Predicate |
Object |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0468 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61B6-037 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D235-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D235-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D411-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-62 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-78 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-76 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K36-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D243-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-62 |
filingDate |
2015-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate |
2019-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate |
2019-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
CN-106458935-B |
titleOfInvention |
Radiolabeled tracers for poly(ADP-ribose) polymerase-1 (PARP-1), methods and uses thereof |
abstract |
PARP-1 inhibitors are disclosed that can be labeled with 18 F for use as tracers for positron emission tomography (PET) imaging. Synthetic methods are also disclosed. In the synthesized compound, 2-[p-(2-fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]tridecane-2,4(13) , 5,7-tetraene-9-one (12) had the highest inhibitory potency against PARP-1 (IC 50 =6.3 nM). The synthesis of [ 18 F]-12 with high specific activity and 40-50% decay-corrected yield under conventional conditions is disclosed. [ 18 F]-12 accumulation in tumors was confirmed using micro-PET imaging of [ 18 F ]-12 in MDA-MB-436 tumor-bearing mice. Binding can be blocked by olaparib. The compound can be used for tumor imaging. |
priorityDate |
2014-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |