专利号:US-10925977-B2 优先权日:2006-10-05 标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications 发明人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S 权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS 摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.
专利号:US-2024197774-A1 优先权日:2021-04-16 标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles 发明人:LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO 权利人:UNIV TEXAS 摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.
专利号:US-2005186197-A1 优先权日:2002-08-29 标 题:Peptide inhibitors of beta lactamases 发明人:PALZKILL TIMOTHY; HUANG WANZHI 摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.
专利号:US-2022233673-A1 优先权日:2019-06-04 标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF 发明人:BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M 权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND 摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.
专利号:US-9125880-B2 优先权日:2002-12-26 标 题:Polymer conjugates of interferon-beta with enhanced biological potency 发明人:SAIFER MARK G P; MARTINEZ ALEXA L; WILLIAMS L DAVID; SHERMAN MERRY R 权利人:SAIFER MARK G P; MARTINEZ ALEXA L; WILLIAMS L DAVID; SHERMAN MERRY R; MOUNTAIN VIEW PHARMACEUTICALS 摘要:Methods are provided for the synthesis of polymer conjugates of cytokines and receptor-binding antagonists thereof, especially a non-glycosylated interferon-beta, which conjugates retain unusually high biological potency. Preparation of polymer conjugates according to the methods of the present invention diminishes or avoids steric inhibition of receptor-ligand interactions that commonly results from the attachment of polymers to receptor-binding regions of cytokines, as well as to agonistic and antagonistic analogs thereof. The invention also provides conjugates and compositions produced by such methods. The conjugates of the present invention retain a high level of biological potency compared to those produced by traditional polymer coupling methods that are not targeted to avoid receptor-binding domains of cytokines. In assays in vitro, the biological potency of the conjugates of non-glycosylated interferon-beta of the present invention is substantially higher than that of unconjugated interferon-beta and is similar to that of interferon-beta-1a that is glycosylated. The conjugates of the present invention also exhibit an extended half-life in vivo compared to the corresponding unconjugated cytokine. The present invention also provides kits comprising such conjugates and/or compositions, and methods of use of such conjugates and compositions in a variety of diagnostic, prophylactic and therapeutic applications, including treatment of multiple sclerosis.
专利号:US-2022395555-A1 优先权日:2020-06-11 标题:Derivatives of antibiotics 发明人:FARBER BORIS; FARBER SOF'YA; MARTYNOV ARTUR VIKTOROVICH 权利人:FARBER BORIS; FARBER SOFYA; MARTYNOV ARTUR VIKTOROVICH 摘要:Field of application: The invention relates to chemistry, pharmacy and cosmetology, allows to synthesize of supramolecular structure on base antibiotics derivatives for use in pharmacy, cosmetology and pharmacy. n The essence of the invention: a new derivatives of antibiotics based on supramolecular structures and a method for their preparation, characterized in that the supramolecular structures are obtained by combinatorial synthesis of an antibiotic from one source molecule with two or more groups available in the reaction for covalent modification, at least with two different modifiers simultaneously, this creates a mixture of modified derivatives of the original molecule, with a maximum variety of derivatives with forming new supramolecular structure, and as biologically active substances to create pharmaceutical compositions use such supramolecular structure without separation into individual components, and in the reaction a combinatorial mixture of modified derivatives of the original molecule is formed antibiotic, the maximum number of combinations. n Technical result: modified combinatorial derivatives of antibiotics with antimicrobial and antifungal activity against multiresistant and pan drug resistance strains of microorganisms and fungi. Means have a wide spectrum of action, and the supramolecular and combinatorial structure of their tens and hundreds of derivatives eliminates the resistance of microorganisms.
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合成参考文献
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