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公开(公告)号:US20210121585A1
公开(公告)日:2021-04-29
申请号:US16663387
申请日:2019-10-25
申请人: MING-HSIN LI , Sheng-Nan Lo , Shih-Wei Lo , Shih-Ying Lee , Su-Jung Chen , Shih-Min Wang , Ming-Wei Chen , Wei-Lin Lo
发明人: MING-HSIN LI , Sheng-Nan Lo , Shih-Wei Lo , Shih-Ying Lee , Su-Jung Chen , Shih-Min Wang , Ming-Wei Chen , Wei-Lin Lo
IPC分类号: A61K51/08
摘要: The invention features a novel precursor provided for radioisotope labeling with ligands for specific binding of prostate-specific membrane antigen (PSMA) for prostate cancer diagnosis and treatment, and the pharmacophore of a PSMA inhibitor composed of three molecules of glutamic acid, urea and lysine is provided with three variable linkers based on pharmacological activity of the PSMA inhibitor for labeling with radioactive nucleus Ga-67, Ga-68, In-111, Lu-177, Cu-64, or Y-90 through a chelating agent for imaging analysis of human tumor models of prostate cancer and serving as a PSMA-targeted radioligand therapy for prostate cancer diseases.
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公开(公告)号:US20220089574A1
公开(公告)日:2022-03-24
申请号:US17027748
申请日:2020-09-22
申请人: MING-HSIN LI , SHENG-NAN LO , SHIH-WEI LO , SHIH-YING LEE , SU-JUNG CHEN , WEI-LIN LO , MING-WEI CHEN , YUAN-RUEI HUANG
发明人: MING-HSIN LI , SHENG-NAN LO , SHIH-WEI LO , SHIH-YING LEE , SU-JUNG CHEN , WEI-LIN LO , MING-WEI CHEN , YUAN-RUEI HUANG
IPC分类号: C07D403/12 , C07F5/00
摘要: The structure and preparation method of a compound D-L2(-B)-L1-A is disclosed, A is a physiologically and pharmacologically active molecule that physically binds to a specific biological molecule or receptor; L1 is a variable structure with the molecular connection activity at both ends connecting to A and L2; L2 is a variable structure, which has three-terminal molecular connection activity connecting to L1, D and B; B is a physiologically and pharmacologically active molecule that binds to albumin, changing the A molecule in the body cyclic characteristics; D is a polycarboxylic macrocyclic structure that binds to radioisotopes; D-L2(-B)-L1-A compound can be used to express chemokine receptor 4 (CXCR4) receptors on cells, tissues, and/or organs, and after binding with radionuclides, it is suitable for detection of CXCR4 protein binding in vitro, detection of CXCR4 cell binding in vitro or detection of CXCR4 expression in in vivo animal imaging.
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