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.
专利号:US-5274162-A 优先权日:1991-12-13 标 题:Antineoplastic drugs with bipolar toxification/detoxification functionalities 发明人:GLAZIER ARNOLD 权利人:GLAZIER ARNOLD 摘要:The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect. The application of this invention is exemplified by a new class of antineoplastic drugs which are designed to be selectively toxic for tumor cells bearing the enzyme guanidinobenzoatase.
专利号:US-4235813-A 优先权日:1977-01-11 标 题:Aromatic sulfonamide sulfonyl chloride compounds 发明人:SAWAGUCHI HIROSHI; UEDA HIDEO 权利人:FUJI PHOTO FILM CO LTD 摘要:An aromatic sulfonamide sulfonyl chloride, useful as an intermediate in the preparation of cyan dye-releasing redox compounds for diffusion transfer photographic materials, represented by the following general formula (I) (I) wherein A represents a divalent benzene nucleus or a divalent naphthalene nucleus, in which in each nucleus the bonding thereto is symmetrical, and a method for the synthesis thereof comprising reacting an aromatic disulfonyl chloride represented by the formula (IIa) or (IIb) (IIa) (IIb) wherein the two sulfonyl chloride groups are substituted at symmetrical positions on the benzene and the naphthylene ring, with 5-amino-1-naphthol.
参考文献:10.1055/s-0030-1258104 摘要:Barbero M, Bazzi S, Cadamuro S, Dughera S, Magistris C, Venturello P. A New Effective Synthesis of Arene Mono- and Disulfonyl Chlorides. Synlett. 2010 Jun 30;2010(12):1803–6. doi: 10.1055/s-0030-1258104.