[EN] BIS(2-HALOACETAMIDO)-COMPOUNDS FOR USE AS LINKING AGENTS AND RESULTANT PRODUCTS WHICH COMPRISE ANTIBODIES, HALF-ANTIBODIES AND ANTIBODY FRAGMENTS<br/>[FR] COMPOSÉS BIS(2-HALOACÉTAMIDO) DESTINÉS À ÊTRE UTILISÉS EN TANT QU'AGENTS DE LIAISON ET PRODUITS RÉSULTANTS QUI COMPRENNENT DES ANTICORPS, DES DEMI-ANTICORPS ET DES FRAGMENTS D'ANTICORPS
申请人:UNIV BATH
公开号:WO2020260514A1
公开(公告)日:2020-12-30
Bis(2-haloacetamido)- compounds for use as linkers to chemically cross-linking multiple thiol groups, and particularly, although not exclusively, the thiol groups of cysteine amino acids in peptide chains are described, along with their use as linking agents and resultant products which comprise antibodies, half-antibodies and antibody fragments having thiol groups bonded to said linkers (e.g. antibody- protein conjugates and antibody-drug conjugates), and methods of making said conjugates and products. (Formula I)
[EN] ORGANONITRO THIOETHER COMPOUNDS AND MEDICAL USES THEREOF<br/>[FR] COMPOSÉS D'ORGANONITRO THIOÉTHER ET UTILISATIONS MÉDICALES DE CEUX-CI
申请人:RADIORX INC
公开号:WO2013052164A1
公开(公告)日:2013-04-11
The invention provides organonitro thioether compounds, compositions containing such compounds, isolated organonitro thioether compounds and methods for using such compounds and compositions to treat cancer in a patient. Exemplary organonitro thioether compounds described herein include 2-(3,3-dinitroazetidin-l-yl)-2-oxoethyl thioethers and variants thereof. Another aspect of the invention provides a pharmaceutical composition, comprising a pharmaceutically acceptable carrier and an organonitro thioether compound described herein, such as a compound of Formula I or II. Another aspect of the invention provides a method of treating cancer in a patient. The method comprises administering to a patient in need thereof a therapeutically effective amount of an organonitro thioether compound described herein, such as a compound of Formula I or II, to treat the cancer.
Pharmaceutical compositions and therapeutic applications for the use of a novel vitamin B12 derivative, N-acetyl-L-cysteinylcobalamin
申请人:Brasch E. Nicola
公开号:US20080076733A1
公开(公告)日:2008-03-27
Therapeutic applications, such as prevention, treatment and supplementation, for the use of novel and other thiolatocobalamins to protect human cells against the effects of oxidative stress. In particular, this invention relates to the use of a novel synthetic thiolatocobalamin, N-acetyl-L-cysteinylcobalamin (NACCbl) to protect animal cells against oxidative stress damage. This invention also relates to the use of thiolatocobalamins, such as NACCbl, in lieu of current, commercially available forms of vitamin B
12
for the treatment and prevention of conditions associated with oxidative stress damage and for dietary supplementation.
Rapid <sup>18</sup>F-labeling <i>via</i> Pd-catalyzed <i>S</i>-arylation in aqueous medium
作者:Swen Humpert、Mohamed A. Omrane、Elizaveta A. Urusova、Lothar Gremer、Dieter Willbold、Heike Endepols、Raisa N. Krasikova、Bernd Neumaier、Boris D. Zlatopolskiy
DOI:10.1039/d1cc00745a
日期:——
Rapid Pd-catalyzed S-arylation with easily accessible 2-[18F]fluoro-5-iodopyridine enables facile preparation of radiolabeled peptides and proteins.
Synthesis, Characterization, and Glutathionylation of Cobalamin Model Complexes [Co(N4PyCO<sub>2</sub>Me)Cl]Cl<sub>2</sub> and [Co(Bn-CDPy3)Cl]Cl<sub>2</sub>
作者:Jai Prakash、Jeremy J. Kodanko
DOI:10.1021/ic2026736
日期:2012.2.20
Synthetic Co(III) complexescontaining N5 donor sets undergo glutathionylation to generate biomimetic species of glutathionylcobalamin (GSCbl), an important form of cobalamin (Cbl) found in nature. For this study, a new Co(III) complex was synthesized derived from the polypyridyl pentadentate N5 ligand N4PyCO2Me (1). The compound [Co(N4PyCO2Me)Cl]Cl2 (3) was characterized by X-ray crystallography,
含有N5个供体的合成Co(III)配合物经过谷胱甘肽酰化反应生成仿生物种谷胱甘肽钴胺素(GSCbl),这是自然界中重要的钴胺素(Cbl)形式。对于本研究,合成了一种新的Co(III)配合物,该配合物是由五齿的聚吡啶基N5配体N4PyCO 2 Me(1)衍生而来的。化合物[Co(N4PyCO 2 Me)Cl] Cl 2(3)的特征在于X射线晶体学,紫外可见,IR,1 H NMR和13 C NMR光谱法和质谱(HRMS)。3与H 2 O中的谷胱甘肽(GSH)反应生成仿生菌种[Co(N4PyCO 2 Me)(SG)]2+(5),它是原位生成的,并通过UV-vis和1 H NMR光谱学和HRMS进行了表征。1 H NMR和UV-vis光谱数据与GSH的半胱氨酸硫醇盐与5的Co(III)中心的连接相一致,就像在GSCbl中那样。动力学分析表明,氯化物被GS –取代是通过二次过程[ k 1 =(10.1±0