6-[2-(叔丁氧羰基)肼基]烟酸置于盐酸体系中,化学反应 16.0H,反应生成6-肼基烟酸 参考文献:Trifluoroacetyl-Hynic Peptides: Synthesis And 99Mtc Radiolabeling 标题:Trifluoroacetyl-Hynic Peptides: Synthesis And 99Mtc Radiolabeling 摘要:Fmoc-Lys(Hynic-Boc)-Oh,A Precursor For Solid-Phase Synthesis Of Tc-99M-Labeled Peptides,Was Synthesized Efficiently Without HPLC Purification. HPLC-Esms Showed That Deprotection And Decoupling Of Peptide From The Resin With Trifluoroacetic Acid Gave Initially Hynic-Peptide,Which Was Trifluoroacetylated Upon Prolonged Incubation. The Trifluoroacetyl-Hynic Group Was Hydrolyzed During Tc-99M Labeling,Rendering Deprotection Unnecessary. Trifluoroacetyl-Hynic Peptide Was Tc-99M-Labeled As Efficiently,Producing The Same Product,As Hynic-Peptide. These Modifications Enhance The Versatility Of Hynic For Tc-99M Peptide Labeling. Doi:10.1021/jm061274L
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:WO-0021982-A1 优先权日:1998-10-13 标 题:A process for the preparation of a thrombus imaging agent 发明人:BISHOP JOHN 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to the synthesis of reagents useful for the preparation of radiopharmaceuticals which serve as imaging agents for the diagnosis of cardiovascular disorders, infection, inflammation, and cancer. They have formula (I). It is also claimed a method for preparing pertinent intermediates.
专利号:WO-2024169886-A1 优先权日:2023-02-16 标 题 :Psma targeted radioactive drug for integrated diagnosis and treatment, and synthesis and use thereof 发明人:YAN CHENGLONG; YU SHANYOU; FANG PENG; ENG WAI-SI; YANG SI 权利人:NORROY BIOSCIENCE CO LTD 摘要:Provided are a PSMA targeted radioactive drug for integrated diagnosis and treatment, and the synthesis and use thereof. Specifically, the present invention relates to a compound or a pharmaceutically acceptable salt, ester or solvate thereof. The structure of the compound is as represented by formula (I). The compound can be used for diagnosing and/or treating one or more tumors, cancers or cells expressing PSMA.
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:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-2011143967-A1 优先权日:2009-12-15 标 题:Surface modifications and methods for their synthesis and use 发明人:MCGALL GLENN H; BARONE ANTHONY D; TRUE RANDALL J 权利人:MCGALL GLENN H; BARONE ANTHONY D; TRUE RANDALL J 摘要:Novel processes are disclosed for forming an array of polymers by functionalizing the surface of particles by methods that include covalently attaching a functionalized silicon compound. Substrates such as microparticles having functionalized silicon compounds attached thereto are produced by introducing at least one carboxyl group directly by silanating a carboxylated silane compound to the surface of a microparticle. In a further aspect of the invention, the silane compound is a dipodal carboxylated silane.
参考文献:10.1021/bc010043k 摘要:Ono M, Arano Y, Mukai T, Saga T, Fujioka Y, Ogawa K, Kawashima H, Konishi J, Saji H. Control of Radioactivity Pharmacokinetics of 99mTc−HYNIC-Labeled Polypeptides Derivatized with Ternary Ligand Complexes. Bioconjugate Chem. 2002 Apr 09;13(3):491–501. doi: 10.1021/bc010043k. 参考文献:10.1021/bc0155566 摘要:Su Z, Liu G, Gupta S, Zhu Z, Rusckowski M, Hnatowich DJ. In Vitro and in Vivo Evaluation of a Technetium-99m-Labeled Cyclic RGD Peptide as a Specific Marker of αVβ3 Integrin for Tumor Imaging. Bioconjugate Chem. 2002 Apr 20;13(3):561–70. doi: 10.1021/bc0155566. 参考文献:10.1089/108497804323071986 摘要:Vermeersch H, Ham H, Rottey S, Lahorte C, Corsetti F, Dierckx R, Steinmetz N, Van de Wiele C. Intraobserver, Interobserver, and Day-to-Day Reproducibility of Quantitative 99m Tc-HYNIC Annexin-V Imaging in Head and Neck Carcinoma. Cancer Biotherapy and Radiopharmaceuticals. 2004 Apr;19(2):205–10. doi: 10.1089/108497804323071986.