Alkyl, Hydroxyalkyl, Alkoxyalkyl Or Alkanoyloxyakyl Bonded Directly To 3-position Patents (Class 514/207)
  • Publication number: 20150140111
    Abstract: The invention relates to effervescent pharmaceutical dosage forms including cefdinir as the active agent, and their preparation. The invention also relates to effervescent formulations including ceftibuten and/or its pharmaceutically acceptable salts, hydrates, solvates, esters, amorphous and crystal forms and/or a combination thereof. The invention also relates to pharmaceutical compositions including (Z)-3-Carboxymethyl-7-(2-(2-furyl)-2-methoxyiminoacetylamino)-3-sefem-4-carboxylic acid which is named cefuroxime axetil or any pharmaceutically acceptable derivative thereof, and the use of these compositions in the treatment of bacterial infections. Lastly, the invention relates to pharmaceutical formulations including a third generation cephalosporin together with clavulanic acid and/or derivatives thereof as the active agents.
    Type: Application
    Filed: June 19, 2014
    Publication date: May 21, 2015
    Inventor: Mahmut BILGIC
  • Publication number: 20150094293
    Abstract: Novel solid forms of ceftolozane are described, as well as methods for the preparation and use of these solid forms.
    Type: Application
    Filed: May 28, 2014
    Publication date: April 2, 2015
    Applicant: CALIXA THERAPEUTICS, INC.
    Inventors: Valdas Jurkauskas, Nicole Miller Damour, Lisa Duong, You Seok Hwang, Kristos Adrian Moshos, Sanjay Mudur, Asli Ovat, Joseph Terracciano, Jason Woertink
  • Publication number: 20150045337
    Abstract: The present invention relates to a composition, the composition including a therapeutically effective amount of at least one active agent, and a base including, an amount of colloidal silica; at least one oil; and at least one surfactant, wherein the viscosity of the composition is below 1000 mPas at a shear rate of 100 l/s and at a temperature of 20° C.
    Type: Application
    Filed: February 27, 2013
    Publication date: February 12, 2015
    Inventors: Fadil Al Alawi, Olaf Bork, Ian George Tucker
  • Publication number: 20140275001
    Abstract: This disclosure provides compositions containing solid forms of sodium (2S,5R)-2-(1,3,4-oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate, and methods of manufacturing and using these compositions.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: You Seok Hwang, Jian-Qiao Gu, Akash Jain, Sudhakar Garad, Jacob P. Sizemore
  • Publication number: 20140274991
    Abstract: Pharmaceutical compositions can include ceftolozane and an amount of sodium chloride effective to provide improved ceftolozane stability.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Nicole Miller Damour, Joseph Terracciano
  • Publication number: 20140274925
    Abstract: Disclosed herein are compositions and methods for diagnosing, treating, and monitoring Lyme disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chenggang Jin, Gottfried H. Kellermann
  • Patent number: 8722656
    Abstract: The present invention provides novel cephalosporin derivatives of formula I, their analogues, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: May 13, 2014
    Assignee: Zoetis LLC
    Inventors: Brian A. Duclos, Edmund L. Ellsworth, Richard A. Ewin, Paul D. Johnson, Timothy A. Johnson, Graham M. Kyne, Susan M. K. Sheehan, Rajendran Vairagoundar
  • Publication number: 20140088069
    Abstract: An antibacterial composition is provided including a combination of a ?-lactam antibiotic that has a binding affinity for bacterial penicillin-binding protein 2; and a non-antibiotic compound which may be a thienopyridine or a non-thienopyridine compound. A method of treatment using the composition is also provided.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Inventors: Eric D. Brown, Maya Farha, Alexander Leung, Gerry Wright, Kalinka Koteva, Ted Sewell, Linda Ejim
  • Publication number: 20130345190
    Abstract: ?-Lactamase inhibitor compounds (BLIs) are disclosed, including compounds that have activity against class A, class C or class D ?-lactamases. Methods of manufacturing the BLIs, and uses of the compounds in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: March 29, 2013
    Publication date: December 26, 2013
    Inventor: Cubist Pharmaceuticals, Inc.
  • Patent number: 8575144
    Abstract: Inhibitors of the enzyme beta-lactamase are provided comprising compounds of formula (II) wherein R1 or R2 is a pyridyl group and R5 is a group of formula The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: November 5, 2013
    Assignee: Southern Methodist University
    Inventors: John D. Buynak, Anjaneyulu Sheri, Sundar Ram Reddy Pagadala
  • Publication number: 20130203726
    Abstract: The present invention relates to the use of inhibitors of FtsZ, an ancestral tubulin of prokaryotes, to restore susceptibility to ?-lactam antibiotics, including carbapenems and cephalosporins, particularly in methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphyloccus epidermis (MRSE), and other coagulase negative staphylococci (MRCNS).
    Type: Application
    Filed: March 4, 2011
    Publication date: August 8, 2013
    Inventors: Terry Roemer, Sang Ho Lee, Lisa Wang Jarantow
  • Publication number: 20130150311
    Abstract: In one aspect, the present invention is directed to a dry, flowable and compressible composition, useful as a pharmaceutical excipient, which composition comprises a mixture of hydrophobic and hydrophilic poly(ethylene oxide)-polypropylene oxide)-poly(ethylene oxide) block copolymers, and which possesses a Carr index of less than about 20. In other aspects, the present invention is directed a pharmaceutical composition comprising such adjuvant and a pharmaceutically active ingredient; as well as to a method of making the compositions.
    Type: Application
    Filed: December 13, 2011
    Publication date: June 13, 2013
    Inventors: Grzegorz Pietrzynski, Valery Alakhov, Kishore Patel
  • Publication number: 20130129791
    Abstract: The invention relates to effervescent pharmaceutical dosage forms including cefdinir as the active agent, and their preparation. The invention also relates to effervescent formulations including ceftibuten and/or its pharmaceutically acceptable salts, hydrates, solvates, esters, amorphous and crystal forms and/or a combination thereof. The invention also relates to pharmaceutical compositions including (Z)-3-Carboxymethyl-7-(2-(2-furyl)-2-methoxyiminoacetylamino)-3-sefem-4-carboxylic acid which is named cefuroxime axetil or any pharmaceutically acceptable derivative thereof, and the use of these compositions in the treatment of bacterial infections. Lastly, the invention relates to pharmaceutical formulations including a third generation cephalosporin together with clavulanic acid and/or derivatives thereof as the active agents.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 23, 2013
    Inventor: Mahmut Bilgic
  • Publication number: 20130064772
    Abstract: Provided are wound caring compositions and devices containing a pH-sensitive, preferably acid degradable, components contained in a water-permeable and hydronium ion permeable material. The pH-sensitive component encloses an antibiotic which is released to the wound upon infection by a microorganism at the wound site, and/or encloses a pH indicator. The antibiotic release is triggered by the microorganism's production of CO2 at the wound site which forms carbonic acid, lowers the pH at the pH sensitive components, and thus results in rupture of the liposome.
    Type: Application
    Filed: September 7, 2012
    Publication date: March 14, 2013
    Inventors: Gerald F. Swiss, Stefan Schwabe, Robert M. Moriarty
  • Publication number: 20130053336
    Abstract: The invention relates to a method for treating infections of bacteria of the Chlamydiaceae family using a ?-lactam. The invention also relates to a method for treating diseases caused by an infection of bacteria of the Chlamydiaceae family using a ?-lactam.
    Type: Application
    Filed: January 13, 2011
    Publication date: February 28, 2013
    Inventors: Philippe Verbeke, Maud Dumoux, Colette Kanellopoulos
  • Publication number: 20130018029
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: July 16, 2012
    Publication date: January 17, 2013
    Inventor: Chongxi YU
  • Publication number: 20120329770
    Abstract: The present invention relates to cephalosporin derivatives having ?-lactamase inhibitory activity. The compounds are useful in preventing or treating bacterial resistance to an antibiotic, e.g. a ?-lactam antibiotic. Disclosed herein are compounds that are inhibitors of class B metallo-?-lactamases, as well as class A, C, and D serine ?-lactamases. In some preferred embodiments, the compounds are 3?-thiobenzoate derivatives of a cephalosporin. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the compounds are also disclosed.
    Type: Application
    Filed: February 25, 2011
    Publication date: December 27, 2012
    Inventors: Gary Igor Dmitrienko, Ahmad Ghavami, Valerie Joy Goodfellow, Jarrod W. Johnson, Anthony Paul Krismanich, Laura Marrone, Thammaiah Viswanatha, Sundaramma Viswanatha
  • Publication number: 20120172292
    Abstract: This invention discloses a method for enhancing the efficacy of antimicrobial, anti-protozoa and anti-cancer treatments by co-administering an inhibitor of endogenous NO production and/or NO scavenger.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 5, 2012
    Applicant: NEW YORK UNIVERSITY
    Inventors: Evgeny A. Nudler, Ivan Gusarov
  • Publication number: 20120141574
    Abstract: A palatable, edible soft chewable medication vehicle for delivery of a pharmaceutically acceptable active ingredient, such as a drug, to an animal or human subject. The edible soft chews contain only food grade or better inactive ingredients, and preferably do not contain ingredients of animal origin. Processes for manufacturing the edible soft chews do not require the use of heat or the addition of water during mixing of active and inactive ingredients, provide stable concentrations of the active ingredient, and produce chews of consistent weight and texture.
    Type: Application
    Filed: February 14, 2012
    Publication date: June 7, 2012
    Inventors: Neil E. Paulsen, Roland Johnson, Michael Coffee
  • Patent number: 8168622
    Abstract: ?-lactamase resistant cephalosporin ester compound chosen from those represented by formula (I): wherein, and pharmaceutical salts thereof, composition thereof, and use thereof are disclosed.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: May 1, 2012
    Assignee: Zhejiang Yongning Pharmaceutical Co., Ltd.
    Inventors: Fengqi Ye, Shanzong Fang, Xiuwei Lu
  • Publication number: 20120039969
    Abstract: A novel dosage form. The dosage form is presented in particulate form and before oral ingestion the particulate material is subjected to an aqueous medium, whereby it is converted to a semi-solid form by swelling or gelling of one or more of the components, especially of a gellan gum, of the particulate matter. The invention also relates to a vehicle for oral administration of one or more active substances, the vehicle comprising a gellan gum arranged in a configuration allowing optimal water diffusion so that upon addition of a predetermined amount of an aqueous medium, without the necessity of applying shear forces or other mixing forces, within a time period of 5 minutes or less swells and/or gels and the texture of the swelled vehicle being similar to that of a soft pudding and having a viscosity of at least about 10,000 cps as measured by a Brookfield Viscometer with a #4 LV spindle at 6 rpm and at 20-25° C.
    Type: Application
    Filed: August 18, 2011
    Publication date: February 16, 2012
    Inventors: Daniel Bar-Shalom, Lillian Slot, Gina Fischer, Pernille Hoyrup Hemmingsen
  • Publication number: 20120022031
    Abstract: A diluted solution of ceftiofur sodium is intrathecally or ventricularly delivered to effectively treat bacterial meningitis while maintaining the patient's threshold and reducing the likelihood of seizure.
    Type: Application
    Filed: May 9, 2008
    Publication date: January 26, 2012
    Applicant: NBR PATHFINDER LLC
    Inventor: Robert B. Boyd
  • Publication number: 20110301127
    Abstract: The instant methods and compositions represent an advance in controlling drug resistance in microbes. AcrAB-like efflux pumps have been found to control resistance to drugs, even in highly resistant microbes. Accordingly, methods of treating infection, methods of screening for inhibitors of AcrAB-like efflux pumps, and methods of enhancing antimicrobial activity of drugs are provided. Pharmaceutical composition comprising an inhibitor of an AcrAB-like efflux pump and an antimicrobial agent are also provided.
    Type: Application
    Filed: August 16, 2011
    Publication date: December 8, 2011
    Applicant: TRUSTEES OF TUFTS COLLEGE
    Inventors: Margret OETHINGER, Stuart B. LEVY
  • Publication number: 20110301139
    Abstract: A pharmaceutical suspension dosage form comprising greater than 80 mg/ml and not more than 150 mg/ml of Cefixime and pharmaceutically acceptable excipients.
    Type: Application
    Filed: June 8, 2011
    Publication date: December 8, 2011
    Applicant: Lupin Limited
    Inventors: Shrenik Annasaheb KOLE, Bharat Raghunath Metkar, Makarand Krishnakumar Avachat
  • 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: 20110223234
    Abstract: A palatable, edible soft chewable medication vehicle for delivery of a pharmaceutically acceptable active ingredient, such as a drug, to an animal or human subject. The edible soft chews contain only food grade or better inactive ingredients, and preferably do not contain ingredients of animal origin. Processes for manufacturing the edible soft chews do not require the use of heat or the addition of water during mixing of active and inactive ingredients, provide stable concentrations of the active ingredient, and produce chews of consistent weight and texture.
    Type: Application
    Filed: May 25, 2011
    Publication date: September 15, 2011
    Inventors: Neil E. Paulsen, Roland Johnson, Michael Coffee
  • Patent number: 7994329
    Abstract: Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: August 9, 2011
    Assignee: Helsinn Therapeutics (U.S.), Inc.
    Inventor: Michael Ankerson
  • Publication number: 20110172200
    Abstract: The present invention relates to a pharmaceutical composition with broad-spectrum of activity against class A, class C and D enzymes comprising an antibiotic and a pharmaceutically effective amount of a compound of Formula (I), compounds of Formula (I), the use of a therapeutically effective amount of one or more compounds of Formula (I) as a broad-spectrum beta-lactamase inhibitor and the use of such a pharmaceutical composition for the treatment of an infection in humans or animals caused by bacteria.
    Type: Application
    Filed: January 28, 2009
    Publication date: July 14, 2011
    Applicant: LEK PHARMACEUTICALS D. D.
    Inventors: Andrej Prezelj, Uros Urleb, Gregr Vilfan
  • 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: 20110046103
    Abstract: The treatment of neurological disorders using cefazolin compositions and pharmaceutical compositions including oral dosage forms that include cefazolin compositions are described.
    Type: Application
    Filed: November 3, 2010
    Publication date: February 24, 2011
    Applicant: Revaax Pharmaceuticals, LLC
    Inventors: Gary A. Koppel, Michael O. Chaney
  • 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: 20100272808
    Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also motes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to size that is retained in the stomach during the postprandial or fed mode.
    Type: Application
    Filed: April 29, 2010
    Publication date: October 28, 2010
    Inventors: Bret Berner, Jenny Louie-Helm, Gloria Gusler, John N. Shell
  • Publication number: 20100222410
    Abstract: The present invention generally relates to various nucleases and uses thereof, and in some cases, to the UPF0054 protein superfamily. Members of the UPF0054 protein superfamily, such as the E. coli protein YbeY, may possess RNase activity and may be involved in certain important cellular processes. Disruption of YbeY activity can lead to increased sensitivity to antibiotics. Accordingly, certain embodiments of the invention are directed to systems and methods for screening target compounds for activity against UPF0054 superfamily proteins. In some embodiments, the screening method allows to target compositions to be determined that show selective activity against UPF0054 superfamily proteins. Other embodiments of the invention provide for nucleases capable of site-specific cleavage of nucleic acids.
    Type: Application
    Filed: July 17, 2009
    Publication date: September 2, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Bryan W. Davies, Caroline Koehrer, Asha I. Jacob, Uttam L. RajBhandary, Graham C. Walker, Brenda Kathleen Minesinger, Shree Prakash Pandey
  • Publication number: 20100143295
    Abstract: The present invention relates to new quinazoline inhibitors of EGFR tyrosine kinase, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 4, 2009
    Publication date: June 10, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • 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
  • Patent number: 7687519
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: March 30, 2010
    Assignee: Theravance, Inc.
    Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
  • Publication number: 20090269400
    Abstract: The present invention is directed to compositions comprising a nanoparticulate antibiotic having improved bioavailability. Preferably, the antibiotic comprises nanoparticulate cephalosporin particles with an effective average particle size of less than about 2000 nm and are useful in the treatment of bacterial infection. The invention also relates to a controlled release composition comprising a cephalosporin or a nanoparticulate cephalosporin that in operation delivers the drug in a pulsed or bimodal manner for the treatment of bacterial infection. The nanoparticulate cephalosporin particles may be formulated as a controlled release drug delivery system whereby the particles are coated one or more times with one or more natural or synthetic hydrophilic or hydrophobic polymer coating materials or dispersed throughout a natural or synthetic hydrophilic and/or hydrophobic polymer matrix.
    Type: Application
    Filed: May 16, 2006
    Publication date: October 29, 2009
    Applicant: ELAN PHARMA INTERNATIONAL LIMITED
    Inventors: John Devane, Paul Stark, Niall Fanning, Gurvinder Rekhi, Scott Jenkins, Gary Liversidge
  • Publication number: 20090197855
    Abstract: A chewable tablet dosage form comprising Cefdinir or pharmaceutically acceptable salts thereof for the oral administration of Cefdinir in a manner that is more palatable and less objectionable to population group's especially young children and older patients. A method of preparing the chewable tablets comprising Cefdinir and method of treatment using the same.
    Type: Application
    Filed: March 8, 2007
    Publication date: August 6, 2009
    Inventors: Makarand Krishnakumar Avachat, Sanjay Chhagan Wagh, Nital Arvind Jugade
  • Publication number: 20090004279
    Abstract: A method for improvement of tolerance for therapeutically effective agents delivered by inhalation comprising a pretreatment of a patient with a nebulized lidocaine or a lidocaine-like compound administered immediately or up to about thirty minutes before administration of the primary therapeutically effective agent. The pretreatment of the patient with the nebulized lidocaine or a lidocaine-like compound improves airway tolerance and deposition of the agent in the lungs and makes such deposition more safe, efficacious, controllable and predictable. The method of the invention is especially useful for enhancement of deposition of immunosuppressive agents in the lung(s) of transplant patients, improved tolerance of the drugs by reducing cough, and improving pulmonary drug deposition.
    Type: Application
    Filed: September 10, 2008
    Publication date: January 1, 2009
    Inventors: Thomas Hofmann, Alan Bruce Montgomery, Kevin Stapleton, William R. Baker
  • Publication number: 20080312203
    Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: August 21, 2008
    Publication date: December 18, 2008
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Patent number: 6911441
    Abstract: Novel pharmaceutical compositions of a cephalosporin in a prolonged release vehicle, comprising an oil and aluminium distearate, provide a prolonged duration of effective blood-plasma concentration of the cephalosporin after injection to animals.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: June 28, 2005
    Assignee: Akzo Nobel N.V.
    Inventors: Peter Schmid, Alexander Boettner, Carsten Schmidt, Mark Allan, Carole Barbot
  • Patent number: 6599892
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: July 29, 2003
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Patent number: 6514963
    Abstract: The present invention comprises methods and compositions for use in inhibiting egg production by parasitic trematode worms comprising administering to an individual in need thereof an effective amount of an agent which transiently inhibits the influx of calcium through a cell membrane calcium channel. Inhibition of egg production in the worms ameliorates many of the symptoms and pathology related to infection by trematode related diseases, including Schistosomiasis. The methods can also effect disease transmission by reducing the number of eggs released into the environment available to continue the worm life cycle.
    Type: Grant
    Filed: July 18, 2001
    Date of Patent: February 4, 2003
    Assignee: The Regents of the University of California
    Inventors: Mark Walter, Armand Kuris
  • Publication number: 20020099206
    Abstract: The object of the invention is to provide cephalosporin crystals which are highly stable for a long period under economical storage conditions. The cephalosporin crystals of the invention are obtainable by crystallizing an oily cephalosporin in a solvent containing an alcohol.
    Type: Application
    Filed: January 9, 2002
    Publication date: July 25, 2002
    Inventors: Yutaka Kameyama, Takashi Shiroi
  • Patent number: 6407091
    Abstract: The invention provides compounds of formula I and IV: wherein R1-R11 and A 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 IV, and novel intermediates useful for the synthesis of compounds of formula I and IV. The A can be, for example, thio, sulfinyl, or sulfonyl.
    Type: Grant
    Filed: April 13, 2000
    Date of Patent: June 18, 2002
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
  • Patent number: 6303592
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: October 16, 2001
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Publication number: 20010011085
    Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.
    Type: Application
    Filed: August 14, 1997
    Publication date: August 2, 2001
    Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
  • 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: 5728691
    Abstract: Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are described. These compounds possess antibacterial, growth promoting and probiotic activity.
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: March 17, 1998
    Assignees: Laboratorios Aranda S.A. De C.V., Judith Marcia Arrieta Munguia
    Inventor: Miguel Angel Corpi Constantino