http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2016065435-A2

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filingDate 2015-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_db77841f6c31c533c9486146658fc18a
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publicationDate 2016-05-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2016065435-A2
titleOfInvention Methods for low temperature fluorine-18 radiolabeling of biomolecules
abstract New chelators such as H 3 L1, H 3 L2, H 3 L3, H 3 L26 and derivatives were synthesized for the complexation of {Al 18 F} 2+ . These new chelators are able to complex {AI 18 F} 2+ with good radiochemical yields using a labeling temperature of 37 °C. The stability of the new Al 18 F- complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI 18 F-L3 and AI 18 F-L26 showed a stability comparable to that of the previously reported Al 18 F-NODA. Moreover, the biodistribution of Al 18 F-L3 and AI 18 F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H 3 L3 and Al 18 F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with 18 F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI 18 F} 2+ with new chelators and obtained very favourable radiochemical yields (> 85%) using a labeling temperature of 37 °C. The stability of the new Al 18 F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37 °C, where AI 18 F-L3 and AI 18 F-L26 showed a stability comparable to that of the previously reported Al 18 F-NODA. Moreover, the biodistribution of Al 18 F-L3 and Al 18 F-L26 showed high stability, since only very limited bone uptake- which would be an indication of release of fluorine-18 in the form of fluoride- was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H 3 L3 and H 3 L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with 18 F-fluorine and several derivatives have been synthesized.
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http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IT-201900003905-A1
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http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2023076938-A1
priorityDate 2014-10-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID456171974
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691156
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419519717
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691155
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691154
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID467330603
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691153
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID57181882
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458395503
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID85309
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691152
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID12049464
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691167
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID53852069
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691166
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID7397
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691165
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226489683
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691163
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID66633189
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID22497
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691162
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691161
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID450502338
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID426015736
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691160
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226607190
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID5360835
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID78934
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID21896526
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226492018
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID12069279
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID23929
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID424440445
http://rdf.ncbi.nlm.nih.gov/pubchem/gene/GID419011
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID95695
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID31251
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID23007
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID152317
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID416224543
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691191
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID316691190

Total number of triples: 348.