专利号:US-8697862-B2 优先权日:2008-05-16 标题 :Synthesis of galactoside inhibitors 发明人:NILSSON ULF 权利人:NILSSON ULF; GALECTO BIOTECH AB 摘要:Novel synthesis routes for preparation of thiodigalactosides and intermediates are presented. The method includes the use of a 3-azido-galactosyl thiouronium salt derivative, which is activated to the corresponding thiol in situ, which in turn is directly reacted with a 3-azido-galactosyl bromide resulting in the 3,3′-di-azido-thio-di-galactoside before the thiol has a chance to reduce the azido 10 group. Hence, in situ formation of the 3-azido-galactosyl thiol from the thiouronium salt is essential in the synthesis procedure, because any other method that generate the thiol separately results in extensive unwanted azide reduction.
专利号:US-2022265691-A1 优先权日:2019-07-12 标 题 :Methods for use of gene expression as an indicator of e-selectin inhibitor efficacy and clinical outcome for multiple tumor types 发明人:MAGNANI JOHN L; FOGLER WILLIAM E; THACKRAY HELEN M; FELDMAN ERIC J; STEWART DAVID 权利人:GLYCOMIMETICS INC 摘要:Cancer patients that express high levels of the E-selectin ligand (sialyl Lea/x) on their tumors have a poorer outcome. Interestingly, relapsed/refractory acute myeloid leukemia (AML) patients expressing high levels of sialyl Lex on their blasts show the greatest therapeutic response when treated with the E-selection inhibitor compound of Formula I. Transcriptome profiling of E-selectin ligand-forming glycosylation genes showed that ST3GAL4 and FUT7 were consistently expressed in the majority of cancers evaluated. Poor survival outcomes of FLT3-mutated AML patients that express high levels of ST3GAL4 and FUT7 implicated E-selectin in this disease state. These genes may be predictive biomarkers in AML patients. Methods of treatment of cancer comprising screening AML patients for expression of genes that contribute to the synthesis of the E-selectin ligand sialyl Lex, then treating those patients with an E-selection inhibitor, are disclosed.
专利号:WO-2013131872-A1 优先权日:2012-03-05 标 题 :Imaging neural activity 发明人:BETTS HELEN MAY; DESMOND ANTONIA; ROBINS EDWARD GEORGE 权利人:GE HEALTHCARE LTD; UCL SCHOOL OF PHARMACY 摘要:The present invention provides a novel radiofluorinated compound for imaging voltage-gated sodium channels (VGSCs) that is more straightforward to synthesise than the known radiofluorinated phenoxyphenyl pyrazole carboxylic acid compounds. The compound of the present invention demonstrates specific uptake and retention in key tissues as well as good in vivo stability. Also provided by the present invention is a radiopharmaceutical composition comprising the radiofluorinated compound of the invention, precursor compounds and methods for the synthesis of said radiofluorinated compound, and methods for using said radiofluorinated compound.
专利号:US-10799522-B2 优先权日:2015-07-27 标 题 :Compositions and methods relating to galectin detection 发明人:GELOVANI JURI G; TURKMAN NASHAAT; POPOV VADIM; BONOMI ROBIN; SHAVRIN ALEKSANDR; ALTHER PHILIP; BORISOV ANDREI 权利人:UNIV WAYNE STATE 摘要:Compositions and methods for detection and assessment of galectins are provided by the present invention, including labeled compositions, pharmaceutical composition including a labeled composition for galectin detection and a pharmaceutically acceptable carrier, method of aiding in diagnosis and/or treatment of a condition characterized by upregulation of one or more galectins in a subject in need thereof and precursor compositions for synthesis of chemical compositions, including but not limited to labeled compositions for detection and assessment of galectins.
专利号:WO-2009139719-A9 优先权日:2008-05-16 标 题 :Novel synthesis of galactoside inhibitors
专利号:CN-104860864-A 优先权日:2015-06-04 标 题 :A new method for the synthesis of 2-carbonyl-5-alkynylpyrrole compounds
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