CAS: 139504-50-0; (14S,16S,32S,33S,2R,4S,10E,12E,14R)-86-Chloro-14-Hydroxy-85,14-Dimethoxy-33,2,7,10-Tetramethyl-12,6-Dioxo-7-Aza-1(6,4)-Oxazinana-3(2,3)-Oxirana-8(1,3)-Benzenacyclotetradecaphane-10,12-Dien-4-Yl N-(3-Mercaptopropanoyl)-N-Methyl-L-Alaninate

上下游产品

2'-deacetyl-N2'-[3-(methyldithio)-1-oxopropyl]maytansineN2'-deacetyl-N2'-[3-(methyldithio)-1-oxopropyl]maytansine N-methyl-N-[(3-methyldithio)-1-oxopropyl]-L-alanine maytansinol ansamit°Cin P-32'-deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine dimerN2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)maytansine dimer 2'-deacetyl-N2'-[3-[[1-[[4-[[[(1S)-5-amino-1-carboxypentyl]amino]carbonyl]cyclohexyl]methyl]-2,5-dioxo-3-pyrrolidinyl]thio]-1-oxopropyl]maytansineN2'-deacetyl-N2'-[3-[[1-[[4-[[[(1S)-5-amino-1-carboxypentyl]amino]carbonyl]cyclohexyl]methyl]-2,5-dioxo-3-pyrrolidinyl]thio]-1-oxopropyl]maytansine

安丝菌素 P 3置于l-1,4-二硫代苏糖醇,Zinc Trifluoromethanesulfonate,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,Lithium-Tri-Methoxy-Alanat,N,N-二异丙基乙胺体系中,用 四氢呋喃,甲醇,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 用作溶剂,化学反应 28.0H,反应生成美登素
参考文献:一种美登素脱氯化物,中间体,其制备方法及应用
标题:一种美登素脱氯化物,中间体,其制备方法及应用
摘要:本发明公开了一种如式i所示的美登素脱氯化物,中间体,其制备方法及应用.本发明提供了一种如式i所示的美登素脱氯化物;其可作为杂质标准品,用于美登素dm1的杂质研究,来建立美登素dm1质量控制的分析方法,以及选择合适方法有效去除该类杂质;有助于提高美登素dm1乃至adc药物的质量和临床应用的安全性和有效性.本发明还提供了一种如式i所示的美登素脱氯化物的制备方法及其中间体.

专利信息

专利号:US-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

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-2024400608-A1
优先权日:2021-09-03
标题:Synthesis of bicycle toxin conjugates, and intermediates thereof
发明人：WITTY DAVID; LIMB DARREN; MIN BYOUNG JOON; HE LIWEN; SANDERS WILLIAM J; NNANABU ERNEST OBINNA
权利人:BRICYCLETX LTD
摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.

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.

专利号:US-2022135614-A1
优先权日:2019-03-04
标题:Synthesis of bicycle toxin conjugates, and intermediates thereof
发明人：TEUFEL DANIEL
权利人:BICYCLERD LTD
摘要:The present invention relates to Bicycle toxin conjugates, methods for preparation, and methods of use for treating cancer.