Chalcogen Bonded Directly To The Ring Nitrogen Of The Four-membered Ring Patents (Class 514/210.15)
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Publication number: 20100144699Abstract: Use of a monobactam antibiotic of formula (I) wherein the oxyimino group i.e. >C?N—O— has Z-orientation, or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for the treatment of a bacterial infection in combination with a carbapenem antibiotic or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 19, 2008Publication date: June 10, 2010Inventors: Eric Desarbre, Malcolm G.P. Page
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Publication number: 20100137247Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100092443Abstract: The invention relates to the combination of nitrogenated heterocyclic antibacterial compounds of formula (I) with other antibacterial compounds and the use of same as drugs. The nitrogenated heterocyclic compounds are of general formula (I) wherein R1 represents a (CH2)n-NH2 or (CH2)n—NHR radical, where R is a (C1-C6) alkyl and n is equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 together form an aromatic nitrogenated heterocycle with 5 apexes with 1, 2 or 3 nitrogen atoms optionally substituted by one or several R? groups, R? being selected in the group composed of a hydrogen atom and the alkyl radicals with 1 to 6 carbon atoms, in free form, as zwitterions, and in the form of salts of pharmaceutically acceptable inorganic or organic bases and acids.Type: ApplicationFiled: August 5, 2009Publication date: April 15, 2010Applicant: NovexelInventors: Premavathy Levasseur, John Lee Pace, Kenneth Coleman, John Lowther
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Publication number: 20100087416Abstract: The present invention relates to the field of antimicrobial agents. In particular, the present invention relates to the use of aerosolized fluoroquinolones formulated with divalent or trivalent cations and having improved pulmonary availability for the treatment and management of bacterial infections of the lung and upper respiratory tract.Type: ApplicationFiled: October 6, 2009Publication date: April 8, 2010Applicant: MPEX PHARMACEUTICALS, INC.Inventors: David C. Griffith, Michael N. Dudley, Mark W. Surber, Keith A. Bostian, Olga Rodny
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Patent number: 7674786Abstract: Compounds comprising: or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein Y is a carboxylic acid functional group, sulfonic acid functional group, or phosphonic acid functional group; or an amide or ester thereof comprising from 0 to 12 carbon atoms; or Y is a hydroxymethyl, or tetrazolyl functional group; A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o wherein Ar is substituted or unsubstituted phenyl or monocyclic heteroaryl, the sum of m and o is from 1 to 4, and wherein one CH2 may be replaced by with S or O; R, D, and n are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 2, 2006Date of Patent: March 9, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh, Robert M. Burk
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Publication number: 20100048530Abstract: The invention relates to 2-azetidinone derivatives of formula (I), including pharmaceutically acceptable salts, solvates and prodrugs thereof. The compounds inhibit cholesterol absorption and are useful in the treatment of hyperlipidaemic conditions. The invention also relates to processes for their manufacture and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 21, 2006Publication date: February 25, 2010Applicant: ASTRAZENECA ABInventors: Mikael Dahlstrom, Staffan Karlsson, Peter Nordberg, Tore Skjaret, Ingemar Starke
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Patent number: 7635693Abstract: The subject invention concerns N-thiolated ?-lactam compounds of formula A, wherein R1 is a hydrocarbon group having 1-8 carbon atoms; R3 is an organothio group; and R4 is alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, and analogs and pharmaceutically acceptable salts, esters and amides thereof. The subject invention also concerns methods for inducing tumor cell death or inhibiting tumor cell proliferation, and methods for inducing DNA damage, inhibiting DNA replication, activating p38 MAP kinase, or activating caspase cascade activation, or releasing cytochrome C from mitochondria into the cytoplasm in a tumor cell. Methods for treating cancer using N-thiolated ?-lactam compounds, as well as pharmaceutical compositions comprising the same are further disclosed.Type: GrantFiled: March 14, 2006Date of Patent: December 22, 2009Assignee: University of South FloridaInventors: Q. Ping Dou, Edward Turos, David M. Smith
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Publication number: 20090306040Abstract: The invention relates to the use of a functional muscarinic M1/M4 receptor agonist or a pharmaceutically acceptable salt thereof for the treatment of negative symptoms of schizophrenia. It also relates to adjunctive and simultaneous combination therapies for the treatment of negative symptoms of schizophrenia in which the functional muscarinic M1/M4 receptor agonist or a pharmaceutically acceptable salt thereof, in particular sabcomeline or a pharmaceutically acceptable salt thereof and at least one neuroprotective agent, neuroleptic and/or atypical antipsychotic agent are administered adjunctively or simultaneously. The invention also provides methods of treatment of the negative symptoms of schizophrenia utilising such therapies and such adjunctive or simultaneous therapeutic combination therapies, therapeutic combinations for use therein and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 23, 2007Publication date: December 10, 2009Inventors: Paul Christopher Sharpe, Peter Robin Blower, Jill Galloway Chisnall Rasmussen
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Publication number: 20090264340Abstract: The present invention provides compositions and methods for increasing absorption of antibacterial agents, particularly third generation cephalosporin antibacterial agents, in oral dosage solid and/or suspension forms. Specifically, the composition is comprised of a biopolymer that is preferably swellable and/or mucoadhesive, a antimicrobial agent, and a cationic binding agent contained within the biopolymer such that the binding agent is ionically bound or complexed to at least one member selected from the group consisting of the biopolymer and the antimicrobial agent.Type: ApplicationFiled: April 16, 2009Publication date: October 22, 2009Inventors: SEUNG-HO CHOI, JEOUNG-SOO LEE, DENNIS KEITH
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Publication number: 20090176719Abstract: Methods for treating perioral dermatitis are described herein. The method includes administering topically a composition containing an effective amount of a systemic or topical antibiotic and a corticosteroid. The concentration of the antibiotic is from about 0.01% to about 5% by weight of the composition and the concentration of the corticosteroid is from about 0.01% to about 5% by weight of the composition. The composition can contain one or more pharmaceutically acceptable excipients and/or carriers. The compositions can be formulated as a lotion, cream, gel, ointment, paste, powder, solution, suspension, spray, foam, or patch.Type: ApplicationFiled: January 7, 2009Publication date: July 9, 2009Applicant: LioLabs LLCInventor: Jay Goldstein
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Publication number: 20090124594Abstract: Provided is a method of treating the health-related quality-of-life (HRQOL) symptoms of a lung disease, comprising the administration of an inhalable aerosole of aztreonam lysine. The method is suitable for the short term and sustainable long term treatment of HRQOL symptoms.Type: ApplicationFiled: September 15, 2008Publication date: May 14, 2009Applicant: Gilead Sciences, Inc.Inventors: Alan B. Montgomery, Melissa A. Yeager
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Publication number: 20090093422Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.Type: ApplicationFiled: June 17, 2008Publication date: April 9, 2009Inventors: Roger Tung, Scott Harbeson
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Publication number: 20090069286Abstract: The present application describes deuterium-enriched aztreonam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 3, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090053149Abstract: A surfactant can be added, safely and effectively, to a drug solution containing any antimicrobial agent, such as an antibiotic like tobramycin, that is suitable for administration to the lungs via inhalation. Thus, when an aerosolized drug solution includes surfactant, Marangoni flows cause the drug particles, once deposited in the lungs, to spread over a wider surface area, thereby ensuring greater antimicrobial efficacy. A solution that contains, for example, an antibiotic and tyloxapol or another surfactant providing a similar surface tension to the composition is optimally delivered by the functional combination of a breath-actuated nebulizer and a high-flow compressor.Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Inventors: Tim Corcoran, Amy Lise Marcinkowski, Joseph Pilewski, Kristina Thomas
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Publication number: 20090042819Abstract: The invention describes novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.Type: ApplicationFiled: February 16, 2006Publication date: February 12, 2009Applicant: NitroMed, Inc.Inventors: James L. Ellis, David S. Garvey, Chia-En Lin
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Publication number: 20090018091Abstract: The invention describes compositions and kits comprising at least one nitric oxide enhancing group antimicrobial compound, or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitric oxide enhancing antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. The antimicrobial compounds of the invention are preferably tobramycin, aztreonam, ciprofloxacin and doripenam. The nitric oxide enhancing antimicrobial compounds are substituted with at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.Type: ApplicationFiled: August 2, 2006Publication date: January 15, 2009Applicant: NITROMED, INC.Inventors: James L. Ellis, David S. Garvey
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Patent number: 7439253Abstract: The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a method for preparing these compounds, and to their use as medicaments, in particular as antibacterials and ?-lactamase inhibitors.Type: GrantFiled: December 4, 2003Date of Patent: October 21, 2008Assignee: NovexelInventors: Maxime Lampilas, Branislav Musicki, Michel Klich, David Alan Rowlands
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Publication number: 20080233196Abstract: A sterile pharmaceutical composition having as its active principles piperacillin sodium and tazobactam sodium of substantially the same density, mixed with sodium bicarbonate. The mixture is soluble in water to give injectable reconstituted solutions having high stability with time.Type: ApplicationFiled: December 6, 2007Publication date: September 25, 2008Applicant: ACS DOBFAR S.p.A.Inventors: Angelo Giovanni CATTANEO, Leonardo Marsili
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Publication number: 20080167285Abstract: The invention relates to heterosubstituted N-thiolated beta-lactams, compositions comprising these compounds, methods for their production, and methods of use as antibiotics to inhibit the growth of bacteria. The antibacterial agents of the invention can be administered to a human or animal to treat or inhibit bacterial infection, such as that of Staphylococcus species, including methicillin-resistant Staphylococcus aureus (MRSA).Type: ApplicationFiled: September 7, 2007Publication date: July 10, 2008Inventors: Edward Turos, Praveen Ramaraju
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Publication number: 20080107707Abstract: The present invention provides a polymerizable antimicrobial composition and a method for using the same. The polymerizable antimicrobial composition of the invention comprises an antimicrobial compound, a linker, and a polymerizable function group.Type: ApplicationFiled: July 6, 2007Publication date: May 8, 2008Applicant: REGENTS OF THE UNIVERSITY OF COLORADOInventors: McKinley C. Lawson, Kristi S. Anseth
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Patent number: 7214364Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.Type: GrantFiled: July 3, 2003Date of Patent: May 8, 2007Assignee: Corus Pharma, Inc.Inventor: Alan Bruce Montgomery
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N-thiolated beta-lactams: novel antibacterial agents for methicillin-resistant Staphylococcus aureus
Patent number: 6946458Abstract: The invention relates generally to novel N-thiolated ?-lactams. More specially, the invention relates to the use of these novel antibacterial agents in the treatment or inhibition of methicillin-resistant Staphylococcus aureaus.Type: GrantFiled: November 5, 2002Date of Patent: September 20, 2005Assignee: University of South FloridaInventor: Edward Turos -
Patent number: 6916803Abstract: The present invention relates to novel Syn isomers of racemates and optical isomers of 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids of the following formula: and their use in treating infections caused by gram-negative pathogenic bacteria.Type: GrantFiled: September 14, 2001Date of Patent: July 12, 2005Assignee: Pantherix, Ltd.Inventors: Ronald George Micetich, Samarendra Maiti, Charles Fiakpui, George Thomas, Andhe V. Narender Reddy, Sameeh M. Salama, Rajeshwar Singh
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Patent number: 6821963Abstract: Phenylamino benzhydroxamic acid derivatives of formula (I) where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.Type: GrantFiled: June 4, 2002Date of Patent: November 23, 2004Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
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Publication number: 20040062721Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.Type: ApplicationFiled: July 3, 2003Publication date: April 1, 2004Inventor: Alan Bruce Montgomery
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N-thiolated beta-lactams: novel antibacterial agents for methicillin-resistant staphylococcus aureus
Publication number: 20030191108Abstract: The invention relates generally to novel N-thiolated &bgr;-lactams. More specially, the invention relates to the use of these novel antibacterial agents in the treatment or inhibition of methicillin-resistant Staphylococcus aureaus.Type: ApplicationFiled: November 5, 2002Publication date: October 9, 2003Inventor: Edward Turos -
Publication number: 20030133925Abstract: Methods, compounds and compositions are provided for inhibiting the growth of pathogenic microbes in vitro and of treatment of pathogenic bacterial infections in vivo using an antibacterial monobactam compound and a mucolytic agent.Type: ApplicationFiled: September 26, 2002Publication date: July 17, 2003Inventor: Ribhi M. Shawar
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Publication number: 20030055034Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam, or a pharmaceutically acceptable salt thereof, delivered as an aerosol or dry powder formulation.Type: ApplicationFiled: December 20, 2001Publication date: March 20, 2003Inventor: Alan Bruce Montgomery
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Patent number: 6476015Abstract: Substituted monocyclic &bgr;-lactam compounds that are N-1-thiolated monolactams, and which exhibit wide-ranging antibacterial activities, having a single 4-membered azetidinone ring in which: the N-1 nitrogen atom of the azetidinone ring is bonded to sulfur but is not sulfonated, of the formula: wherein R1-5 are independently hydrogen, alkyl, heteroalkyl, aryl, heteroaryl, alkenyl, or alkynyl; X is H, C, or O; and n=0-3. Chemical synthesis of these compounds by a [2+2]-imine-acid chloride cycloaddition, and methods for subsequent derivatization, are also disclosed. The compounds and compositions disclosed herein are useful as antibacterial and antibiotic agents.Type: GrantFiled: July 24, 2000Date of Patent: November 5, 2002Assignee: University of South FloridaInventors: Edward Turos, Edward T. Carpenter, Timothy Long, Daniel V. Lim, Sonja S. Dickey
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Patent number: 6335324Abstract: Compounds of the formulas: are disclosed. These compounds inhibit tryptase as well as other enzyme systems or are selective tryptase inhibitors and are useful as antiinflammatory agents particularly in the treatment of chronic asthma.Type: GrantFiled: December 13, 1999Date of Patent: January 1, 2002Assignee: Bristol-Myers Squibb Co.Inventors: Gregory S. Bisacchi, William A. Slusarchyk, Uwe Treuner, James C. Sutton, Robert Zahler, Steven Seiler, David R. Kronenthal, Michael E. Randazzo, Mark D. Schwinden, Zhongmin Xu, Zhongping Shi