CAS: 33419-42-0; (5R,5Ar,8Ar,9S)-9-(((4Ar,6R,7R,8R,8As)-7,8-Dihydroxy-2-Methylhexahydropyrano[3,2-D][1,3]Dioxin-6-yl)Oxy)-5-(4-Hydroxy-3,5-Dimethoxyphenyl)-5,5A,8A,9-Tetrahydrofuro[3',4':6,7]Naphtho[2,3-D][1,3]Dioxol-6(8H)-One

上下游产品

CAS号270928-23-9 benzyl (4-((5R,... | CAS号23363-35-1 木质素 P | CAS号534-15-6 乙缩醛二甲醇 | CAS号6559-91-7 4'-去甲基表鬼臼毒素 | CAS号23363-33-9 4'-demethyl-4'-... | CAS号23363-34-0 4-(2,3,4,6-tetr... | CAS号3947-62-4 2,3,4,6-四-O-乙酰基... | CAS号23363-35-1 木质素 P | CAS号138261-30-0 2'-chloroetoposide

在 5%-Palladium/activated Carbon,氢气体系中,用 乙酸乙酯 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,以94 %的收率获得产物依托泊苷
参考文献:一种依托泊苷及其类似物的合成方法
标题:一种依托泊苷及其类似物的合成方法
摘要:本发明涉及一种依托泊苷及其类似物的合成方法,包括以下反应步骤:(1)糖基片段(式i)与炔丙基异氰酸酯(式ii)在碱性条件下反应反应生成糖基炔丙氨基碳酸酯给体(式iii);(2)4'‑去甲基表鬼臼毒素分子中4'位酚羟基选择性保护引入r3保护基,得到去甲基表鬼臼毒素衍生物(式iv);(3)糖基炔丙氨基碳酸酯给体(式iii)与4'位羟基保护的表鬼臼毒素类衍生物(式iv)在au(I)催化剂及盐类添加剂的作用下发生糖苷化反应,高选择性的反应生成β‑糖苷(式v);(4)化合物(式v)中的酚羟基保护基(R3)及糖基片段中的羟基保护基(Op)在一定的条件下完全脱除,即可制备依托泊苷及其类似物(式vi).

专利信息

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-2022265691-A1
优先权日:2019-07-12
标 题 :Methods for use of gene expression as an indicator of e-selectin inhibitor efficacy and clinical outcome for multiple tumor types
发明人：MAGNANI JOHN L; FOGLER WILLIAM E; THACKRAY HELEN M; FELDMAN ERIC J; STEWART DAVID
权利人:GLYCOMIMETICS INC
摘要:Cancer patients that express high levels of the E-selectin ligand (sialyl Lea/x) on their tumors have a poorer outcome. Interestingly, relapsed/refractory acute myeloid leukemia (AML) patients expressing high levels of sialyl Lex on their blasts show the greatest therapeutic response when treated with the E-selection inhibitor compound of Formula I. Transcriptome profiling of E-selectin ligand-forming glycosylation genes showed that ST3GAL4 and FUT7 were consistently expressed in the majority of cancers evaluated. Poor survival outcomes of FLT3-mutated AML patients that express high levels of ST3GAL4 and FUT7 implicated E-selectin in this disease state. These genes may be predictive biomarkers in AML patients. Methods of treatment of cancer comprising screening AML patients for expression of genes that contribute to the synthesis of the E-selectin ligand sialyl Lex, then treating those patients with an E-selection inhibitor, are 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-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.