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-9963472-B2 优先权日:2013-11-04 标 题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (PKAN) and methods for the synthesis of such compounds 发明人:JENKO BRANKO; KOSEC GREGOR; PETKOVIC HRVOJE; PODGORSEK BERKE AJDA; PAHOR JERCA; CUSAK ALEN; SIBON ODA CORNELIA MARIA; SRINIVASAN BALAJI 权利人:ACIES BIO D O O; UNIV GRONINGEN; ACADEMISCH ZIEKENHUIS GRONINGEN 摘要:The invention relates to (S)-acyl-4′-phosphopantetheine derivatives, methods of their synthesis, and related medical uses of such compounds. Preferred medical uses relate to the treatment of neurodegenerative diseases, such as PKAN.
专利号:WO-9511893-A1 优先权日:1993-10-27 标题 :Compounds and methods for synthesizing pantethine, pantetheine and derivatives thereof 发明人:PATIL GHANSHYAM 权利人:OCULON CORP 摘要:There is disclosed compounds and methods for the synthesis of pantethine, pantetheine, and derivatives thereof. The methods utilize crystalline derivatives of the above compounds as intermediates which readily permit purification by recrystallization, and thus allow the generation of highly pure products. The synthesis utilizes the 1,3-diol functional group present in pantothenic acid to produce the crystalline derivatives by formation of ketal intermediates. Subsequent hydrolisis of the ketal intermediates yields pantethine or pantetheine in highly pure form.
专利号:US-2024173273-A1 优先权日:2021-03-24 标 题 :Use of pantethine for the treatment of sars cov-2 infections 发明人:LAFORGE MIREILLE; ABOU HAMDAN MOHAMAD; DE REGGI LUCIEN; SALEH RACHELLE 权利人:INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT; UNIV PARIS CITE; LEBANESE UNIV 摘要:SARS-COV and SARS-COV-2 share similar pathogenic pathways that interact with pathways of cellular cholesterol metabolism. Depletion of cholesterol from cell membranes reduced the infectivity of SARS-COV by 90%. Several studies reported that pantethine was able to reduce total cholesterol levels and total fatty acids synthesis but its anti-SARS COV-2 activity has never been investigated. The inventors now demonstrate that pantethine is highly effective in the control of SARS-COV-2 infections in vitro. In particular, the inventors show that the effect of pathethine on the inhibition of the replication of SARS-COV-2 is interested at the dose of 100 μM (inhibition is around 76%) and the most effective concentration is 1000 μM (inhibition is around 98%). Pantethine treatments were able to reduce significantly the expression of the viral Spike and Nucleocapsid proteins and the accessory proteins ORF6. Thus the present invention relates to the use of pantethine for the treatment of a SARS COV-2 infection.
专利号:EP-1600499-B1 优先权日:2003-03-03 标 题 :Process for producing lactonase and utilization thereof 发明人:SHIMIZU SAKAYU; KATAOKA MICHIHIKO; SAKAMOTO KEIJI 权利人:DAIICHI FINE CHEM CO LTD 摘要:It has been required to economically produce a large amount of optically active gamma -lactone derivatives (for example, pantolactone), which are useful as intermediates in synthesizing useful substances such as pharmaceutical drugs. To achieve this object, it is advantageous to employ an enzymatic technique of asymmetric hydrolysis with a hydrolyzing enzyme lactonase. However, it remains troublesome to prepare the enzyme or utilize a microorganism capable of producing the enzyme. Also, it is difficult to obtain a sufficient and stable enzymatic activity in the case of using recombination techniques. In producing lactonase, which asymmetrically hydrolyzes a gamma -lactone derivative such as racemic pantolactone selectively, by a recombination technique, both mature lactonase DNA and signal peptide region DNA are transferred into a host. Thus, a stable lactonase activity comparable to naturally-occurring one can be achieved and a transformant sustaining a high enzyme activity in a stable manner can be acquired, thereby allowing the efficient and industrially advantageous asymmetric synthesis of gamma -lactone derivatives.
专利号:US-2018118767-A1 优先权日:2013-11-04 标题 :Stable pantetheine derivatives for the treatment of pantothenate kinase associated neurodegeneration (pkan) and methods for the synthesis of such compounds
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合成参考文献
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