[2-{2-(T-Butoxycarbonylamino)Ethoxy}Ethyl]Methane Sulfonate置于sodium Azide,三苯基膦体系中,用 四氢呋喃,水,N,N-二甲基甲酰胺 用作溶剂,化学反应生成[2-(2-氨基乙氧基)乙基]氨基甲酸叔丁酯 参考文献:Peptide Nucleic Acid Derivatives With Good Cell Penetration And Strong Affinity For Nucleic Acid 标题:Peptide Nucleic Acid Derivatives With Good Cell Penetration And Strong Affinity For Nucleic Acid 摘要:本发明提供了一类新型的肽核酸衍生物,它们具有非常好的细胞穿透性和对核酸的强结合亲和力.
专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:US-8420850-B2 优先权日:2010-05-14 标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers 发明人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE 权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA 摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.
专利号:US-6486350-B1 优先权日:1998-09-30 标 题:Biological reagents and methods for determining the mechanism in the generation of β-amyloid peptide 发明人:AUDIA JAMES E; HYSLOP PAUL A; NISSEN JEFFREY S; THOMPSON RICHARD C; TUNG JAY S; TANNER LAURA I 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are biological reagents which comprise compounds that inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of beta-amyloid peptide.
专利号:US-12054471-B2 优先权日:2018-07-13 标题:Thiocycloheptyne derivatives and their use 发明人:WETERINGS JOSEPHUS JOHANNES; RIJCKEN CRISTIANNE JOHANNA FERDINAND 权利人:CRISTAL DELIVERY B V 摘要:The present invention pertains to novel thiocycloheptyne derivatives of general formula (I): and in particular to thiacycloalkynesulfoimine derivatives and their synthesis. The invention also relates to the use of the novel thiocycloheptyne derivatives in coupling reactions with linkers and drugs. The invention further relates to the use of the novel thiocycloheptynes in bioorthogonal (copper-free) click reactions. The invention further pertains to the use of the novel thiocycloheptyne derivatives in the generation of advanced multifunctional drug delivery systems (drug-loaded) nanoparticles.
1: Pignatello R, Impallomeni G, Pistarà V, Cupri S, Graziano AC, Cardile V, Ballistreri A. New amphiphilic derivatives of poly(ethylene glycol) (PEG) as surface modifiers of colloidal drug carriers. III. Lipoamino acid conjugates with carboxy- and amino-PEG(5000) polymers. Mater Sci Eng C Mater Biol Appl. 2015 Jan;46:470-81. doi: 10.1016/j.msec.2014.10.054. Epub 2014 Oct 23. doi: 10.1039/c0cc02615h. Epub 2010 Nov 26. doi: 10.1016/j.jpba.2010.07.008. Epub 2010 Aug 1. doi: 10.1039/b811818c. Epub 2008 Sep 16.
合成参考文献
参考文献:10.1007/s00044-025-03434-0 摘要:Shi R, Zhang P, Chen M, Lu W, Xu M, Zeng H, He J, Wang Y, Lin Y, Liu J. Dual-PROTACs based on natural product derivative potassium dehydrographolide succinate: design, synthesis, and antitumor activity of a novel EGFR degrader. Med Chem Res. 2025 Jun 30;34(8):1695–713. doi: 10.1007/s00044-025-03434-0.