脑膜炎奈瑟菌 (Men X) 的血清型 X 最近成为对公共健康的重大威胁。由于目前可用或正在研究的抗脑膜炎球菌疫苗不包含 Men X 荚膜多糖的抗原成分,因此需要开发能够提供更高保护的更全面的结合疫苗。作为实现这一目标的初步步骤,描述了三个可结合的 Men X 荚膜多糖片段的合成。关键的 α-糖基磷酸二酯键的安装基于磷酸氢盐方法,使用分别从半缩醛 9 和 11 获得的纯 α-糖基磷酸氢盐 10 和 12。
[EN] CYCLIC DINUCLEOTIDES AS AGONISTS OF STIMULATOR OF INTERFERON GENE DEPENDENT SIGNALLING<br/>[FR] DINUCLÉOTIDES CYCLIQUES UTILISÉS EN TANT QU'AGONISTES DU STIMULATEUR DE LA SIGNALISATION DÉPENDANTE DU GÈNE DE L'INTERFÉRON
申请人:UNIV TEXAS
公开号:WO2018156625A1
公开(公告)日:2018-08-30
Disclosed herein are new cyclic dinucleotide compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulation of immune response to disease, and induce Stimulator of Interferon Genes (STING) dependent type I interferon production and co-regulated genes in a human or animal subject are also provided for the treatment diseases such as cancer, particularly metastatic solid tumors and lymphomas, inflammation, allergic and autoimmune disease, infectious disease, and for use as anti-viral agents and vaccine adjuvants.
[EN] A NEW METHOD OF 18F LABELLING AND INTERMEDIATE SALTS<br/>[FR] NOUVEAU PROCÉDÉ D'ÉTIQUETAGE DE 18F ET DE SELS INTERMÉDIAIRES
申请人:NAT UNIV SINGAPORE
公开号:WO2021126080A1
公开(公告)日:2021-06-24
Disclosed herein is a salt of formula I: where R1, X, n, R, R1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET imaging, as well as methods to make the compounds of formula I.
Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
申请人:——
公开号:US20020147160A1
公开(公告)日:2002-10-10
The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
[EN] MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2<br/>[FR] MODULATEURS DU RÉCEPTEUR MÉTABOTROPIQUE DU GLUTAMATE 2
申请人:MASSACHUSETTS GEN HOSPITAL
公开号:WO2021155196A1
公开(公告)日:2021-08-05
The present application provides a compound of Formula: or a pharmaceutically acceptable salt thereof, wherein ring B, L1, ring A, L2, n, R1, R2, R3, R4, and X1 are as described herein. Pharmaceutical compositions comprising the compound, as well as the methods of making and using the compound, are also provided.
[EN] METHODS AND COMPOUNDS USING IN-LOOP FLUORINATION<br/>[FR] PROCÉDÉS ET COMPOSÉS FAISANT APPEL À UNE FLUORATION EN BOUCLE
申请人:CAMH
公开号:WO2020222041A1
公开(公告)日:2020-11-05
This invention provides a novel method that is simple, efficient, and allows for a reliable production of fluorine- 18 (18F) radiofluorinated compounds and radiopharmaceuticals. The method comprises an "in-loop" process, where an 18F source is reacted with a precursor compound in an injection loop of a high-performance liquid chromatography (HPLC) system to form a radiolabeling reagent. The [18F]triflyl fluoride, the radiolabeling agent, is reacted with 1,4-dinitrobenzene to form [18F] l-fluoro-4-nitrobenzene, which was then reacted with compounds of interest. The invention provides 18F radiolabeled compounds in high radiochemical yield. The resulting compounds have use as radiotracers and PET imaging agents. The method can also be used to produce 19F compounds.