CAS: 54-62-6; (S)-2-(4-(((2,4-Diaminopteridin-6-yl)Methyl)Amino)Benzamido)Pentanedioic Acid

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CAS号59368-16-0 6-(溴甲基)-2,4-蝶啶二胺 | CAS号4271-30-1 N-(4-氨基甲酰)-L-谷氨酸 | CAS号59-30-3 叶酸 | CAS号7732-18-5 水 | CAS号52853-40-4 6-溴乙基-喋啶-2,4-二胺氢溴酸盐 | CAS号5221-17-0 2,3-二溴丙醛 | CAS号36093-85-3 4-(N-[2,4-二氨基-6... | CAS号945-24-4 2,4-二氨基-6-羟甲基蝶啶 | CAS号89043-75-4 4-[[2-(2,4-diam... | CAS号948-60-7 2-氨基-4-氧代-3,4-二... | CAS号432545-60-3 甲氨蝶呤-d3二甲酯 | CAS号36093-85-3 4-(N-[2,4-二氨基-6... | CAS号89043-75-4 4-[[2-(2,4-diam... | CAS号432545-63-6 甲氨蝶呤-D3

(S)-(4-(((4-((1,5-Dimethoxy-1,5-Dioxopentan-2-yl)Carbamoyl)Phenyl)Amino)Methyl)Phenyl)Boronic Acid置于双氧水,三乙胺,Sodium Hydroxide体系中,用 Aq. Phosphate Buffer,N,N-二甲基乙酰胺,水,二甲基亚砜 作为反应溶剂,化学反应 74.08H,反应生成 氨基蝶呤
参考文献:甲氨蝶呤和氨基蝶呤对过氧化氢敏感的前药的合成与评价
标题:甲氨蝶呤和氨基蝶呤对过氧化氢敏感的前药的合成与评价
摘要:合成了一系列新的甲氨蝶呤(mtx)和氨蝶呤(amt)对过氧化氢敏感的前药,并评估了胶原诱导的关节炎(cia)作为慢性类风湿关节炎(ra)的模型对小鼠的治疗效果.选择的前药策略是基于不稳定的ros,通过氨基甲酸酯键或直接的c-n键与药物相连的4-甲基苯基硼酸.在病理生理浓度的H2O 2下激活被证明是有效的,并且与相关体外实验一致地选择了前药候选物物理化学和药代动力学分析.与cia模型中的母体药物相比,选定的候选药物显示出中等至非常好的溶解度,较高的化学和酶稳定性以及治疗功效.重要的是,与mtx和amt相比,前药显示出预期的更安全的毒性特征并增加了治疗范围,同时保持了可比的治疗功效,这极大地鼓舞了ra患者的未来使用.
DOI:10.1021/acs.Jmedchem.7B01775

专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2003159164-A1
优先权日:1998-05-29
标 题:Compositions and methods for the synthesis of fatty acids, their derivatives and downstream products
发明人：KOPCHICK JOHN JOSEPH; KELDER BRUCE; HUANG YUNG-SHENG; KIRCHNER STEPHEN J; MUKERJI PRADIP
摘要:The invention generally relates to synthesis of essential fatty acids and their derivatives, long-chain polyunsaturated fatty acids (LC-PUFAs) and eicosanoids in transfected cells and in transgenic animals.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:WO-2004113530-A1
优先权日:2003-06-18
标题:Polynucleotide for synthesis of labeled protein
发明人：NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU
权利人:MITSUBISHI CHEM CORP; NAKA DAIJI; NAKANO HIROSHI; SHIRATORI MIWA; KOBAYASHI TERUAKI; SUZUKI KATSUHIKO; HASHIMOTO HIDEMI; SASAKI TOORU
摘要:A process for producing a labeled protein, comprising translating a gene template in the presence of a labeled compound having a label portion consisting of a labeled substance and an acceptor portion consisting of a compound capable of binding to the C-terminus of protein synthesized by a translation system. In particular, there are provided a polynucleotide for use in synthesis of labeled protein characterized by having the capability of enhancing labeling efficiency through addition to the 3’ end of a base sequence coding for target protein within the gene template and provided a process for producing a labeled protein that is carried out with the use of the polynucleotide.

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-2014234364-A1
优先权日:2011-09-23
标 题:Total synthesis and immunological evaluation of saccharide moieties of the lipopolysaccharide from neisseria meningitidis
发明人：SEEBERGER PETER H; YANG YOU; ANISH CHAKKUMKAL; REINHARDT ANIKA
权利人:MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V
摘要:The present invention relates to the total chemical synthesis of the monosaccharide 35 # (R′â•?H), the disaccharide 36 # (R′≠H; R″â•?H), the trisaccharide 37 # (R′≠H; R″≠H; R′″≠H) and the tetrasaccharide 1 # (R′≠H; R″≠H; R′″≠H) of the following general formula wherein R represents —Y—NH 2 Y represents a linker R′ is H or R″ is H or R′″ is H or of the lipopolysaccharide from Neisseria meningitidis , as well as to the trisaccharide 37 # and the tetrasaccharide 1 # , to vaccines containing at least one of the saccharides 1 # , 35 # , 36 # , and 37 # and to the use of such vaccine for immunization against diseases caused by infection with bacteria containing the tetrasaccharide α-GlcNAc-(1→2)-α-Hep-( 1→3 )-α-Hep-(1→5)-α-Kdo or the trisaccharide α-Hep-(1→3)-α-Hep-(1→5)-α-Kdo or α-GlcNAc-(1→2)-±-Hep-(1→3)-α-Hep, especially for immunization against meningitis, septicaemia, pneumonia and nasopharyngitis caused by Neisseria meningitidis.