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Topic: Oxazolidinones

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	Ink jet inks containing oxazolidinones - Patent 5882389 (Site not responding. Last check: 2007-10-29)
		An ink composition according to claim 1 wherein the oxazolidinone compound is 3-methyl-2-oxazolidinone, 3-ethyl-2-oxazolidinone, 3-butyl-2-oxazolidinone, 3-cyclohexyl-2-oxazolidinone, 3-(hydroxyethyl)-2-oxazolidinone, 4-methyl-2-oxazolidinone, 5-methyl-2-oxazolidinone, 3,5-dimethyl-2-oxazolidinone, 3-ethyl-5-methyl-2-oxazolidinone, 3-butyl-5-methyl-2-oxazolidinone, 3-(2-hydroxypropyl)-5-methyl-2-oxazolidinone, 4-ethyl-2-oxazolidinone, 5-ethyl-2-oxazolidinone, 4,4-dimethyl-2-oxazolidinone, 5,5,3-trimethyl-2-oxazolidinone, 5-methyl-3-ethyl-2-oxazolidinone, 3-(2-hydroxypropyl)-5-methyl-2-oxazolidinone, 5-isopropyl-3-methyl-2-oxazolidinone, 5-ethyl-4-methyl-2-oxazolidinone, 5-methyl-3-(hydroxyethyl)-2-oxazolidinone, 4,5-dimethyl-3-(hydroxyethyl)-2-oxazolidinone, 5,5-dimethyl-3-ethyl-2-oxazolidinone, 3,5-diethyl-5-methyl-2-oxazolidinone, 5-methyl-3-cyclohexyl-2-oxazolidinon e, 4,5-dimethyl-3-cyclohexyl-2-oxazolidinone, 3,4,5-trimethyl-2-oxazolidinone, 3-butyl-4-ethyl-5-methyl-2-oxazolidinone, 4-ethyl-2-oxazolidinone, 4,4-diethyl-2-oxazolidinone, 5,5-diethyl-3-methyl-2-oxazolidinone, 3-(hydroxyethoxyethyl)-2-oxazolidinone, or mixtures thereof.
		A process according to claim 11 wherein the oxazolidinone compound is 3-methyl-2-oxazolidinone, 3-ethyl-2-oxazolidinone, 3-butyl-2-oxazolidinone, 3-cyclohexyl-2-oxazolidinone, 3-(hydroxyethyl)-2-oxazolidinone, 4-methyl-2-oxazolidinone, 5-methyl-2-oxazolidinone, 3,5-dimethyl-2-oxazolidinone, 3-ethyl-5-methyl-2-oxazolidinone, 3-butyl-5-methyl-2-oxazolidinone, 3-(2-hydroxypropyl)-5-methyl-2-oxazolidinone, 4-ethyl-2-oxazolidinone, 5-ethyl-2-oxazolidinone, 4,4-dimethyl-2-oxazolidinone, 5,5,3-trimethyl-2-oxazolidinone, 5-methyl-3-ethyl-2-oxazolidinone, 3-(2-hydroxypropyl)-5-methyl-2-oxazolidinone, 5-isopropyl-3-methyl-2-oxazolidinone, 5-ethyl-4-methyl-2-oxazolidinone, 5-methyl-3-(hydroxyethyl)-2-oxazolidinone, 4,5-dimethyl-3-(hydroxyethyl)-2-oxazolidinone, 5,5-dimethyl-3-ethyl-2-oxazolidinone, 3,5-diethyl-5-methyl-2-oxazolidinone, 5-methyl-3-cyclohexyl-2-oxazolidinon e, 4,5-dimethyl-3-cyclohexyl-2-oxazolidinone, 3,4,5-trimethyl-2-oxazolidinone, 3-butyl-4-ethyl-5-methyl-2-oxazolidinone, 4-ethyl-2-oxazolidinone, 4,4-diethyl-2-oxazolidinone, 5,5-diethyl-3-methyl-2-oxazolidinone, 3-(hydroxyethoxyethyl)-2-oxazolidinone, or mixtures thereof.
		Oxazolidinones wherein the ring nitrogen atom is bonded to a hydrogen atom rather than to an alkyl group may be preferred in some instances for their ability to impart to the ink higher surface tension and greater paper compatibility.
	www.freepatentsonline.com /5882389.html (4531 words)

	Catalytic process for converting oxazolidinones to their corresponding aminoalcohols - Patent 4281200
		The method of claim 4 wherein the source of the oxazolidinone is the reclaimer bottoms from a gas treating process employing a mixture of sulfolane and an alkanolamine to separate carbon dioxide from a gas stream comprising same.
		The method of claim 1 wherein the oxazolidinone is contacted with the inorganic base by virtue of the in situ formation of the oxazolidinone in a gas treating process stream employing an aqueous alkanolamine containing a catalytic amount of the inorganic base and, optionally, sulfolane.
		It would be, therefore, advantageous to have a process for converting the cyclic nirogen compounds (the oxazolidinones) back to their corresponding amino alcohols without the generation of the large solids volume of the conventional base conversions, without the use of elevated pressure or indeed without any separate step of separating and treating oxazolidinone "bottoms".
	www.freepatentsonline.com /4281200.html (1658 words)

	5-trityloxymethyl-oxazolidinones and process for the preparation thereof - US Patent 6288239 (Site not responding. Last check: 2007-10-29)
		Oxazolidinones are an important class of molecules in the pharmaceutical industry especially in the areas of antimicrobials and behavioral disorders.
		Optically pure oxazolidinones can be obtained by carbonylation of vicinal amino alcohols with reagents such as phosgene, ethyl chloroformate and carbonyl imidazole.
		Oxazolidinones have emerged as a very important class of compounds in drug development especially in the areas of antimicrobials (Diekema, D. J., et al., Drugs 59 7-16 (2000)) and behavioral disorders (Brenner, R., et al., Clin.
	www.patentstorm.us /patents/6288239.html (1987 words)

	INFORMEX® - SOCMA - Press Room/Important Links (Site not responding. Last check: 2007-10-29)
		Oxazolidinones were used to develop Zyvox, which is the most effective drug on the market today to treat drug resistant bacteria.
		The oxazolidinone breakthrough came in Spring 2000, when Dr. Hollingsworth and his research team at Michigan State University (MSU) developed a direct synthesis of optically active oxazolidinone intermediates from carbohydrates and outlined a strategy for their combinatorial transformation to drug candidates.
		Oxazolidinones are the basic compounds used in a number of therapeutic agents including antibiotics, antidepressants and antihypertensives.
	www.informex.com /pressroom/SynthonHarvardRel.htm (682 words)

	Patent 6,562,820
		In another embodiment the invention is directed to a method of treating or preventing mastitis in a mammal comprising administering to said mammal a therapeutically effective amount of an oxazolidinone in combination with administration of an exogenous lactoferrin at amount effective to enhance the therapeutic effect of the oxazolidinone.
		When lactoferrin is used in combination with the oxazolidinones, the lactoferrin should be administered via intramammary injection, typically by infusion into the teat through the milk canal, and in the same frequency and duration as the oxazolidinones.
		In another embodiment, the invention is directed to a composition for use in the treatment or prevention of mastitis in a mammal, comprising (a) an oxazolidinone and (b) a lactoferrin at an amount effective to enhance the therapeutic effect of said oxazolidinone.
	www.pharmcast.com /Patents/Yr2003/May2003/051303/6562820_Mastitis051303.htm (1195 words)

	The protein synthesis inhibitors, oxazolidinones and chloramphenicol, cause extensive translational inaccuracy in vivo. (Site not responding. Last check: 2007-10-29)
		The oxazolidinone family is a new class of synthetic antibiotics that bind to the bacterial 50S ribosomal subunit.
		Two members of the family, linezolid and XA043, were examined for their effects on translational fidelity using a lacZ reporter gene in vivo.
		Neither the oxazolidinones nor chloramphenicol stimulated misincorporation of amino acid residues at position 461 in the lacZ gene.
	www.pdg.cnb.uam.es /UniPub/iHOP/gp/9549031.html (158 words)

	Oxazolidinone Resistance Mutations in 23S rRNA of Escherichia coli Reveal the Central Region of Domain V as the Primary ...
		Oxazolidinone antibiotics inhibit bacterial protein synthesis by interacting with the large ribosomal subunit.
		The oxazolidinone eperezolid binds to the 50S ribosomal subunit and competes with binding of chloramphenicol and lincomycin.
		Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721.
	jb.asm.org /cgi/content/full/182/19/5325 (4541 words)

	1-Oxa-3-azapentalen-2-ones as precursors (Site not responding. Last check: 2007-10-29)
		Oxazolidinones (3) are often prepared by the addition of organometallic compounds to oxazolidin-2,4-diones.
		The oxazolidinone cycle is characterized by the twist conformation with the deviation of C(11) and C(12) atoms by 0.218 and -0.186, correspondingly.
		All steps of the synthesis (dioxolanone 1 to oxazolidinone 3 to azapentalenone 5 or/and 4) proceed with good yields and under mild conditions, with easy separation of products i (intermediates 3 may be used without isolation).
	www.arkat-usa.org /ark/journal/2000/I04_General/0-060B/0055.asp (3463 words)

	Patent 6,740,652
		The ophthalmic infections are treated by administering the desired OXAZOLIDINONE(s) directly to the eye by use of a pharmaceutical formulation consisting of a solution, cream, ointment, emulsion, suspension and slow release formulations.
		It is preferred that the ophthalmologically effective amount of the OXAZOLIDINONE for treatment of ophthalmic infections is from about 0.3% to about 20%, it is more preferred that the ophthalmologically effective amount be from about 0.5% to about 18%.
		The OXAZOLIDINONE should be administered in the pharmaceutical formulation two thru four times daily for 7 thru 10 days or until the infection is gone.
	www.pharmcast.com /Patents100/Yr2004/May2004/052504/6740652_Eye052504.htm (1839 words)

	(S)-4-(4-AMINOBENZYL)-2-OXAZOLIDINONE
		Oxazolidinones, containing not only nitrogen but also oxygen atom in lactam ring, are used in developing novel drug especially antibiotics of low toxicity for the host but effective against penicillin-resistant pathogens.
		Chiral oxazolidinones are used in the enantioselective synthesis of beta-lactams and alpha-amino acids.
		Chiral oxazolidinones have wide and effective chiral applications as chiral auxiliaries, building blocks and ligands.
	www.chemicalland21.com /bioscience/Chiral/(S)-4-(4-AMINOBENZYL)-2-OXAZOLIDINONE.htm (282 words)

	Catalytic Properties of Mutant 23 S Ribosomes Resistant to Oxazolidinones -- Bobkova et al. 278 (11): 9802 -- Journal ...
		Oxazolidinones, the only novel class of antibiotics identified in the last two decades, are the focus of intensive discovery
		Oxazolidinones impose their action at the initiation stage of translation (4, 5), apparently via inhibition of preinitiation
		to conclude that oxazolidinones are inhibitors of the peptidyltransferase
	www.jbc.org /cgi/content/full/278/11/9802 (3300 words)

	Oxazolidinones (from drug) -- Encyclopædia Britannica
		The oxazolidinones are a novel class of synthetic agents that inhibit protein synthesis by microbes.
		Linezolid is highly active in vivo against infections caused by many common gram-positive pathogens, including Enterococcus bacteria that are resistant to vancomycin (described in the section Other antibiotics).
		More results on "Oxazolidinones (from drug)" when you join.
	www.britannica.com /eb/article-233929 (817 words)

	Activities of Several Novel Oxazolidinones against Mycobacterium tuberculosis in a Murine Model -- Cynamon et al. 43 ...
		Oxazolidinones are a new class of antibacterial protein synthesis inhibitors.
		The oxazolidinones represent a novel class of antibacterial agents whose mechanism of action appears to be inhibition of an
		Oxazolidinone, a new class of synthetic antituberculosis agent: in vitro and in vivo activities of DuP-721 against Mycobacterium tuberculosis.
	aac.asm.org /cgi/content/full/43/5/1189 (2125 words)

	Pfizer, Vicuron in $1.9 billion merger (Site not responding. Last check: 2007-10-29)
		Oxazolidinones are the first new class of antibiotics in more than 30 years.
		The deal could be indicative of an anti-infectives market that is getting back on track after a disappointing 2004 in which growth declined nearly 4 per cent.
		Pfizer’s decision to enter the market for newer classes of these drugs, which include the oxazolidinones and additionally carbapenems, will likely show excellent growth as antibiotic resistance continues to be a growing problem for older agents.
	www.drugresearcher.com /news/printNewsBis.asp?id=60707 (668 words)

	Bicyclic oxazolidinones as antibacterial agents - US Patent 6387896 (Site not responding. Last check: 2007-10-29)
		The oxazolidinone antibacterial agents are a novel synthetic class of antimicrobials with potent activity against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci and streptococci, anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.
		Thus, the use of these oxazolidinone antibacterial agents is limited to infectious states due to gram-positive bacteria.
		The oxazolidinone antibacterial agents of this invention have useful activity against a variety of organisms.
	www.patentstorm.us /patents/6387896.html (12987 words)

	Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability ... (Site not responding. Last check: 2007-10-29)
		Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability for the development of novel oxazolidinones.
		Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability for the development of novel oxazolidinones.In addition, the human plasma concentration-time curve was simulated using a one-compartmental model.
		The pharmacokinetic data for linezolid, a novel oxazolidinone to treat Gram-positive pathogens, in mice, rats and dogs were subjected to simple allometric scaling.
	www.pdg.cnb.uam.es /UniPub/iHOP/gp/10479771.html (292 words)

	Publication: Oxazolidinones: activity, mode of action, and mechanism of resistance.
		Oxazolidinones: activity, mode of action, and mechanism of resistance.
		Oxazolidinones inhibit protein synthesis by binding at the P site at the ribosomal 50S subunit.
		Resistance to other protein synthesis inhibitors does not affect oxazolidinone activity, however rare development of oxazolidinone resistance cases, associated with 23S rRNA alterations during treatment have been reported.
	www.fred.psu.edu /ds/retrieve/fred/publication/15013035 (146 words)

	European Society of Clinical Microbiology and Infectious Diseases
		The oxazolidinones have a unique mechanism of action, inhibiting the formation of the initiation complex in ribosomal protein synthesis.
		Since most of the important gram-positive pathogens have multiple copies of this gene and it requires more than a single mutation to develop clinical resistance, bacteria have been slow to develop immunity to these compounds.
		A number of new oxazolidinones are being developed in an attempt to improve on the valuable properties of linezolid.
	www.blackwellpublishing.com /eccmid15/abstract.asp?id=36202 (341 words)

	New Class of Antibiotics Show Promise in Treating Drug-Resistant Diseases (Site not responding. Last check: 2007-10-29)
		Oxazolidinones, which can be administered orally as well as intravenously, are the first new class of antibiotics to be showcased at this important meeting in a number of years.
		"Oxazolidinones are likely to command considerable attention in light of the urgent need for new therapeutic options," said Charles W. Ford, Ph.D., who with Upjohn colleague Steven J. Brickner, Ph.D., has worked since 1987 to develop these novel drugs.
		"The implications of antibiotic resistance are enormous," said oxazolidinone investigator George M. Eliopoulos, M.D., Associate Chairman of the Department of Medicine at Deaconess Hospital in Boston.
	www.pslgroup.com /dg950921.htm (677 words)

	Activities of the Oxazolidinones Linezolid and Eperezolid in Experimental Intra-Abdominal Abscess Due to Enterococcus ...
		Activities of the Oxazolidinones Linezolid and Eperezolid in Experimental Intra-Abdominal Abscess Due to Enterococcus faecalis or Vancomycin-Resistant Enterococcus faecium -- Schülin et al.
		Levels of the oxazolidinones in plasma achieved with different treatment regimens are shown in Table 2.
		Absorption, distribution, metabolism, and excretion of the oxazolidinone antibiotic linezolid (PNU-100766) in the Sprague-Dawley rat, abstr.
	aac.asm.org /cgi/content/full/43/12/2873 (2464 words)

	OARMFMC (Site not responding. Last check: 2007-10-29)
		For example, studies on recently developed oxazolidinones suggest that Eperezolid inhibits protein synthesis initiation by selective binding to the 50S ribosomal subunits.
		The synthetic methodology of the oxazolidinone core compounds we are developing in our group utilizes readily available carbohydrates.
		These functionally rich oxazolidinone scaffolds can then be modified to provide ample numbers of structurally diverse candidates for biological assay.
	laagc.bch.msu.edu /projects/OARMFMC.htm (190 words)

	Known and selected novel arylmethylenyl derivatives of thiazolidinones, imidazolidinones and oxazolidinones useful as ... (Site not responding. Last check: 2007-10-29)
		It is now found that Compounds from among known and selected novel arylmethylenyl derivatives of thiazolidinones, oxazolidinones or imidazolidinones have activity useful for treating allergies or inflammation.
		Certain thiazolidinones and oxazolidinones are acidic (pKa.about.3-6) due to the presence of a tautomeric proton on the heterocyclic ring: ##STR14##
		If the parent oxazolidinone or thiazolidinone and choline free base or a choline derivative (such as choline bicarbonate or choline chloride) are combined in a suitable solvent (such as an alcohol, water, or an alcohol/water solution), the choline salt can generally be obtained by precipitation from solution or by evaporation of the reaction solution.
	freepatentsonline.com /5208250.html (9536 words)

	Optimization and Mechanistic study of the (Salen)Chromium(III)/DMAP Catalyzed Coupling of Carbon Dioxide and Aziridines ... (Site not responding. Last check: 2007-10-29)
		The oxazolidinone products are produced in high yield (85-97%) and selectivity (9:1-84:1) from the opening of the aziridine at the most substituted N-C bond.
		Not only has this system found to be very useful for aliphatic and aromatic aziridines, but also worked well for aziridines containing a host of electron-withdrawing and donating groups, bulky groups and wide variety of monosubstituted N-aryl and N-alkyl aziridines as well as a 2,3-disubstituted N-alkyl aziridine.
		Oxazolidinones have been shown to have potency as antibacterial agents, and this functional group is widely used in the pharmaceutical industry, specifically in several of the newest antibiotic pharmaceuticals, including furazolidone and linezolid, are based on an oxazolidinone core structure, utilizing different heterocyclic functionalities.
	acs.confex.com /acs/36glrm/techprogram/P9684.HTM (332 words)

	[No title] (Site not responding. Last check: 2007-10-29)
		The oxazolidinones are a class of orally active, synthetic antibacterial agents being studied by investigators at Pharmacia and Upjohn.
		At Pharmacia and Upjohn, we have two drug candidates, a piperazinyl fluorophenyl oxazolidinone and a morpholinyl fluorophenyl oxazolidinone and they are currently in Phase I human clinical trials.
		We have determined some crystal structures of a few oxazolidinones in an attempt to understand their activity.
	www.za.iucr.org /iucr-top/cong/17/iucr/abstracts/abstracts/E0939.html (161 words)

	Process for preparing .beta.-hydroxycarbamates and their conversion to oxazolidinones
		The process electively additional includes treаting the.beta.-hydroxy carbamate рrоduсt with extra basis to form an oxazolidinone.
		The oxazolidinones аre helpful as chiral supplementary agents and as intermediates for the formаtion of pharmaceuticaIIy involved substаnces suсh as aIpha 1 a adrenergic receptor antagonists.
		A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is as well described.
	www.patentalert.com /docs/000/z00032842.shtml (63 words)

	Pharmacoptherapy Volume 18 Number 3 / Abstracts
		The oxazolidinones are a new synthetic class of antimicrobials structurally unrelated to any agent presently marketed.
		Data pertaining to these compounds, with respect to their pharmacology, pharmacokinetics, pharmacodynamics, mechanism of action, and bacteriologic activity, focusing on the analogs linezolid (PNU 100766) and eperezolid (PNU 100592), were retrieved by MEDLINE search and review of relevant abstracts presented at recent clinical conferences.
		The oxazolidinones have bacteriostatic activity against a number of important pathogens including methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, and vancomycin-resistant enterococci.
	www.accp.com /pharmacotherapy/pharm183.html (4240 words)

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