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-2023212204-A1 优先权日:2020-01-16 标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds 发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI 权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
专利号:US-10675366-B2 优先权日:2016-08-12 标 题 :Imaging tumor glycolysis by non-invasive measurement of pyruvate kinase M2 发明人:BEINAT CORRINE GAYE; ALAM ISRAT SHAMIMA; JAMES MICHELLE L; GAMBHIR SANJIV S; SRINIVASAN ANANTH 权利人:UNIV LELAND STANFORD JUNIOR 摘要:The present disclosure provides a positron emission tomography (PET)-detectable 1-((2-fluoro-6-[18F]fluorophenyl)sulfonyl)-4-((4-methoxyphenyl)sulfonyl)piperazine ([18F]DASA-23) probe that can selectively bind to the pyruvate kinase variant M2 (PKM2) found in cancer cells, such as of human glioma. Given the importance of PKM2 in the regulation of tumor metabolism, there is an on-going need to non-invasively measure its expression through the development of PKM2-specific radiopharmaceuticals. Precursors useful for the synthesis of the radiolabeled [18F]DASA-23-PKM2-specific probe and related compounds, and their methods of synthesis, are provided. Since the half-life of the 18F isotope is approximately 110 min, it is advantageous for a practitioner to attach the radionuclide to the precursor shortly before administration. Therefore, a precursor compound suitable for receiving the radionuclide and capable of specifically binding to the PKM2 variant can be provided.
专利号:WO-2008103866-A1 优先权日:2007-02-22 标题 :Synthesis of indoles 发明人:TALLEY JOHN JEFFREY; RENZE JUERGEN T 权利人:MICROBIA INC; TALLEY JOHN JEFFREY; RENZE JUERGEN T 摘要:Method for preparing indoles, including methods that permit high yield production of particular compounds, are described.
专利号:US-7361773-B2 优先权日:2002-03-12 标题 :Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines 发明人:CHAN ANITA WAI-YIN; FEIGELSON GREGG BRIAN; ZELDIS JOSEPH; JIRKOVSKY IVO LADISLAV 权利人:WYETH CORP 摘要:A process for making a compound of the formula comprising dialkylating a benzodioxane aniline
专利号:US-7842834-B2 优先权日:2005-07-21 标 题:Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts 发明人:MICHALAK RONALD S; HELOM JEAN L; ZELDIS JOSEPH 权利人:WYETH LLC 摘要:The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar—(R) z —SO 2 —X and sulfonamides of Formula Ar—(R) z —SO 2 —NR 4 R 5 , where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals.
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合成参考文献
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