Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_00a421ab71bd49a451d0a49d23a082c7 |
classificationCPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2601-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K2123-00 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B59-008 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C331-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-1093 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C259-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D243-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D255-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/G01N33-534 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-088 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K1-13 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0482 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C215-50 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C229-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B59-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-13 |
filingDate |
2015-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_db77841f6c31c533c9486146658fc18a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0f36cae9d52d4cfc079744a1e7fa4d5a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d715524fa330805b9ab193cd39075ad1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_03627dbbfb7bec50e0b75903fa9d8086 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb4b1fa1875b427760145f59ca8fae5c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2bb474c866df7b81a12c3f9e1b49aef9 |
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. |
isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2022167681-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IT-201900003905-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2019166537-A1 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 |