6-position Substituent Contains Hetero Ring Patents (Class 514/196)
  • Publication number: 20110294774
    Abstract: The present invention provides a pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, an antibacterially effective combination of a ?-lactam antibiotic and an inhibitor of any bacterial peptidoglycan biosynthesis enzyme, especially GlmU, GlmU, MurA, MurB, MurC, MurD, MurE, MurF, MurG, MraY, and UppS.
    Type: Application
    Filed: May 6, 2011
    Publication date: December 1, 2011
    Applicant: TRIUS THERAPEUTICS
    Inventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
  • Publication number: 20110275558
    Abstract: The present invention relates to the field of medical treatments for diseases and disorders. More specifically, the present invention relates to the use of the lanthionine synthetase component C-like (LANCL) proteins as therapeutic targets for novel classes of anti-inflammatory, immune regulatory and antidiabetic drugs.
    Type: Application
    Filed: May 4, 2011
    Publication date: November 10, 2011
    Applicant: Virginia Tech Intellectual Properties, Inc.
    Inventors: Josep BASSAGANYA-RIERA, Pinyi LU, Raquel HONTECILLAS
  • Patent number: 8008287
    Abstract: Tricyclic compounds, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: August 30, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhenhong R. Cai, Salman Y. Jabri, Haolun Jin, Rachael A. Lansdown, Samuel E. Metobo, Michael R. Mish, Richard M. Pastor
  • Publication number: 20110166091
    Abstract: An aminocarboxylic acid chelating agent, preferably EDTA, or a salt thereof has been found to be useful for inhibiting particulate formation in piperacillin/tazobactam parenteral combinations. The composition may also contain a buffer, preferably citrate, and optionally an aminoglycoside. The product may be in the form of a frozen composition that can be thawed for use. The product may also be in the form of a cryodesiccated powder that can be reconstituted by addition of an aqueous vehicle to reform a solution.
    Type: Application
    Filed: February 24, 2011
    Publication date: July 7, 2011
    Inventors: Jonathan Marc Cohen, Syed Muzafar Shah, Christian Luther Ofslager, Mahdi Bakir Fawzi
  • Publication number: 20110160156
    Abstract: The present invention relates to a pharmaceutical composition and its preparation method for the eradication of Helicobacter pylorif in the forms of effervescent tablet, suspension or powder. The pharmaceutical composition comprises an effective dose of ?-lactam antibiotic, an effective dose of macrolide antibiotic, an effective dose of antacid such as proton pump inhibitor and H2 blocker, and a pharmaceutical acceptable carrier. An effective dose of alkaline substance such as carbonate or bicarbonate can be added to increase the pH of the stomach when the PPI antacid is used, which can protect the degradation of acid-labile antibiotics or PPI to further increase the bioavailability of the pharmaceutical composition for the purpose of Helicobacter pylori eradication.
    Type: Application
    Filed: June 16, 2010
    Publication date: June 30, 2011
    Applicants: SYNMOSA BIOPHARMA CORPORATION
    Inventors: Chih-Hui Lin, Jui-Ming Chou, Li-Heng Pao, Chia-Wen Chang, Chia-Yi Lin, An-Long Lee
  • Publication number: 20110152231
    Abstract: Embodiments of the invention relate generally to the use of compositions comprising methylsulfonylmethane (MSM), and one or more therapeutic agents, for the treatment of drug-sensitive and drug resistant microorganisms. In several embodiments, such compositions are effective in treating drug resistant infectious diseases, for example, MRSA.
    Type: Application
    Filed: October 29, 2010
    Publication date: June 23, 2011
    Inventors: Rodney Benjamin, Anthony L. Keller, Jeffrey Varelman
  • Patent number: 7964589
    Abstract: Mixtures of at least two active principles, of which at least one is the sodium salt, are precipitated from an organic solution containing the same active principles in salified or non-salified acid form.
    Type: Grant
    Filed: July 27, 2006
    Date of Patent: June 21, 2011
    Assignee: ACS Dobfar S.p.A.
    Inventors: Maurizio Zenoni, Angelo Giovanni Cattaneo, Leonardo Marsili
  • Publication number: 20110086831
    Abstract: The present invention relates to an in vitro method for the diagnosis and treatment guidance of a bacterial infection in patients suffering from an acute ischemic or hemorrhagic stroke, comprising the determination of the level of Procalcitonin (PCT) or a fragment thereof having at least 12 amino acid residues in a sample of a bodily fluid from said patient and the correlation of the determined level to the diagnosis of a bacterial infection in said patient.
    Type: Application
    Filed: October 12, 2010
    Publication date: April 14, 2011
    Applicant: B.R.A.H.M.S Gmbh
    Inventors: Andreas Bergmann, Oliver Hartmann, Frauke Hein, Beat Müller
  • Publication number: 20110053890
    Abstract: Bacterial quorum-sensing molecule analogs having the following structures: and methods of reducing bacterial pathogenicity, comprising providing a biological system comprising pathogenic bacteria which produce natural quorum-sensing molecule; providing a synthetic bacterial quorum-sensing molecule having the above structures and introducing the synthetic quorum-sensing molecule into the biological system comprising pathogenic bacteria. Further is provided a method of targeted delivery of an antibiotic, comprising providing a synthetic quorum-sensing molecule; chemically linking the synthetic quorum-sensing molecule to an antibiotic to produce a quorum-sensing molecule-antibiotic conjugate; and introducing the conjugate into a biological system comprising pathogenic bacteria susceptible to the antibiotic.
    Type: Application
    Filed: September 1, 2009
    Publication date: March 3, 2011
    Applicant: Los Alamos National Security, LLC.
    Inventors: Rashi Iyer, Kumkum Ganguly, Louis A. Silks
  • Publication number: 20110046101
    Abstract: The present invention relates to broad spectrum ?-lactamase inhibitors. More particularly, the invention relates to inhibitors of Class B metallo (MBL) and Class D (OXA) ?-lactamases. A method of treating a bacterial infection is provided, wherein the method comprises administering to a mammalian patient in need of such treatment a compound of formula (I) wherein R1 is selected from R2 is selected from with certain provisos as herein defined; in combination with a pharmaceutically acceptable ?-lactam antibiotic in an amount which is effective for treating the bacterial infection.
    Type: Application
    Filed: March 17, 2008
    Publication date: February 24, 2011
    Inventors: Gary I. Dmitrienko, Jarrod W. Johnson, Timothy R. Ramadhar, Thammaiah Viswanatha, Sundaramma Viswanatha
  • Publication number: 20100303799
    Abstract: Techniques are disclosed for prevention or treatment of physiological shock by administering a specific therapeutic agent, which is able to use smaller volumes of reagent to achieve complete inhibition, than other previously described techniques.
    Type: Application
    Filed: October 6, 2008
    Publication date: December 2, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Geert W. Schmid-Schönbein, Frank A. DeLano
  • Publication number: 20100285012
    Abstract: The subject application provides small compounds that are able to suppress autophagy in various cells. These compounds are useful in augmenting the existing treatments of various cancers and microbial/parasitic infections. Thus, the subject application also provides methods of treating various types of cancers and microbial/parasitic infections. Also provided by the subject application are methods of suppressing the expansion of autophagosomes within cells or individuals and inhibiting the lipidation of autophagy-related protein 8 (Atg8).
    Type: Application
    Filed: January 5, 2009
    Publication date: November 11, 2010
    Applicant: University of FLorida Research Foundation Inc.
    Inventors: William A. Dunn, JR., Debra E. Akin, Ann Progulske-Fox, David A. Ostrov
  • Publication number: 20100239666
    Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.
    Type: Application
    Filed: June 3, 2010
    Publication date: September 23, 2010
    Inventors: Hans-Ulrich Petereit, Thomas Beckert, Manfred Assmus, Wemer Hoess, Wolfgang Fuchs, Hartmut Schikowsky
  • Publication number: 20100240602
    Abstract: The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent such as ibuprofen, clofibrate or clofibric acid that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels and thus improve the effectiveness of treatment regimens involving these drugs. Further agents such as methotrexate and AZT can also be used in cancer and HIV-positive patients employing camptothecin drugs.
    Type: Application
    Filed: April 6, 2010
    Publication date: September 23, 2010
    Inventors: Thomas G. Burke, Daniel C. Carter
  • Patent number: 7723389
    Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.
    Type: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Publication number: 20100105649
    Abstract: The present invention relates to a veterinary composition for the prophylaxis and treatment of mastitis in mammals, preferably cows. The formulations of the present invention comprise two parts that are optionally administered to the animal as a blended formulation or two separate formulations. The first part is a seal formulation comprising a gel base and a non-toxic heavy metal salt in the base. The second part of the formulation is an oil-based product preferably containing an antibiotic in an oil-based formulation. The oil-based formulation may also optionally contain any other pharmaceutically active agent for the treatment or prophylaxis of disease in cattle.
    Type: Application
    Filed: January 4, 2010
    Publication date: April 29, 2010
    Applicant: PFIZER INC.
    Inventor: Roderick John Jeremiah Dorgan
  • Publication number: 20100057047
    Abstract: A nasal delivery device for and method of delivering substance to the middle meatus in a nasal cavity of a subject in the treatment of a condition, in particular an inflammatory or infectious condition, thereof, the delivery device comprising: a nosepiece unit (17) including a nosepiece (20) for fitting to a nostril of a subject and a nozzle (25) through which substance is in use delivered to the respective nasal cavity; and a delivery unit (29) for delivering substance through the nozzle of the nosepiece; wherein the delivery device is configured to provide for deposition of a significant fraction of the delivered dose on, around and in the vicinity of the middle meatus.
    Type: Application
    Filed: February 14, 2007
    Publication date: March 4, 2010
    Applicant: OptiNose AS
    Inventors: Per Gisle Djupesland, Colin David Sheldrake, Roderick Peter Hafner
  • Publication number: 20100040685
    Abstract: Disclosed herein are a collagen-based matrix for use as a restorative material and a method for the preparation thereof. An atelocollagen dispersion is spread at a predetermined thickness over a plate and freeze-dried to form a porous collagen membrane. An atelocollagen dispersion is separately spread over a plate and pressurized to form a dense collagen membrane. This is overlaid with the porous collagen membrane and immersed in an EDS solution in ethanol to crosslink the two membranes with each other. From the bilayer structure thus constructed, EDS is removed, followed by lyophilization and cutting into an appropriate size.
    Type: Application
    Filed: April 15, 2009
    Publication date: February 18, 2010
    Applicant: DALIM TISSEN Inc.
    Inventors: Seong-Ki LEE, Si-Nae Park, Sang-Hee Bae
  • Publication number: 20100029604
    Abstract: The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum ?-lactamase inhibitor.
    Type: Application
    Filed: February 13, 2008
    Publication date: February 4, 2010
    Inventors: Andrej Prezelj, Uros Urleb, Tomaz Solmajer
  • Publication number: 20090264340
    Abstract: 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: Application
    Filed: April 16, 2009
    Publication date: October 22, 2009
    Inventors: SEUNG-HO CHOI, JEOUNG-SOO LEE, DENNIS KEITH
  • Publication number: 20090263495
    Abstract: Particular aspects provide compositions and methods for treating or preventing bacterial infection or at least one symptom related to bacterial infection, and the like in a subject in need thereof by administering a therapeutic composition comprising at least one electrokinetically generated fluid (including gas-enriched electrokinetically generated fluids) as disclosed herein, the electrokinetically altered aqueous fluid suitable to alter cellular membrane structure or function sufficient to provide for modulation of intracellular signal transduction, wherein treating bacterial infection or at least one symptom related to bacterial infection is thereby afforded. In particular embodiments, the fluids are gas-enriched fluids or therapeutic compositions and methods, and include oxygen-enriched water optionally in combination with other therapeutic agents. Other embodiments include particular routes of administration or formulations for the gas-enriched therapeutic compositions.
    Type: Application
    Filed: October 23, 2008
    Publication date: October 22, 2009
    Applicant: REVALESIO CORPORATION
    Inventors: Richard L. Watson, Anthony B. Wood, Gregory J. Archambeau
  • Publication number: 20090247498
    Abstract: Compositions having an effective amount of an antibacterial agent may be useful in the treatment of amyotrophic lateral sclerosis (ALS) and other diseases of the nervous system. The compositions may include an extraordinary amount of an antibacterial agent. Ceftriaxone has stopped the progression of ALS for a second time after nearly 18 years of the disease.
    Type: Application
    Filed: June 10, 2009
    Publication date: October 1, 2009
    Inventor: Milankovits Marton
  • Publication number: 20090176720
    Abstract: An aminocarboxylic acid chelating agent, preferably EDTA, or a salt thereof has been found to be useful for inhibiting particulate formation in piperacillin/tazobactam parenteral combinations. The composition may also contain a buffer, preferably citrate, and optionally an aminoglycoside. The product may be in the form of a frozen composition that can be thawed for use. The product may also be in the form of a cryodesiccated powder that can be reconstituted by addition of an aqueous vehicle to reform a solution.
    Type: Application
    Filed: February 13, 2009
    Publication date: July 9, 2009
    Applicant: Wyeth Holdings Corporation
    Inventors: Jonathan Marc Cohen, Syed Muzafar Shah, Christian Luther Ofslager, Mahdi Bakir Fawzi
  • Publication number: 20090155387
    Abstract: A pharmaceutical composition comprising: at least one ?-lactam antibiotic and at least one ion-chelating agent; wherein when said pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic.
    Type: Application
    Filed: February 24, 2009
    Publication date: June 18, 2009
    Inventor: Hesheng ZHANG
  • Publication number: 20090156518
    Abstract: A pharmaceutical composition, comprising: at least one ?-lactam antibiotic and at least one buffer component; wherein when the pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic mixed with the ?-lactam antibiotic and the buffer component.
    Type: Application
    Filed: February 24, 2009
    Publication date: June 18, 2009
    Inventor: Hesheng ZHANG
  • Publication number: 20090123537
    Abstract: The present invention contemplates a novel oral dosage form for the intestinal delivery of ceftriaxone sodium. The oral dosage form inhibits enteric degradation of the therapeutic compound by encapsulation within an inner core region and having an outer shell, preventing its dissolution until reaching the small intestine. Furthermore, the enzymatic degradation of the compound is substantially inhibited until absorption at the intestinal mucosa.
    Type: Application
    Filed: November 12, 2007
    Publication date: May 14, 2009
    Inventor: Daniel R. DeBrouse
  • Publication number: 20090111788
    Abstract: Novel modified release pharmaceutical compositions wherein the composition comprises at least one antibiotic(s) preferably amoxicillin or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof either alone or in combination with other antibiotic(s) as active ingredient, with at least one release modifying agent(s) for controlling the release of the beta lactam antibiotic optionally with one or more other pharmaceutically acceptable excipient(s) is provided, wherein the dosage form provides a release of not more than about 60% of the antibiotic in about 30 minutes and not less than about 70% of the antibiotic after 8 hours when subjected to in vitro dissolution study or when tested in vivo. Further, the compositions of the present invention which when tested in a group of healthy humans provide a mean peak plasma concentration (Cmax) after at least about 0.5 hour of administration of the dosage form.
    Type: Application
    Filed: March 7, 2007
    Publication date: April 30, 2009
    Inventors: Rajesh Jain, Kour Chand Jindal, Munish Talwar
  • Publication number: 20090093422
    Abstract: 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: Application
    Filed: June 17, 2008
    Publication date: April 9, 2009
    Inventors: Roger Tung, Scott Harbeson
  • Publication number: 20080213366
    Abstract: The present invention provides oral formulations of poorly bioavailable and/or poorly absorbable, and/or poorly water soluble therapeutic agents. The invention features pharmaceutical composition including a biopolymer, a therapeutic agent, for example an antimicrobial agent such as ceftriaxone, and an absorption enhancer, for example a polyoxyethylene alkyl ether absorption enhancer. Methods of making and using the pharmaceutical compositions is also described.
    Type: Application
    Filed: April 27, 2006
    Publication date: September 4, 2008
    Applicant: Cubist Pharmaceuticals, Inc
    Inventors: Walter G. Gowan Jr, Dennis D. Keith, Sandra O'Connor
  • Patent number: 7094431
    Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Publication number: 20030236243
    Abstract: 6(7)-&bgr;-substituted &bgr;-lactam compounds as inhibitors of &bgr;-lactamase activity.
    Type: Application
    Filed: May 14, 2003
    Publication date: December 25, 2003
    Inventors: Brian K. Shoichet, Larry C. Blaszczak
  • Publication number: 20030216372
    Abstract: Compounds of formula (I): 1
    Type: Application
    Filed: April 4, 2003
    Publication date: November 20, 2003
    Applicant: AlamX L.L.C.
    Inventors: John D. Buynak, Hansong Chen
  • Publication number: 20020198180
    Abstract: Compounds of formula I: 1
    Type: Application
    Filed: June 5, 2002
    Publication date: December 26, 2002
    Applicant: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 6436398
    Abstract: Compound of formula I: wherein R1, R2, R3, R4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: November 29, 2000
    Date of Patent: August 20, 2002
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 6319904
    Abstract: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.
    Type: Grant
    Filed: July 7, 1999
    Date of Patent: November 20, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yohko Akiyama, Masafumi Nakao, Naoki Nagahara, Susumu Iwasa
  • Patent number: 6232305
    Abstract: The present invention provides substituted amino bicyclic-&bgr;-lactam penam derivatives and substituted amino bicyclic-&bgr;-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis.
    Type: Grant
    Filed: January 22, 1998
    Date of Patent: May 15, 2001
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Rajeshwar Singh, Nian Zhou, Deqi Guo, Ronald G. Micetich
  • Patent number: 6156745
    Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting .beta.-lactamase enzymes, for enhancing the activity of .beta.-lactam antibiotics, and for treating .beta.-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: December 5, 2000
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 5994340
    Abstract: New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial .beta.-lactamases. These compounds can be used in combination with .beta.-lactam antibiotics to increase the effectiveness of the .beta.-lactam antibiotics in fighting infection caused by .beta.-lactamase producing bacteria.
    Type: Grant
    Filed: August 29, 1997
    Date of Patent: November 30, 1999
    Assignee: SynPhar Laboratories, Inc.
    Inventors: Samarendra N. Maiti, Oludotun A. Phillips, Eduardo L. Setti, Andhe V. Narender Reddy, Ronald G. Micetich, Fusahiro Higashitani, Chieko Kunugita, Koichi Nishida, Tatsuya Uji
  • Patent number: 5840735
    Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
    Type: Grant
    Filed: August 3, 1994
    Date of Patent: November 24, 1998
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5686465
    Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 11, 1997
    Assignee: Endorecherche Inc.
    Inventors: Fernand Labrie, Yves Merand
  • Patent number: 5681563
    Abstract: Cephalosporins with an exocyclic allene in the 7-position and their pharmaceutically active salts are potent inhibitors of .beta.-lactamases and are therefore useful in the treatment of penicillin resistant infections.
    Type: Grant
    Filed: June 17, 1996
    Date of Patent: October 28, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Patent number: 5180719
    Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: January 19, 1993
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Ronald E. White, Thomas P. Demuth, Jr.
  • Patent number: 5126335
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof: ##STR1## wherein X is hydrogen or a group NHR.sup.1, wherein R.sup.1 is hydrogen or an amino protecting group, and R is an optionally substituted 5-membered or 6-membered saturated heterocyclic group containing 1 or 2 heteroatoms selected from oxygen, sulphur or nitrogen, are useful in the treatment of bacterial infections in humans and animals.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: June 30, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Roger J. Ponsford, Andrew V. Stachulski
  • Patent number: 5114929
    Abstract: An unpressurized container containing a palatable pharmaceutical formulation comprising a homogeneous, non-aqueous suspension of an orally active medicament, an edible oily vehicle, an edible emulsifier and a finely particulate sugar having no oily after taste.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: May 19, 1992
    Assignee: Beecham Group p.l.c.
    Inventor: Robert R. Vartan
  • Patent number: 5069899
    Abstract: Anti-thrombobenic, anti-microbial compositions containing heparin reacted with quaternary ammonium components and bound with water-insoluble polymers are disclosed. Such compositions may also contain additional quaternary ammonium compounds not reacted with heparin and may also contain quaternary ammonium compound(s) reacted with antibiotics.
    Type: Grant
    Filed: November 2, 1989
    Date of Patent: December 3, 1991
    Assignee: Sterilization Technical Services, Inc.
    Inventors: Richard J. Whitbourne, Margaret A. Mangan
  • Patent number: 4954489
    Abstract: Compounds of formula (I) and their salts and esters: ##STR1## wherein X is hydrogen or a group NHR.sup.1, wherein R.sup.1 is hydrogen or an amino protecting group, and R is optionally substituted C.sub.5-8 cycloalkyl or cycloalkenyl, are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: April 5, 1989
    Date of Patent: September 4, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Roger J. Ponsford, Andrew V. Stachulski
  • Patent number: 4918067
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is a 5 or 6 membered sulphur and/or nitrogen containing heterocyclic group substituted by an optionally protected amino group, with the proviso that R.sup.1 is not 2-aminothiazol-4-yl, and R is hydrogen; optionally substituted C.sub.1-12 alkyl; optionally substituted C.sub.2-12 alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl.These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organizations.
    Type: Grant
    Filed: July 22, 1987
    Date of Patent: April 17, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Brian C. Gasson, Michael J. Pearson
  • Patent number: 4898731
    Abstract: An antibacterial synergistic composition consisting essentially of a mixture of a penicillin or cephalosporin derivative of the formula ##STR1## and a penicillin of the formula ##STR2## preferably in association with a pharmaceutical carrier.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: February 6, 1990
    Assignees: Astra Lakemedel Aktiebolag, Astra Pharmaceutical Products, Inc.
    Inventors: Peter Bamberg, Bertil A. Ekstrom, Ulf E. Forsgren, Berndt O. H. Sjoberg
  • Patent number: 4861768
    Abstract: Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.
    Type: Grant
    Filed: February 18, 1987
    Date of Patent: August 29, 1989
    Assignee: Taiho Pharmaceutical Company, Limited
    Inventors: Sigeru Torii, Hideo Tanaka, Motoaki Tanaka, Shozo Yamada, Akira Nakai, Hisashi Ohbayashi
  • Patent number: RE33948
    Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing ##STR3## Z representing O, S, or NR.sup.10, and R.sup.2 represents hydrogen or a protective group.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: June 2, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger