CAS: 64987-85-5; 2,5-Dioxopyrrolidin-1-Yl 4-((2,5-Dioxo-2,5-Dihydro-1H-Pyrrol-1-yl)Methyl)Cyclohexanecarboxylate

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CAS号6066-82-6 N-羟基琥珀酰亚胺

凝血酸置于2,4,6-三甲基吡啶,三氟乙酸酐体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 4-(N-马来酰亚胺基甲基)环己烷-1-羧酸琥珀酰亚胺酯
参考文献:Sct200-接头-单甲基澳瑞他汀e偶联物的合成,表征和靶向化疗
标题:Sct200-接头-单甲基澳瑞他汀e偶联物的合成,表征和靶向化疗
摘要:抗体-药物偶联物(adc)目前是治疗实体瘤患者最成功,最重要的策略之一.adc由单克隆抗体和战斗部组成,它们通过连接子偶联.当前,单甲基耳他汀e(mmae)是adc开发中应用最广泛的战斗部.但是,基于mmae的adc通常使用mc-Vc-Pabc链接器构建,并且该设计具有有限的结构多样性和一些缺点.因此,在这项研究中,我们在adc中反应生成了三种类型的新型接头-Mmae(与mc-Vc-Pabc-Mmae相比,间隔区,分解代谢区域和自消灭性改变),称为sct200-接头-Mmae共轭物,然后评估连接蛋白的血浆稳定性和组织蛋白酶b的药物释放速率.结合能力,内在化速率,系统地研究了所有sct200-Linker-Mmae Adc的合成和功效,并评估了凋亡相关蛋白的表达以及sct200-M-2,-C-2和-C-4的治疗效果.结果表明,对于表皮生长因子受体阳性的肿瘤,其中一些adc的活性增加.此外,本研究
DOI:10.1016/j.Ejmech.2021.113297

专利信息

专利号:US-2024287520-A1
优先权日:2021-06-30
标题:Method for synthesis of linkage modified oligomeric compounds
发明人：RODRIGUEZ ANDREW A
权利人:IONIS PHARMACEUTICALS INC
摘要:The present disclosure provides methods of synthesizing modified oligonucletodies and oligomeric compounds (including oligomeric compounds that are antisense agents or portions thereof) comprising a modified oligonucleotide having at least one modified internucleoside linking group. In certain embodiments, the present disclosure provides stabilized formulations of certain sulfonyl azides for use in the synthesis of olignonucleotides comprising one or more sulfonyl phosphoramidate linkages. Some embodiments provide stabilized compositions of high energy reagents that may be used in the synthesis of modified oligonucleotides, allowing for safe process scale preparation thereof.

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-2004038331-A1
优先权日:2002-08-23
标题:Solid phase synthesis of biomolecule conjugates
发明人：REDDY M PARAMESWARA; FAROOQUI FIRDOUS; BRILLHART KURT L
摘要:Processes for the solid state phase formation synthesis of biomolecule conjugates, particularly protein-oligonucleotide conjugates are shown. One of the protein or oligonucleotide is reversibly bound to a solid substrate phase. At least one portion of each of the protein and the oligonucleotide molecules is activated with complementary activation groups. The activated protein and the activated oligonucleotide are then reacted, in a buffered solution resulting in the formation of the desired conjugate which remains reversibly bound to the substrate. The nature of the buffered solution is then modified causing the conjugate to be released from the substrate solid phase.

专利号:WO-2024119509-A1
优先权日:2022-12-09
标 题 :Synthesis method for second strand in dnb paired-end sequencing, sequencing method, and related products
发明人：XU CHONGJUN; JIANG LAN; YANG JIN; GONG MEIHUA
权利人:MGI TECH CO LTD
摘要:Provided are a synthesis method for a second strand in DNB paired-end sequencing, a sequencing method, and related products. The synthesis method for the second strand comprises: after DNB is subjected to first-strand sequencing, using a second-strand synthesis primer to synthesize the second strand, wherein the second-strand synthesis primer is a primer capable of being anchored on the surface of a sequencing chip. Using the second-strand synthesis primer that is anchored on the surface of a sequencing vector for the synthesis of the second strand makes the process of synthesizing the second strand relatively more stable. Moreover, the synthesized second-strand template is anchored on the sequencing vector, and subsequent sequencing of the second-strand template strand that is anchored on the sequencing vector can achieve a relatively higher quality of the second-strand sequencing.

专利号:WO-2017100796-A1
优先权日:2015-12-11
标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI
权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING
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 disgnostic and therapeutic uses.

专利号:US-2008145899-A1
优先权日:2004-09-17
标题 :Production of Oligosaccharides By Microorganisms
发明人：JOHNSON KARL; BYRNE NOEL J; DEFREES SHAWN
权利人:NEOSE TECHNOLOGIES INC
摘要:The present invention relates to the enzymatic synthesis of oligosaccharides, including sialylated product saccharides. In particular, it relates to the use of recombinant cells to take up low cost precursors such as glucose, pyruvate and N-actyl-glucosamine, and to synthesize activated sugar moieties that are used in oligosaccharide synthesis. The methods make possible the synthesis of many oligosaccharides using microorganisms and readily available, relatively inexpensive starting materials.