http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11542234-B2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5a38cf3fa46b43121a3aa71c650befb7 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-82 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B59-002 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B59-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61M36-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K51-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K51-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-82 |
| filingDate | 2019-03-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2023-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2c3b061fe29c3128df7690fe2bfe471a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_68d1fbae075473b6c13ad784457cc0bc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c766f6732511822e10b596f29a23da86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_353694dddb4f06b0c663e32725e82676 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_74e86f92dd3550ab67af269d4b986056 |
| publicationDate | 2023-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-11542234-B2 |
| titleOfInvention | 2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues |
| abstract | 6-[ 18 F]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 [ 18 F]DCFPyL, [ 68 Ga]HBED-CC-PSMA, [ 18 F]PSMA-1007 and [Al 18 F]HBED-CC-PSMA. Unexpectedly, the 6-[ 18 F]fluoro-2-alkoxy and 6-[ 18 F]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 [ 18 F]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. Especially, the 18 F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[ 18 F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [ 68 Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques. |
| priorityDate | 2018-03-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 262.