专利号:WO-2023039068-A1 优先权日:2021-09-08 标题:Compositions and methods for synthesis of peptide nucleic acid intermediates 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:NEUBASE THERAPEUTICS INC 摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
专利号:US-7459443-B2 优先权日:1999-04-08 标 题 :Synthesis of biologically active compounds in cells 发明人:SERGEEV PAVEL 权利人:SERGEEV PAVEL 摘要:This invention relates to a new method of synthesis of biologically active substances of determined structure directly in the cells of living organisms containing specific RNA or DNA molecules of determined sequence. The method is based on the hybridization of two or more oligomers bound with biologically inactive precursors of biologically active substances to specific RNA or DNA in vivo in the cells of living organisms. After hybridization of the oligomers to RNA or DNA the biologically inactive precursors bound to the 5′ and/or 3′ ends of the oligomers can interact with each other to make biologically active form of the substances. This changing of properties is due to chemical reactions which bind the biologically inactive precursors through a chemical bond into a biologically active form of the whole compound.
专利号:US-2007088086-A1 优先权日:1999-08-16 标题 :Method of using synthetic L-Se-methylselenocysteine as a nutriceutical and a method of its synthesis 发明人:SPALLHOLZ JULIAN E; REID TED W; WALKUP ROBERT D 权利人:PHARMASE INC 摘要:A synthesis of and use for L-Se-methylselenocysteine as a nutriceutical is described, based upon the knowledge that L-Se-methylselenocysteine is less toxic than L-selenomethionine towards normal cells. The synthesis proceeds by mixing N-(tert-butoxycarbonyl)-L-serine with a dialkyl diazodicarboxylate and at least one of a trialkylphosphine, triarylphosphine, and phosphite to form a first mixture that includes N-(tert-butoxycarbonyl)-L-serine β-lactone. Methyl selenol or its salt is mixed with the N-(tert-butoxycarbonyl)-L-serine β-lactone to form a second mixture that includes N-(tert-butoxycarbonyl)-Se-methylselenocysteine. The tert-butoxycarbonyl group is removed from the N-(tert-butoxycarbonyl)-Se-methylselenocysteine to form L-Se-methylselenocysteine. This synthesis significantly improves the manufacturability, manufacturing efficiency, and utility of this naturally occurring rare form of organic-selenium. L-Se-methylselenocysteine formed, for example, in this manner may be used as a nutriceutical for supplementation into the diets of humans or animals for various beneficial purposes, such as, for example, to prevent or reduce the risk of developing cancer.
专利号:EP-1205471-A1 优先权日:2000-10-02 标题:A method of using synthetic L-SE-Methylselenocysteine as a nutriceutical and a method of its synthesis 发明人:SPALLHOLZ JULIAN E; REID TED W; WALKUP ROBERT D 权利人:PHARMASE INC 摘要:A synthesis of and use of L-Se-methylselenocysteine as a nutriceutical isndescribed, based upon the knowledge that L-Se-methylselenocysteine is lessntoxic than L-selenomethionine towards normal cells. The synthesis proceedsnby mixing N-(tert-butoxycarbonyl)-L-serine with a dialkyl diazodicarboxylatenand at least one of a trialkylphosphine, triarylphosphine and phosphite to formna first mixture that includes N-(tert-butoxycarbonyl)-L-serine β-lactone.nMethyl selenol or its salt is mixed with the N-(tert-butoxycarbonyl)-L-serine β-lactonento form a second mixture that includes N-(tert-butoxycarbonyl)-Se-methylselenocysteine.nThe text butoxycarbonyl group is removed from the N-(tert-butoxycarbonyl)-Se-methylselenocysteinento form L-Se-methylselenocysteine.nThis synthesis significantly improves thenmanufacturability, manufacturing efficiency and utility of this naturallynoccurring rare form of organic-selenium. L-Se-methylselenocysteine formed,nfor example, in this manner may be used as a nutriceutical for supplementationninto the diets of humans or animals for various beneficial purposes, such as, fornexample, to prevent or reduce the risk of developing cancer.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-2013243770-A1 优先权日:2005-10-14 标 题:Treating diabetes using inhibitors of il-1 发明人:LAU JESPER 权利人:NOVO NORDISK AS 摘要:The present invention describes a method of treating diabetes or metabolic syndrome with a compound that inhibits (a) IL-1, (b) the synthesis of IL-1, or (c) the release of IL-1.
1: Rubino FM, Pitton M, Di Fabio D, Meroni G, Santaniello E, Caneva E, Pappini M, Colombi A. Measurement of S-methylcysteine and S-methyl-mercapturic acid in human urine by alkyl-chloroformate extractive derivatization and isotope-dilution gas chromatography-mass spectrometry. Biomed Chromatogr. 2011 Mar;25(3):330-43. doi: 10.1002/bmc.1451. Japanese. Japanese. doi: 10.1074/jbc.M110.167304. Epub 2010 Oct 5. 7: Thompson JF, Gering RK. Biosynthesis of s-methylcysteine in radish leaves. Plant Physiol. 1966 Oct;41(8):1301-7. 8: Zhao J, Ng CM, Chu IK, Siu KW, Hopkinson AC. Methionine, alpha-methylmethionine and S-methylcysteine radical cations: generations and dissociations in the gas phase. Phys Chem Chem Phys. 2009 Sep 21;11(35):7629-39. Japanese. Japanese. Epub 2005 Dec 7. Japanese.
合成参考文献
摘要:Faber, K.; Glueck, S. M., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 438.