Patents by Inventor Alexander DRZEZGA

Alexander DRZEZGA has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • 2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues
    Patent number: 11542234
    Abstract: 6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: January 3, 2023
    Assignee: Universität zu Köln
    Inventors: Bernd Neumaier, Boris Zlatopolskiy, Philipp Krapf, Raphael Richarz, Alexander Drzezga
  • 2-Alkoxy-6-[18F]fluoronicotinoyl substituted Lys-C(O)-Glu derivatives as efficient probes for imaging of PSMA expressing tissues
    Publication number: 20210032206
    Abstract: 6-[18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [18F]DCFPyL, [68Ga]HBED-CC-PSMA, [18F]PSMA-1007 and [Al18F]HBED-CC-PSMA. Unexpectedly, the 6-[18F]fluoro-2-alkoxy and 6-[18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues.
    Type: Application
    Filed: March 15, 2019
    Publication date: February 4, 2021
    Applicant: Universität zu Köln
    Inventors: Bernd NEUMAIER, Boris ZLATOPOLSKIY, Philipp KRAPF, Raphael RICHARZ, Alexander DRZEZGA