专利号:US-11753440-B2 优先权日:2018-06-05 标题 :Methods for the synthesis of arginine-containing peptides 发明人:HEIDL MARC; GEOTTI-BIANCHINI PIERO 权利人:DSM IP ASSETS BV 摘要:Methods for the synthesis of arginine-containing peptides are provided. The methods include a deprotection step that minimizes the transfer of by-products deriving from cleaved sulfonyl-5 based side chain protecting groups from arginine to amino acids carrying electron rich side chains.
专利号:US-9447149-B2 优先权日:2012-03-06 标 题 :Methods and compositions for the rapid synthesis of radiometal-labeled probes 发明人:CHEN KAI; CONTI PETER STEPHEN 权利人:UNIV SOUTHERN CALIFORNIA 摘要:The present application is directed to rapid and efficient synthesis of radiometal-labeled probes, pharmaceutical compositions comprising radiometal-labeled probes, and methods of using the radiometal-labeled probes. Such radiometal-labeled probes can be used in imaging studies, such as Positron Emitting Tomography (PET) or Single Photon Emission Computed Tomography (SPECT), and therapy studies.
专利号:US-9315483-B2 优先权日:2007-09-13 标题 :Synthesis of deuterated catechols and benzo[D][1,3]dioxoles and derivatives thereof 发明人:JONES ANDREW D; ZELLE ROBERT E; SILVERMAN I ROBERT 权利人:CONCERT PHARMACEUTICALS INC 摘要:The present invention provides a convenient and efficient process for the synthesis of d 2 -benzo[d][1,3]dioxoles.
专利号:US-2022098155-A1 优先权日:2018-11-14 标 题 :Novel pathway for the synthesis of diazirines, that may or may not be enriched in nitrogen-15 发明人:REBOUL VINCENT; FRANCK XAVIER; GLACHET THOMAS; MARZAG HAMID 权利人:UNIV ROUEN NORMANDIE; UNIV CAEN; INSTITUT NAT DES SCIENCES APPLIQUEES DE ROUEN INSA; CENTRE NAT RECH SCIENT; ECOLE NAT SUPERIEURE DINGENIEURS DE CAEN 摘要:The present invention concerns a novel method for synthesising diazirines, that may or may not be enriched in nitro-gen-15, from amino acids or imines, via a one-pot synthesis method, comprising the reaction of the starting amino acid or imine with ammonia, which may or may not be enriched in nitrogen-15, and a hypervalent iodine oxidant. The present invention also relates to a method for synthesising ammonia enriched in nitrogen-15. The invention also concerns certain diazirines of formula (I) likely to be obtained by the claimed synthesis method, and also refers to the 15 N 2 -diazirines of formula (I′). The claimed diazirines can be used in photoaffinity labelling. The 15 N 2 -diazirines can also be used in hyperpolarisation, in particular in the medical imaging field.
专利号:WO-2008150031-A1 优先权日:2007-06-08 标题:Inhibitor of biosynthesis of plant hormone auxin, chemical plant regulator comprising the inhibitor as active ingredient, herbicidal agent, and use thereof 发明人:SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO 权利人:RIKEN; SHIMADA YUKIHISA; GODA HIDEKI; TACHIKAWA TOMOE; ISHII TAKAHIRO; SOENO KAZUO; FUJIOKA SHOZO; ASAMI TADAO 摘要:The first object is to provide an inhibitor of the synthesis of endogenous auxin. The second object is to provide a plant growth inhibitor or a herbicidal agent utilizing the auxin biosynthesis inhibitor. Thus, disclosed are: a method for screening a candidate for an auxin biosynthesis inhibitor capable of inhibiting the expression of an auxin-inducible gene, by adding each of candidate compounds for the auxin inhibitor to a plant; a method for selecting a compound capable of actually inhibiting the auxin synthesis in a plant, by adding each of candidate compounds to the plant, disrupting the plant and then measuring the amount of endogenous auxin; and a method for selecting a compound capable of inhibiting the production of indolpyruvic acid in the presence of a tryptophan deaminase and tryptophan which are prepared in advance. More specifically disclosed are: an auxin biosynthesis inhibitor comprising AVG, AOA, AOIBA, L-AOPP or an analogue thereof; and a plant growth regulator or a herbicidal agent comprising the compound as an active ingredient.
专利号:US-2009124012-A1 优先权日:2007-08-08 标题:Toxin/antitoxin systems and methods for regulating cellular growth, metabolic engineering and production of recombinant proteins 发明人:NIKOLSKY YURI; BAEV MARK 权利人:MAZEF BIOSCIENCES LLC 摘要:The present invention provides compositions and method for regulating cellular growth and metabolism, intra- and extracellular enzymatic activities, and synthesis of endogenous and/or heterologous proteins, comprising the steps of cloning genes encoding an mRNA interferase (toxin) and its cognate antitoxin; expressing these proteins in a host cell from two separate constitutive or inducible promoters on one or more plasmid vectors or on a chromosome; and regulating the cellular growth and metabolism by controlling the ratio of toxin and antitoxin present in the host cell. Optionally, the method provides further steps of modifying an endogenous or heterologous gene of interest to substitute all mRNA recognition sequences with sequences that are not cleavable by the mRNA interferase being expressed without any change in the amino acid sequence of the protein encoded by the gene; and co-expressing the gene of interest in the same host cell.
参考文献:10.1016/j.bmc.2013.07.052 摘要:Sun Q, Yang Q, Gong S, Fu Q, Xiao Q. Synthesis and enzymatic evaluation of phosphoramidon and its β anomer: Anomerization of α-l-rhamnose triacetate upon phosphitylation. Bioorg Med Chem. 2013 Nov 01;21(21):6778–87. doi: 10.1016/j.bmc.2013.07.052.