专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-9549995-B2 优先权日:2012-03-26 标 题:Efficient synthesis of ethylenedicysteine-sugar conjugates for imaging and therapy 发明人:YANG DAVID J; YU DONG-FANG 权利人:UNIV TEXAS 摘要:Novel methods of synthesis of ethylenedicysteine-sugar conjugates and therapeutic and diagnostic applications of such conjugates are disclosed. Methods of synthesizing these conjugates in high purity are also presented as using starting materials such as thiazolidine carboxylic acid. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these conjugates prepared herein, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-8147805-B2 优先权日:2005-01-05 标题:Conjugates for dual imaging and radiochemotherapy: composition, manufacturing, and applications 发明人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND 权利人:YANG DAVID; YU DONGFANG; CHANDA MITHU; AZHDARINIA ALI; OH CHANGSOK; KIM E EDMUND; UNIV T EXAS SYSTEM BOARD OF REGENTS 摘要:Compositions and methods for dual imaging and for dual chemotherapy and radiotherapy are disclosed. More particularly, the invention concerns compounds comprising the structure X 1 —Y—X 2 , wherein Y comprises two or more carbohydrate residues covalently attached to one another, X 1 and X 2 are diagnostic or therapeutic moieties covalently attached to Y, provided that when Y does not comprise a glucosamine residue, X 1 and X 2 are diagnostic moieties. The present invention also concerns methods of synthesis of these compounds, application of such compounds for dual imaging and treatment of hyperproliferative disease, and kits for preparing a radiolabeled therapeutic or diagnostic compound.
专利号:US-6888019-B1 优先权日:2004-02-25 标题 :Method of preparing rhenium complex using borohydride exchange resin 发明人:PARK SANG HYUN; PARK KYUNG BAE; CHOI SUN JU 权利人:KOREA ATOMIC ENERGY RES 摘要:Disclosed is a method of preparing a rhenium complex by use of a borohydride exchange resin, including dissolving perrhenic acid in a solution containing ethylenediamine tetraacetate, mannitol and stannous chloride to obtain a perrhenic acid solution (step 1), which is then mixed with disulfide in the presence of a borohydride exchange resin and reacts at room temperature, to obtain a rhenium complex (step 2). The preparation method of the current invention is characterized in that rhenium is reduced to have a desired oxidation number through the dissolving of the step 1, whereby the reaction of the step 2 can occur at room temperature. In addition, use of the borohydride exchange resin as a reducing agent results in direct formation of the rhenium complex of sulfide from disulfide, without the need of synthesis of thiol-protected S-precursor. Therefore, radioactive pharmaceuticals having high values can be economically and efficiently produced.
专利号:US-2007196275-A1 优先权日:2001-04-26 标题 :Diagnostic Imaging Compositions, Their Methods Of Synthesis And Use 发明人:LI CHUN; WEN XIAOXIA; WU QING-PING; WALLACE SIDNEY; ELLIS LEE M 权利人:LI CHUN; WEN XIAOXIA; WU QING-PING; WALLACE SIDNEY; ELLIS LEE M 摘要:Conjugate molecules comprising a ligand bonded to a polymer are disclosed. One such conjugate molecule comprises a ligand bonded to a polymer, a chelating agent bonded to the polymer, and a radioisotope chelated to the chelating agent. The conjugate molecules may be useful in detecting and/or treating tumors or biological receptors. These conjugate molecules may be synthesized without the necessity of preactivation of the ligand using an SCN-polymer-chelating agent precursor. Conjugate molecules incorporating an annexin V ligand are particularly useful for visualizing apoptotic cells. Conjugate molecules incorporating a C225 ligand are particularly useful for targeting tumors expressing EGFR.
专利号:US-10814013-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
1: Aggarwal P, Gunasekaran V, Gowtham M, Mahajan JK, Sood A, Mittal BR, Menon P, Peters NJ, Malik MA, Bhattacharya A. Assessment of post-pyeloplasty renal drainage in antenatally detected hydronephrosis by 99mTc-L, L-Ethylenedicysteine renal scintigraphy: the importance of delayed imaging. Ann Nucl Med. 2025 Mar;39(3):266-272. doi: 10.1007/s12149-024-01994-6. Epub 2024 Nov 1. 58(2):52-61. doi: 10.1007/s13139-023-00823-4. Epub 2023 Sep 25. 3: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Technetium Tc 99m Ethylenedicysteine. 2023 Nov 15. 43(12):1171-1180. doi: 10.1097/MNM.0000000000001618. Epub 2022 Oct 17. 36(1):21-24. doi: 10.4103/ijnm.IJNM_94_20. Epub 2021 Mar 4. 6: Vadi SK, Bhattacharya A, Sood A, Mittal BR. Acute urinary obstruction during 99mTc-ethylenedicysteine diuretic renal scintigraphy acquisition: Is furosemide the culprit? World J Nucl Med. 2020 Jan 14;19(1):82-84. doi: 10.4103/wjnm.WJNM_30_19.
合成参考文献
参考文献:10.1007/s13139-010-0056-6 摘要:Shetty D, Lee Y, Jeong JM. 68Ga-Labeled Radiopharmaceuticals for Positron Emission Tomography. Nuclear Medicine and Molecular Imaging. 2010 Oct 12;44(4):233–40. doi: 10.1007/s13139-010-0056-6.