4-(N-叔丁氧羰基氨基)-1-丁醇置于tea,Lithium Bromide体系中,用 二氯甲烷,丙酮 用作溶剂,化学反应 7.0H,反应生成N-(4-溴丁基)氨基甲酸叔丁酯 参考文献:Zn2+ Fluorescent Chemosensors And The Influence Of Their Spacer Length On Tuning Zn2+ Selectivityelectronic Supplementary Information (Esi) Available: Job Plot,Partial 1H NMR Spectra Of Free 3 And The 3-zn2+ Complex,Ca2+ And Mg2+ Interference For Zn2+ Sensing Of 3,Kd Measurements,And Buffer Preparation. See Http://www.Rsc.Orgpdata/p2/b2/b200462C/ 标题:Zn2+ Fluorescent Chemosensors And The Influence Of Their Spacer Length On Tuning Zn2+ Selectivityelectronic Supplementary Information (Esi) Available: Job Plot,Partial 1H NMR Spectra Of Free 3 And The 3-zn2+ Complex,Ca2+ And Mg2+ Interference For Zn2+ Sensing Of 3,Kd Measurements,And Buffer Preparation. See Http://www.Rsc.Orgpdata/p2/b2/b200462C/ 摘要:基于配位增强荧光(chef)机制的zn2+荧光化学传感器被制备出来,并通过控制间隔基长度实现了对zn2+选择性的精细调节.对金属离子的荧光发射响应显示,Co2+,Cu2+和ni2+使荧光减弱,而ca2+,Cd2+和zn2+使荧光增强.在3号传感器中实现了对zn2+的最大选择性,优于ca2+和cd2+.基本结合特性(化学计量比,表观解离常数和ph依赖性)通过荧光光谱法测量.3号传感器与zn2+的job图分析表明形成了1:1的复合物.表观解离常数kd在ph 7.5时为0.98(+/-0.43)nm [50 Mm Hepes缓冲液,I = 0.1 (Nano3)].在ph超过7的区域,2号传感器及其与zn2+的复合物的荧光强度平稳,表明荧光测量受生理ph变化的影响不大. Doi:10.1039/b200462C
专利号:WO-2024260325-A1 优先权日:2023-06-19 标题 :Synthesis of macrocyclic compound and medical use of macrocyclic compound 发明人:LU HONGFU; DING XIAO; REN FENG 权利人:INSILICO MEDICINE IP LTD 摘要:Provided in the present invention are the synthesis of a macrocyclic compound and the medical use of the macrocyclic compound. Specifically, provided in the present invention are a compound as show in formula (II), a stereoisomer thereof or a pharmaceutically acceptable salt thereof, which can be used as a CDK7 inhibitor.
专利号:US-12337036-B2 优先权日:2018-01-01 标题:Compounds and methods for trans-membrane delivery of molecules 发明人:ZIV ILAN; GRIMBERG HAGIT; DUBROVSKY JOSEPH 权利人:APOSENSE LTD 摘要:The Invention provides a novel delivery system for delivery of drugs across biological membranes. It provides novel chemical conjugates that comprise said delivery system, methods for synthesis of said compounds, and methods for utilization of said delivery system, among others, for delivery of genetic drugs into tissues and cells, in vitro, ex vivo, and in vivo, for the treatment of various medical disorders.
专利号:US-9115172-B2 优先权日:2007-01-11 标 题 :Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:D SOUZA CHRISTOPHER A; MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 18 F- or 19 F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18 F- or 19 F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.
专利号:US-2016045626-A1 优先权日:2007-01-11 标题 :Methods and Compositions for Improved Labeling of Targeting Peptides 发明人:MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a therapeutic or diagnostic isotope, such as 61 Cu, 62 Cu, 64 Cu, 67 Cu, 18 F, 19 F, 66 Ga, 67 Ga, 68 Ga, 72 Ga, 111 In, 177 Lu, 44 Sc, 47 Sc, 86 Y, 88 Y, 90 Y, 45 Ti or 89 Zr, preferably 18 F or 19 F. More preferably, the targeting peptide is NOTA-octreotate, NOTA-MPAA-octreotate, pyridine-NOTA-octreotate or triazole-NOTA-octreotate. The labeled targeting peptides may be used for detection, diagnosis, imaging and/or treatment of sst 2 + tumors, such as neuroendocrine tumors.
专利号:US-9028800-B2 优先权日:2007-01-11 标 题 :Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:D SOUZA CHRISTOPHER A; MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 18 F or 19 F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may be directly or indirectly attached to the targeting molecule. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the labeled molecule may be used for imaging in a subject without purification after labeling.
专利号:US-8709382-B2 优先权日:2007-01-11 标 题:Methods and compositions for improved F-18 labeling of proteins, peptides and other molecules 发明人:D SOUZA CHRISTOPHER A; MCBRIDE WILLIAM J; GOLDENBERG DAVID M 权利人:IMMUNOMEDICS INC 摘要:The present application discloses compositions and methods of synthesis and use of 18 F- or 19 F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18 F- or 19 F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.
1. Dang Z, Xie H, Zhu L, Zhang Q, Li Z, Huang L, Chen CH. Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors. ACS Med Chem Lett. 2017 Oct 9;8(11):1199-1203. doi: 10.1021/acsmedchemlett.7b00376. 2. https://pubs.rsc.org/en/content/articlelanding/2015/ra/c5ra12114k 3. Spadoni G, Bedini A, Furiassi L, Mari M, Mor M, Scalvini L, Lodola A, Ghidini A, Lucini V, Dugnani S, Scaglione F, Piomelli D, Jung KM, Supuran CT, Lucarini L, Durante M, Sgambellone S, Masini E, Rivara S. Identification of Bivalent Ligands with Melatonin Receptor Agonist and Fatty Acid Amide Hydrolase (FAAH) Inhibitory Activity That Exhibit Ocular Hypotensive Effect in the Rabbit. J Med Chem. 2018 Sep 13;61(17):7902-7916. doi: 10.1021/acs.jmedchem.8b00893. Epub 2018 Sep 4.
合成参考文献
参考文献:10.1007/s12149-020-01573-5 摘要:Shimizu Y, Nakai Y, Iikuni S, Watanabe H, Nakamoto Y, Ono M. Synthesis and evaluation of gallium-68-labeled nitroimidazole-based imaging probes for PET diagnosis of tumor hypoxia. Annals of Nuclear Medicine. 2021 Jan 09;35(3):360–9. doi: 10.1007/s12149-020-01573-5.