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-5508389-A 优先权日:1990-09-27 标题 :Process for producing concentrated aqueous solutions of anionic azo dyes 发明人:MISCHKE PETER; HOHMANN KURT; SCHWAB ECKHARD; SITTIG MANFRED 权利人:HOECHST AG 摘要:PCT No. PCT/EP91/01830 Sec. 371 Date Mar. 26, 1993 Sec. 102(e) Date Mar. 26, 1993 PCT Filed Sep. 25, 1991 PCT Pub. No. WO92/06140 PCT Pub. Date Apr. 16, 1992.If highly concentrated aqueous solutions of azo dyes are prepared directly by diazotization and coupling reactions, appreciable difficulties generally result as a consequence of the fact that the diazotization and coupling reactions give rise to viscous phases which lead to stirring problems in the reaction apparatus used, which in turn results in an incomplete synthesis. The novel process for preparing concentrated aqueous dye solutions of an anionic dye in an aqueous medium overcomes this disadvantage by carrying out the diazotization of the aromatic amine diazo component and/or the coupling reaction between the diazonium salt and the coupling component in the presence of an auxiliary which exerts a viscosity-reducing effect on pasty phases. Examples of such auxiliaries are optionally alkyl-substituted naphthalenesulfonic acid-formaldehyde condensation products, ligninsulfonates, polyacrylates and copolymers of maleic anhydride and methacrylic acid or acrylic acid.
专利号:US-4390342-A 优先权日:1980-04-01 标 题:Process for the preparation of solid composition of water-soluble dyes 发明人:BRUTTEL BEAT; PFENNINGER HEINZ 权利人:CIBA GEIGY CORP 摘要:A process for producing solid dye compositions, which process comprises passing an aqueous solution or suspension of at least one water-soluble crude dye, to effect separation of synthesis by-products having a molecular weight of below 500 and partial separation of water, through a semipermeable membrane, subsequently drying the resulting aqueous preparation which has become more highly concentrated, and optionally adding further additives before and/or after passage of the aqueous solution or suspension through the semipermeable membrane, these additives being added beforehand only when they do not become separated by the membrane. There are obtained by this process low-dust to dust-free compositions which are distinguished by high mechanical strength, high bulk density, free-flowing characteristics and good dissolving behavior. Employing these compositions it is possible to prepare low-foam to foam-free aqueous dye liquors having very good solution stability, even in the presence of electrolytes.
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:WO-9718209-A1 优先权日:1995-11-15 标 题:ALPHA 1a ADRENERGIC RECEPTOR ANTAGONISTS 发明人:BOCK MARK G; PATANE MICHAEL A 权利人:MERCK & CO INC; BOCK MARK G; PATANE MICHAEL A 摘要:This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha 1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
专利号:CN-101234996-B 优先权日:2008-02-29 标题:A kind of green synthesis method of ketazine