Invention Grant
- Patent Title: Hydroxamic acid type contrast agent containing radioisotope fluoride, preparation method and application thereof
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Application No.: US15795600Application Date: 2017-10-27
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Publication No.: US10538486B2Publication Date: 2020-01-21
- Inventor: Mei-Hui Wang , Chia-Yu Hu , Mao-Chi Weng , Jyun-Hong Chen , Chun-Hung Yang , Hung-Man Yu
- Applicant: Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan, R.O.C.
- Applicant Address: TW Taoyuan
- Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN. R.O.C
- Current Assignee: INSTITUTE OF NUCLEAR ENERGY RESEARCH, ATOMIC ENERGY COUNCIL, EXECUTIVE YUAN. R.O.C
- Current Assignee Address: TW Taoyuan
- Agency: Locke Lord LLP
- Agent Tim Tingkang Xia, Esq.
- Priority: TW106134788A 20171011
- Main IPC: A61K51/00
- IPC: A61K51/00 ; A61M36/14 ; C07C259/06 ; C07B59/00 ; A61K51/04 ; C07C205/37

Abstract:
The present invention relates to a hydroxamic acid-based contrast agent containing an isotope of fluorine, which comprises a compound having a structure of Formula (III): wherein R1 represents radioactive fluorine-18 (18F) or isotope fluorine-19 (19F), and R2 represents hydroxyamine —(NH)OH. The hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention has the capability of selectively inhibiting histone deacetylase (HDAC) subtypes 8/6/3, and specifically targets to the focus of spinocerebellar ataxia with over-activation of HDAC. By labeling with the radioisotope fluorine-18, a positron emission tomography (PET) image is obtained with the hydroxamic acid-based contrast agent containing radioisotope fluorine-18, whereby spinocerebellar ataxia is effectively detected. Therefore, the hydroxamic acid-based contrast agent containing an isotope of fluorine provided in the present invention is potentially useful as a probe for early diagnosis and evaluation of the therapeutic effect of spinocerebellar ataxia.
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