顺式-5-氮杂-4-氧代-辛-2-烯-二酸置于三乙胺,N,N'-二环己基碳二亚胺体系中,用 二氯甲烷,甲苯 作为反应溶剂,化学反应 4.33H,反应生成 3-马来酰亚胺基丙酸羟基琥珀酰亚胺酯 参考文献:Comblike Dendrimers Containing Tn Antigen Modulate Natural Killing And Induce The Production Of Tn Specific Antibodies 标题:Comblike Dendrimers Containing Tn Antigen Modulate Natural Killing And Induce The Production Of Tn Specific Antibodies 摘要:Comblike Glycodendrimers Were Prepared By The Chemoselective Ligation Of Cysteine-Modified Glycopeptides (1-7) With A 3-Maleimidopropionate-Modified Linear Synthetic Carrier (8). Glycodendrimers Bearing Mono-,Di-,Or Tri-Tn Clusters (9-11) Were Tested As Inhibitors Using Plant And Mammalian Lectins. In The Former Group,The Codium Fragile Lectin Showed Moderate Discrimination Among 9,10,And 11. In The Latter Group,A And B Isoforms Of Rat Nkr-P1 Lectin Strongly Discriminated Between 9 And 10. 10 Caused A 4-Fold Increase In Killing Of The Nk Resistant Tumor Cell Lines At Concentrations As Low As 10(-8) M. Surprisingly,11 Interacted Exclusively With The Rat Nkr-P1B Isoform And Inhibited Efficiently Natural Killing In Both Rats And Humans,Even In The Presence Of The Activating Compounds 9 And 10. Dinitrophenol Haptenization Or Influenza Virus Hemagglutinin T-Cell Epitope Conjugation Increased The Immunogenicity Of The Parent Compounds And Resulted In The Production Of Tn Specific Antibodies. DOI:10.1021/jm050741G
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:WO-03064360-A1 优先权日:2002-02-01 标 题:Synthetic tetraethers and synthesis strategies therefor 发明人:KUEHL CHRISTINE; LITTGER RALF 权利人:BERNINA BIOSYSTEMS GMBH; KUEHL CHRISTINE; LITTGER RALF 摘要:The invention relates to novel synthetic tetraethers and a novel method for producing said substances. The inventive tetraethers are characterised in that they can be modified in a simple and targeted manner according to said synthesis method, which enabling the synthesis of the desired model substances. The synthesis concept guarantees high variability with simple individual production.
专利号:US-10254287-B2 优先权日:2015-07-21 标题 :Protein fluorescent nanoparticles and methods of synthesis thereof 发明人:KUMAR CHALLA VIJAYA; STROMER BOBBI SHANYELLE 权利人:UNIV CONNECTICUT 摘要:Disclosed herein are stable and versatile protein nanoparticles having a range of tunable fluorescent properties. Such nanoparticles may find utility in biological imaging. Methods of synthesis of such nanoparticles are also disclosed.
专利号:WO-0136626-A9 优先权日:1999-11-15 标 题 :Pentraxin i and pentraxin receptor, inhibitors of said proteins and pharmaceutical compositions containing said compounds 发明人:MESSEGUER PEYPOCH RAMON; ROSELL VIVES ELISABET; MARTINEZ ESCOLA JOSEP MA; RODES GUBERN BLANCA; ADAN PLANA JAUME; PUIG CALVO NURIA; CARCELLER ROSA ANA; MASA ALVAREZ MARC; PIULATS XANCO JAUME; DEN DAAS IZAAK; TRULLAS OLIVA RAMON; DE GREGORIO-ROCASOLANO BARBANY 权利人:MERCK PATENT GMBH; MESSEGUER PEYPOCH RAMON; ROSELL VIVES ELISABET; MARTINEZ ESCOLA JOSEP MA; RODES GUBERN BLANCA; ADAN PLANA JAUME; PUIG CALVO NURIA; CARCELLER ROSA ANA; MASA ALVAREZ MARC; PIULATS XANCO JAUME; DEN DAAS IZAAK; TRULLAS OLIVA RAMON; DE GREGORIO-ROCASOLANO BARBANY 摘要:Described are nucleic acid sequences encoding the human Pentraxin receptor and related proteins and pharmaceutical composition comprising a therapeutically effective amount of (a) Pentraxin I or the human Pentraxin receptor, (b) a nonfunctional variant of the protein of (a), (c) an antibody to the protein of (a) or (b), (d) a nucleic acid sequence encoding the protein of (a) or (b), (e) an antisense RNA sequence, said sequence being capable of inhibiting the synthesis of Pentraxin 1 or the human Pentraxin receptor, or (f) a ribozyme characterized in that it is complementary to a Pentraxin I or human Pentraxin receptor mRNA and can selectively bind to and cleave said mRNA, thus inhibiting the synthesis of Pentraxin I or the human Pentraxin receptor.
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.
专利号:US-5439798-A 优先权日:1993-12-17 标 题:Maleimide adduct conjugates of procainamide and NAPA 发明人:SIGLER GERALD F; WALTER CHARLES F; DURANT CHARLES E; GLANCY TODD; KLEIN FRANK E; DORN ALLAN R 权利人:BOEHRINGER MANNHEIM CORP 摘要:Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having the following formula: +TR wherein: X=hydrogen or acetyl; R1=an alkyl group having 1 to 3 carbon atoms; m=an integer from 2 to 10; R2=an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms; Z=a poly(amino acid); and n=1 to p where p=MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.
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合成参考文献
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