专利号:WO-9403593-A1 优先权日:1992-08-04 标题 :Amplifier molecules for enhancement of diagnosis and therapy 发明人:KEANA JOHN F W 权利人:OREGON STATE 摘要:Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
专利号:US-8461298-B2 优先权日:2004-11-01 标 题:Compositions and methods for modification of biomolecules 发明人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL 权利人:BERTOZZI CAROLYN R; AGARD NICHOLAS J; PRESCHER JENNIFER A; BASKIN JEREMY MICHAEL; UNIV CALIFORNIA 摘要:The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
专利号:US-2004022857-A1 优先权日:2002-07-31 标 题 :Synthesis of highly conjugated polymers 发明人:UZGIRIS EGIDIJUS E; MOASSER BAHRAM; FISH KENNETH M; SMITH JOANNE F 摘要:Improved methods for forming substituted polymers having a high degree of conjugation include the steps of activating a steric hindrance molecule under conditions that ensure substantially all the steric hindrance molecules are mono-activated and then reacting with a polymer. An improved method for recovering polypeptides substituted with steric hindrance molecules and having an elongate configuration removes impurities and volatiles without achieving complete dryness of the copolymer.
专利号:WO-2010034314-A1 优先权日:2008-09-24 标题:Retroviral delivery of synthectic gene cassettes 发明人:PEDERSEN FINN SKOU; BAHRAMI SHERWIN 权利人:UNIV AARHUS; PEDERSEN FINN SKOU; BAHRAMI SHERWIN 摘要:The present invention relates to a multifunctional molecule which is capable of initiating first and/or second strand DNA synthesis of a retroviral RNA genome or derivatives thereof. The multifunctional molecule comprises a first part complementary to a part of the retroviral RNA genome or derivatives thereof. A second part of the multifunctional molecule comprises genetic elements and/or labels. The genetic elements may be gene cassettes for the expression of proteins, peptides or polypeptides or for example functional RNA elements such as shRNA, siRNA, miRNA and the like. The multifunctional molecule represents a novel tool for insertion of genes into host cell genomes. The present invention therefore relates to the field of gene delivery and methods employed therefore.
专利号:US-2007196275-A1 优先权日:2001-04-26 标题 :Diagnostic Imaging Compositions, Their Methods Of Synthesis And Use 发明人:LI CHUN; WEN XIAOXIA; WU QING-PING; WALLACE SIDNEY; ELLIS LEE M 权利人:LI CHUN; WEN XIAOXIA; WU QING-PING; WALLACE SIDNEY; ELLIS LEE M 摘要:Conjugate molecules comprising a ligand bonded to a polymer are disclosed. One such conjugate molecule comprises a ligand bonded to a polymer, a chelating agent bonded to the polymer, and a radioisotope chelated to the chelating agent. The conjugate molecules may be useful in detecting and/or treating tumors or biological receptors. These conjugate molecules may be synthesized without the necessity of preactivation of the ligand using an SCN-polymer-chelating agent precursor. Conjugate molecules incorporating an annexin V ligand are particularly useful for visualizing apoptotic cells. Conjugate molecules incorporating a C225 ligand are particularly useful for targeting tumors expressing EGFR.
专利号:US-11426470-B2 优先权日:2019-01-17 标 题 :Complex of gadolinium and a chelating ligand derived of a diastereoisomerically enriched PCTA and synthesis method 发明人:LE GRENEUR SOIZIC; CHÉNEDÉ ALAIN; CERF MARTINE; DECRON STÉPHANE; FRANÇOIS BRUNO 权利人:GUERBET SA 摘要:The present invention relates to a complex of formula (II) constituted of at least 80% of a diastereoisomeric excess comprising a mixture of isomers II-RRR and II-SSS of formulae: n n n n n n n n n n The present invention also relates to a process for preparing said complex of formula (II), and also to two synthetic intermediates.