Hydroxamic acid type contrast agent containing radioisotope fluoride, preparation method and application thereof
US10538486B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Oct 27, 2017 |
| Grant date | Jan 21, 2020 |
| Priority date | — |
| Expiry date | Feb 17, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/05
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.