草酸置于silver Nitrate,四乙基碘化铵体系中,用 水 作为反应溶剂,化学反应 90.0H,以54%的收率获得产物奥沙利铂 参考文献: Oxaliplatin With A Low Content Of Accompanying Impurities And A Method For Preparation Thereof[fr] Oxaliplatine Presentant Une Faible Teneur En Impuretes,Et Son Procede De Preparation 标题: Oxaliplatin With A Low Content Of Accompanying Impurities And A Method For Preparation Thereof[fr] Oxaliplatine Presentant Une Faible Teneur En Impuretes,Et Son Procede De Preparation 摘要:奥沙利铂含有低含量的伴生杂质,来源于其制备过程,按重量计,最多含有0.01%,最好少于0.001%的碱金属,最多含有0.0005%,最好少于0.0002%的银,以及最多含有0.01%,最好少于0.001%的硝酸盐.制备上述奥沙利铂的方法在于,将(Sp-4-2)-二氯化-[(1R,2R)-1,2-环己二胺-N,N`]铂(II)的悬浮液在水中处理,然后经过去除固相后,所得溶液与化学式为(R)4Ni的季铵碘化物处理,去除分离的固相,将所得溶液与草酸处理,分离的奥沙利铂被分离出来,用水和极性有机溶剂或它们的混合物洗涤,干燥,从水中再结晶,用水和极性有机溶剂或它们的混合物洗涤,然后干燥.
专利号:WO-2024104433-A9 优先权日:2022-11-16 标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament 发明人:ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING 权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING 摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.
专利号:US-10975069-B2 优先权日:2014-04-01 标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof 发明人:HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN 权利人:UNIV WASHINGTON 摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
专利号:US-2025009786-A1 优先权日:2021-09-30 标 题 :Automated synthesis of polymeric dual drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
专利号:US-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:EP-3030516-B1 优先权日:2013-08-07 标题:The synthesis of core-shell metal-semiconductor nanomaterials 发明人:REVAPRASADU NEERISH; DUNPALL REKHA 权利人:UNIV OF ZULULAND
专利号:US-2024350645-A1 优先权日:2021-07-22 标 题 :Automated synthesis of polymeric drugs 发明人:MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL 权利人:SONY GROUP CORP 摘要:Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein L 1 , L 2 , L 3 , R 1 R 2 , M, p, q, m, and n are as defined herein. Additional compounds, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.
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合成参考文献
摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355