2-((2-(Piperidin-1-yl)Ethyl)Disulfanyl)Ethyl(1As,8S,8Ar,8Bs)-6-Amino-8-((Carbamoyloxy)Methyl)-8A-Methoxy-5-Methyl-4,7-Dioxo-1A,4,7,8,8A,8B-Hexahydroazirino [2',3':3,4]Pyrrolo[1,2-A]Indole-1(2H)-Carboxylate置于l-半胱氨酸盐酸盐无水物体系中,用 乙醇,水 作为反应溶剂,化学反应 2.0H,以92%的收率获得产物丝裂霉素 C 参考文献: Mitomycin C Prodrug Liposome Formulations And Uses Thereof[fr] Formulations De Liposome De Promédicament De Mitomycine C Et Leurs Utilisations 标题: Mitomycin C Prodrug Liposome Formulations And Uses Thereof[fr] Formulations De Liposome De Promédicament De Mitomycine C Et Leurs Utilisations 摘要:本发明提供了用于治疗癌症的mmc前药化合物和脂质体mmc前药及其组合物.该组合物包括含有磷脂酰胆碱脂质,固醇,Peg-脂质和mmc前药的脂质体.本发明还提供了用于治疗癌症的脂质体组合物,包括向需要的患者施用脂质体,其中脂质体包括:磷脂酰胆碱脂质;固醇;peg-脂质和mmc前药或其药用可接受的盐.
专利号:US-5523411-A 优先权日:1994-03-14 标题 :Synthesis of mitomycin and its analogs 发明人:JIMENEZ LESLIE; WANG ZHENG 权利人:UNIV RUTGERS 摘要:The present invention relates to the synthesis of mitomycin and analogs thereof that are useful as anticancer antibiotics. The invention further relates to analogs of mitomycin, which can be prepared according to the methods of synthesis provided. The synthetic method of the invention provides for reacting a derivitized indole with a dialkylvinylsulfonium salt to yield a tricyclic skeleton having the precursors of the fourth ring in one step, followed by an oxidation step or steps to close the fourth ring and prepare mitomycin or a related compound.
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:US-10975048-B2 优先权日:2015-12-14 标题 :Composition of 1,3,4-selenadiazole containing compounds with pharmacological activity 发明人:RUAN BENFANG HELEN; RUAN JENNIFER JIN 权利人:HANGZHOU JENNIFER BIOTECH CO LTD 摘要:The invention belongs to the field of biomedical research involving the 1,3,4-selenyldiazo derivatives that have cell protective activity. Because there are not so many heterocyclic selenium compounds, we synthesized a new type of selenium analog of BPTES. As the isoacceptor of BPTES, the compounds have antitumor activity, anti-oxidation and cell protection function. Currently many drugs contain the thiodiazo motif, so synthesis of selenyldiazo functional group could further optimize these drugs and are important in new drug development and application.