CAS: 1423758-00-2; (((S)-1-Carboxy-5-(6-Fluoronicotinamido)Pentyl)Carbamoyl)-L-Glutamic Acid

专利信息

专利号:US-11851407-B2
优先权日:2016-06-10
标 题 :Synthesis of the radiolabeled prostate-specific membrane antigen (PSMA) inhibitor [18F]DCFPYL
发明人：RAVERT HAYDEN T; HOLT DANIEL P; CHEN YING; MEASE RONNIE C; FAN HONG; POMPER MARTIN G; DANNALS ROBERT F
权利人:UNIV JOHNS HOPKINS; THE JOHNS HOPKINS UNIVERSTY
摘要:Methods, and related compositions, for the improved synthesis of [ 18 F]DCFPyL are disclosed. Also provided are methods, and related compositions, for the use of [ 18 F]DCFPyL so produced.

专利号:US-2025019350-A1
优先权日:2023-06-16
标题 :Synthesis of the prostate specific membrane antigen (psma) radiolabeled inhibitor [18f]dcfpyl
发明人：BENITES PEDRO; ROBINSON SIMON P; SIEGLER ROBERT W
权利人:PROGENICS PHARM INC
摘要:Provided herein are methods and related compositions, including kits, for the improved synthesis, preparation and/or storage of [18F]DCFPyL. Also provided are methods of using [18F]DCFPyL, such as for imaging.

专利号:US-2019151483-A1
优先权日:2016-07-25
标 题:Methods of making 18f-labeled precursors and peptides, labeled c-met binding peptides, and methods of use thereof
发明人：BHATTACHARYYA FALGUNI; SWENSON ROLF; JAGODA ELAINE MARIE
权利人:US HEALTH
摘要:Described herein are novel methods for the synthesis of radiolabeling synthons such as [18F]fluoronicotinic acid-2,3,5,6-tetrafluorophenyl ester, and also methods of labeling a protein or peptide comprising a free amine group. A novel c-Met binding peptide, and imaging methods, are also described.

专利号:US-2019177275-A1
优先权日:2016-06-10
标题:Improved synthesis of the radiolabeled prostate-specific membrane antigen (psma) inhibitor [18f]dcfpyl

专利号:HR-P20250070-T1
优先权日:2016-06-10
标 题 :IMPROVED SYNTHESIS OF THE RADIOACTIVELY LABELED INHIBITOR [18F]DCFPyL OF PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA)

专利号:US-11542234-B2
优先权日:2018-03-16
标题 :2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues
发明人：NEUMAIER BERND; ZLATOPOLSKIY BORIS; KRAPF PHILIPP; RICHARZ RAPHAEL; DRZEZGA ALEXANDER
权利人:UNIV KOELN
摘要: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. Especially, the 18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[18F]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 [68Ga]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.