Intermediates for fluorinated tetrabenazine carbinol compounds imaging agents and probes
US7919622B2 · kind B2 · utility
Inventors
Key dates
| Filing date | Dec 7, 2007 |
| Grant date | Apr 5, 2011 |
| Priority date | — |
| Expiry date | Jan 24, 2030 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/05
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The present invention provides novel fluorophilic compounds having structure VIIwherein R1 is a C1-C20 aliphatic, a C2-C20 cycloaliphatic, or a C2-C20 aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2 is a C1-C10 aliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; R4 is hydrogen or a C1-C10 aliphatic radical; and R5 is hydrogen, a C1-C10 aliphatic radical, a C2-C10 cycloaliphatic radical, or a C2-C20 aromatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.