CAS: 147149-76-6; 2-Amino-6-Methyl-5-(Pyridin-4-Ylthio)Quinazolin-4(3H)-One

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2-氨基-5-溴-6-甲基-4(1H)-喹唑啉酮 2-Amino-5-Bromo-6-Methyl-3-H-Quinazolin-4-One 147149-89-1

📜5-Bromo-6-Methyl-1H-Benzo<1,3>Oxazine-2,4-Dione置于copper(I) Oxide,Sodium Hydride,Copper(I) Bromide体系中,用 二乙二醇二甲醚 用作溶剂,化学反应 6.0H,反应生成诺拉曲特
参考文献:使用蛋白质晶体结构设计胸苷酸合酶抑制剂:一类新的5-取代的喹唑啉酮的合成和生物学评价.
标题:使用蛋白质晶体结构设计胸苷酸合酶抑制剂:一类新的5-取代的喹唑啉酮的合成和生物学评价.
摘要:描述了新型胸苷酸合酶(ts)抑制剂的设计,合成和生物学评估.通过对蛋白质-配体结构的重复晶体学分析来进行分子设计.在该项目开始时,我们专注于大肠杆菌ts,5'-氟脱氧尿酸(5-Fdump)和经典的含谷氨酸叶酸类似物的高分辨率三元晶体复合物的叶酸辅因子结合位点.一种新型化合物的初步三元晶体结构已成功解决.通过分析该初始复合物,进行了进一步的结构修饰,并开发了一系列活性5-(芳硫基)喹唑啉酮.合成策略基于各种芳基硫代阴离子置换喹唑啉酮5位上的卤素.测试化合物对纯化的大肠杆菌和/或人ts的抑制作用,并在体外测定针对三种肿瘤细胞系的细胞毒性.用几种抑制剂观测到了重要的胸腺嘧啶核苷保护作用,表明ts是细胞内活性位点.
Doi:10.1021/jm00058A010

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-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-2012149888-A1
优先权日:2009-02-22
标 题:Synthesis of ara-2'-o-methyl-nucleosides, corresponding phosphoramidites and oligonucleotides incorporating novel modifications for biological application in therapeuctics, diagnostics, g- tetrad forming oligonucleotides and aptamers
发明人：SRIVASTAVA SURESH C; PANDEY DIVYA; SRIVASTAVA NAVEEN P; SRIVASTAVA ALOK
权利人:SRIVASTAVA SURESH C; PANDEY DIVYA; SRIVASTAVA NAVEEN P; SRIVASTAVA ALOK
摘要:The present invention relates to synthesis, purification and methods to obtain high purity novel 2′-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2′-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents. It is further anticipated that the nucleosides, phosphates and triphosphates of this invention could develop as therapeutic agents.