, BNL-26a-CHCH18FF, BNL-26b-CHCH18F, BNL-26c-CHCH18F and BNL-26d-CHCH18F. These nuclear medicine with imaging agents can be used as a tracer in vivo binding to over-expression HDAC and produce a HDAC nuclear medicine imaging effect to serve for clinical diagnosis. The second part of the method is to provide a slightly adjusted a structural framework of BNL-26 and use pyridine to substitute the benzene ring of the BNL-26 structure, and then synthesize with other substituent to produce a series of additional 30 more HDAC inhibitors, named from Iner-1 to Iner-30 compounds.

Growing community of inventors

Taoyuan, Taiwan

Han-Chih Chang