(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
US9133143B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Sep 14, 2010 |
| Grant date | Sep 15, 2015 |
| Priority date | — |
| Expiry date | Dec 9, 2030 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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 β-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 β-amyloid peptide conjugates to inhibit the generation of malignant high molecular β-amyloid plaque, and thus can be effectively used as a therapeutic agent for neurodegenerative brain diseases such as Alzheimer's disease.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.