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-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: Processes For Synthesis Of 1,3,3,3-Tetrafluoropropene And 2,3,3,3-Tetrafluoropropene Procedes Pour La Synthese De 1,3,3,3-Tetrafluoropropene Et De 2,3,3,3-Tetrafluoropropene 摘要:Disclosed In One Embodiment Is A Process For The Synthesis Of 1,3,3,3-Tetrafluoropropene That Comprises (A) Reacting A Compound Of Formula (I) X1X2 With A Compound Of Formula (II) Cf3Ch=ch2 To Produce A Reaction Product Comprising A Compound Of Formula (III) Cf3Chx1Ch2X2, Wherein X1 And X2 Are Each Independently Selected From The Group Consisting Of Hydrogen, Chlorine, Bromine And Iodine, Provided That X1 And X2 Are Not Both Hydrogen; (B) When X2 In Formula (III) Is Not Fluorine, Fluorinating The Compound Of Formula (III) To Produce A Reaction Product Comprising A Compound Of Formula (III) Wherein X1 Is As Described Above And X2 Is Fluorine; And (C) Exposing Said Compound Of Formula (III) To Reaction Conditions Effective To Convert Said Compound To 1,3,3,3,-Tetrafluoropropene. In Another Embodiment, The Process Comprises (A) Reacting Chlorine With A Compound Of Formula (I) Ch3Ch=ch2 To Produce A Reaction Product Comprising A Compound Of Formula (II) Cci3Chc1Ch2C1; (B) Fluorinating The Compound Of Formula (II) To Produce A Reaction Product Comprising A Compound Of Formula (III) Cf3Chc1Ch2F; And (C) Exposing Said Compound Of Said Formula (III) To Reaction Conditions Effective To Convert Said Compound To 1,3,3,3-Tetrafluoropropene.
合成参考文献
摘要:Journal of Pharmacology and Experimental Therapeutics., 86(197), 1946