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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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2.发明申请公开(公告)号：US20200237938A1
公开(公告)日：2020-07-30
申请号：US16215647
申请日：2018-12-11
申请人： Ming-Hsin Li , Su-Jung Chen , Ming-Wei Chen , Yuan-Ruei Huang , Shih-Ying Lee , Chun-Fang Feng , Sheng-Nan Lo , Chih-Hsien Chang
发明人： Ming-Hsin Li , Su-Jung Chen , Ming-Wei Chen , Yuan-Ruei Huang , Shih-Ying Lee , Chun-Fang Feng , Sheng-Nan Lo , Chih-Hsien Chang
摘要： The present invention provides a radioactive labeling method for neuropeptide Y (NPY) compound and a mammalian diagnostic radioactive targeting medicine with NPY peptide being modified at position 27th to 36th, and after binding with the chelating agent and labeling the radiation nucleus 66Ga, 67Ga, 68Ga, 177Lu or 111In to provide a radioactive targeting medicine for multi-type breast cancer diagnosis and treatment.
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3.发明申请公开(公告)号：US20200078478A1
公开(公告)日：2020-03-12
申请号：US16125787
申请日：2018-09-10
申请人： Ming-Hsin Li , Ming-Wei Chen , Shin-Min Wang , Shih-Wei Lo , Chun-Fang Feng , Cheng-Hui Chuang , Sheng-Nan Lo
发明人： Ming-Hsin Li , Ming-Wei Chen , Shin-Min Wang , Shih-Wei Lo , Chun-Fang Feng , Cheng-Hui Chuang , Sheng-Nan Lo
IPC分类号： A61K51/04
摘要： A PSMA targeting peptide derivative for radiotherapy, which is a structural molecule developed for diagnosis or treatment of prostate cancer, as prostate-specific membrane antigen (PSMA) is a protein present on the surface of healthy prostate cells, which is often at a high level of expression on the surface of prostate cancer cells, and the molecular composition of PSMA inhibitor is mainly composed of glutamic acid, urea and lysine, in addition to the linker of the present invention, PSMA inhibitor can be combined with a chelating agent and truncated Evans Blue, which can be labeled with radionuclides Ga-67, Ga-68, In-111, Lu-177, Cu-64 or Y-90, used for image analysis and analysis of human prostate cancer tumor pattern as a new PSMA targeting peptide receptor radionuclide therapy (PRRT), and which has a longer half-life in vivo and is featured by specific binding of PSMA for radiotherapy diagnosis or treatment.
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公开(公告)号：US11850291B2
公开(公告)日：2023-12-26
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
CPC分类号： A61K51/088
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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6.发明申请公开(公告)号：US20220227728A1
公开(公告)日：2022-07-21
申请号：US17152344
申请日：2021-01-19
申请人： MING-HSIN LI , KAI-HUNG CHENG , SHENG-NAN LO , SHIH-WEI LO , YUAN-RUEI HUANG , JENN-TZONG CHEN
发明人： MING-HSIN LI , KAI-HUNG CHENG , SHENG-NAN LO , SHIH-WEI LO , YUAN-RUEI HUANG , JENN-TZONG CHEN
IPC分类号： C07D401/04 , A61K51/04
摘要： The present invention discloses a series of nuclear medicine tracers that are combined with brain microtubule-associated protein Tau targeting compounds to produce a group of compounds of nuclear medicine that can be utilized for imaging of microtubule-associated protein Tau. When the positrons released by the decay encounter the electrons of the cells in the sample, utilizing the positron decay characteristics of fluorine-18 or iodine-124 isotope to generate mutual destruction reactions, a pair of opposite gamma rays is formed which are imaged by positron emission tomography. The compounds can be applied for the in vivo detection of microtubule-associated protein Tau deposits in the brain. The invention provides a strategy for diagnosis of Alzheimer's disease and a method to measure the efficacy of therapeutic drugs targeting microtubule-associated protein Tau.
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公开(公告)号：US11077217B2
公开(公告)日：2021-08-03
申请号：US16215647
申请日：2018-12-11
申请人： Ming-Hsin Li , Su-Jung Chen , Ming-Wei Chen , Yuan-Ruei Huang , Shih-Ying Lee , Chun-Fang Feng , Sheng-Nan Lo , Chih-Hsien Chang
发明人： Ming-Hsin Li , Su-Jung Chen , Ming-Wei Chen , Yuan-Ruei Huang , Shih-Ying Lee , Chun-Fang Feng , Sheng-Nan Lo , Chih-Hsien Chang
摘要： The present invention provides a radioactive labeling method for neuropeptide Y (NPY) compound and a mammalian diagnostic radioactive targeting medicine with NPY peptide being modified at position 27th to 36th, and after binding with the chelating agent and labeling the radiation nucleus 66Ga67Ga68Ga177Lu or 111In to provide a radioactive targeting medicine for multi-type breast cancer diagnosis and treatment.
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