专利号:US-2009099061-A1 优先权日:2006-01-27 标 题:Synthesis of carotenoid analogs or derivatives with improved antioxidant characteristics 发明人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 权利人:FOSS BENTE J; NADOLSKI GEOFFRY T; LOCKWOOD SAMUEL F 摘要:A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.
专利号:US-5137660-A 优先权日:1991-03-15 标题:Regioselective synthesis of 1,3-disubstituted glycerides 发明人:MAZUR ADAM W; HILER II GEORGE D 权利人:PROCTER & GAMBLE 摘要:A process for the selective esterification of glycerol and 1-glyceryl derivatives to 1,3-disubstituted glycerides is disclosed. This process uses a water immiscible solvent, either a hydrocarbon or halogenated hydrocarbon, a 1,3-lipase and fatty acid anhydrides. This reaction mixture selectively esterifies the primary alcohol groups of glycerol or glycerol derivatives. The preferred derivatives of glycerol are alkyl ethers, alkyl phosphates, phospholipids, alkyl and diaklyl phosphates, and sugar glycosides.
专利号:US-7344868-B2 优先权日:2003-06-03 标题:Method for synthesizing ceramide-type compounds 发明人:LASSALLE LAURENT; YVERGNAUX FLORENT 权利人:LASSALLE LAURENT; YVERGNAUX FLORENT 摘要:The invention relates to the fields of fatty substance chemistry, specifically of the ceramide-type compound synthesis. The invention resides substantially in the synthesis of ceramide-type compounds. Specifically, the aim of the invention is a new enzymatic synthesis method, comprising at least one amidification step and one esterification step, achieved through lipases, among fatty acids and/or esters thereof and amino alcohols. The resulting ceramide-type compounds can be used as cosmetic and/or pharmaceutical compositions, in particular as dermatological compositions in conjunction or in admixture with one or more suitable cosmetic and/or pharmaceutical excipients or carriers. The method has an interest particularly in the synthesis of active compounds useful in the fields of cosmetology and/or pharmacology and specifically of dermatology.
专利号:US-2012282652-A1 优先权日:2011-02-28 标题 :Preparation of peptide mixtures by protease catalysis designed to provide useful biological and physical properties 发明人:GROSS RICHARD A; VISWANATHAN KODANDARAMAN; QIN XU 权利人:GROSS RICHARD A; VISWANATHAN KODANDARAMAN; QIN XU; POLITECHNIC INST UNIV NEW YORK 摘要:A process for preparing unique peptide mixtures with a broad range of uses using combinations of natural and non-natural amino acid alkyl ester monomers and specific combinations of these monomers as dimers, trimers and higher oligomers selected from the large group of structural motifs that lead to useful physical and/or biological properties and that have been or may be identified from solid state peptide synthesis, isolation of peptides from natural sources, and production of peptides by recombinant DNA methods, or identification of peptides by recombinant methods such as phage display, the method of peptide synthesis comprising a) admixing one or more natural and non-natural amino acid alkyl ester monomer, dimer, trimer and higher oligomers with one or more proteases in a reaction medium; b) heating the mixture to between about 5° C. to about 90° C. for between 5 minutes and 24 hours; and c) recovering the formed oligopeptide.
专利号:US-8183409-B2 优先权日:2004-05-06 标题:High yield and rapid synthesis methods for producing metallo-organic salts 发明人:CHRISTGAU STEPHAN; ANDERSEN JENS E T 权利人:CHRISTGAU STEPHAN; ANDERSEN JENS E T; OSTEOLOGIX AS 摘要:A new method for preparing salts of metal cations and organic acids, especially divalent salts of alkaline earth metal ions from group II of the periodic system and carboxylic acids. The method comprising the use of a high temperature (about 90° or more) and, optionally. high pressure, in order to obtain a higher yield, purity and faster reaction speed than obtained with known synthesis methods. In particular, the present invention relates to the production of strontium salts of carboxylic acids. Novel strontium salts are also provided by the present method.
专利号:US-9738678-B2 优先权日:2007-07-09 标 题 :Substituted nucleoside derivatives with antiviral and antimicrobial properties 发明人:DONCEL GUSTAVO F; PARANG KEYKAVOUS; AGARWAL HITESH KUMAR 权利人:EASTERN VIRGINIA MEDICAL SCHOOL; BOARD OF GOVERNORS FOR HIGHER EDUCATION STATE OF RHODE ISLAND AND PROVIDENCE PLANTATIONS 摘要:The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.
[参考文献]: John Marshall, Et Al. Inhibition Of N-Methyl-D-Aspartate-Induced Retinal Neuronal Death By Polyarginine Peptides Is Linked To The Attenuation Of Stress-Induced Hyperpolarization Of The Inner Mitochondrial Membrane Potential. J Biol Chem. 2015 Sep 4;290(36):22030-48. [参考文献]: K M Patel, Et Al. A Convenient Synthesis Of Phosphatidylcholines: Acylation Of Sn-Glycero-3-Phosphocholine With Fatty Acid Anhydride And 4-Pyrrolidinopyridine. J Lipid Res. 1979 Jul;20(5):674-7.
合成参考文献
参考文献:10.1007/bf02533539 摘要:Patel KM, Morrisett JD, Sparrow JT. The conversion of phosphatidylethanolamine into phosphatidylcholine labeled in the choline group using methyl lodide, 18‐crown‐6 and potassium carbonate. Lipids. 1979 Jun;14(6):596–7. doi: 10.1007/bf02533539. 参考文献:10.1038/s44222-023-00082-0 摘要:Couvreur P, Lepetre-Mouelhi S, Garbayo E, Blanco-Prieto MJ. Self-assembled lipid–prodrug nanoparticles. Nat Rev Bioeng. 2023 Jun 28;1(10):749–68. doi: 10.1038/s44222-023-00082-0.