专利号:US-7923584-B2 优先权日:2008-01-23 标题 :Synthesis of difunctional oxyethylene-based compounds 发明人:HOLMES BRIAN T; SNOW ARTHUR W 权利人:US NAVY 摘要:A method of reacting a toluenesulfonyl-terminated polyoxyethylene compound having the formula CH 3 —C 6 H 4 —SO 2 —(O—CH 2 —CH 2 ) n —O—R 1 with an ammonium salt having the formula NR 2 4 X to form a compound having the formula X—CH 2 —CH 2 —(O—CH 2 —CH 2 ) n-1 —R 3 . The value n is a positive integer. X is a halogen, cyanide, cyanate, thiocyanate, or azide. R 1 is a terminating group. Each R 2 is hydrogen or an alkyl group. —R 3 is —O—R 1 or —X.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:US-9889182-B2 优先权日:2009-09-15 标 题 :Assisted enzyme replacement therapy 发明人:ESKO JEFFREY D; TOR YITZHAK 权利人:ESKO JEFFREY D; TOR YITZHAK; UNIV CALIFORNIA 摘要:Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various therapeutic compounds and treatment modalities using these conjugates.
专利号:US-2009187037-A1 优先权日:2008-01-23 标题:Synthesis of difunctional oxyethylene-based compounds
专利号:US-7179794-B2 优先权日:1998-06-08 标题 :Multivalent macrolide antibiotics 发明人:GRIFFIN JOHN H; PACE JOHN L 权利人:THERAVANCE INC 摘要:Disclosed are multibinding compounds which include macrolide antibiotics, aminoglycosides, lincosamides, oxazolidinones, streptoramins, tetracycline and/or other compounds which bind to bacterial ribosomal RNA and/or to one or more proteins involved in ribosomal protein synthesis in the bacterium, which are useful in treating bacterial infections. The compounds adversely affect protein expression and have an antibacterial effect. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is macrolide antibiotic, aminoglycoside, lincosamide, oxazolidinone, streptogramin, tetracycline or other compound which binds to bacterial ribosomal RNA and/or one or more proteins involved in ribosomal protein synthesis in the bacterium.
参考标题:Synthesis Of Difunctional Oxyethylene-Based Compounds 摘要:A Method Of Reacting A Toluenesulfonyl-Terminated Polyoxyethylene Compound Having The Formula Ch 3 -C 6 H 4 -So 2 -(O-Ch 2 -Ch 2 ) N -O-R 1 With An Ammonium Salt Having The Formula Nr 2 4 X To Form A Compound Having The Formula X-Ch 2 -Ch 2 -(O-Ch 2 -Ch 2 ) N-1 -R 3 . The Value N Is A Positive Integer. X Is A Halogen, Cyanide, Cyanate, Thiocyanate, Or Azide. R 1 Is A Terminating Group. Each R 2 Is Hydrogen Or An Alkyl Group. -R 3 Is -O-R 1 Or -X.
合成参考文献
摘要:Toxicology and Applied Pharmacology., 28(313), 1974 []