The Other Cyclo Of The Bicyclo Ring System Is Five-membered Patents (Class 514/210.09)
  • Patent number: 10953070
    Abstract: The present disclosure provides dry powder antibiotic compositions that are effective in the treatment of bacterial infections and associated conditions. Moreover, the present disclosure provides dry powder antibiotic compositions for the treatment of bacterial infections, by multi-drug resistant bacteria, resulting in the subsequent reduction in the prevalent rates of drug resistance.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: March 23, 2021
    Assignees: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY HOSPITAL
    Inventors: Desmond Heng, Sie Huey Lee, Jeanette Teo, Wai Kiong Ng, Reginald Tan
  • Patent number: 10016383
    Abstract: The present application relates to combination treatments for bacterial infections. For example, the application relates to the use of one or more ?-lactam antibiotics and one or more compounds of Formula I: (I) for treatment of a metallo-B-lactamase-expressing bacterial infection or a disease, disorder or condition arising from a metallo-B-lactamase-expressing bacterial infection.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: July 10, 2018
    Assignee: McMaster University
    Inventors: Gerry Wright, Wenliang Wang, Andrew King
  • Patent number: 9751856
    Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: April 17, 2017
    Date of Patent: September 5, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20150126435
    Abstract: Disclosed are primers, probes, and single nucleotide polymorphisms (SNP) specific to a distinct subclones of the E. coli sequence type 131 (ST131). Also disclosed are methods and assay kits useful in detecting the presence of the distinct subtype of E. coli and methods of treating a subject suffering from an infection from a subclone of ST131.
    Type: Application
    Filed: July 2, 2013
    Publication date: May 7, 2015
    Inventors: Lance B. Price, Evgueni V. Sokurenko, James R. Johnson
  • Publication number: 20150045340
    Abstract: The present invention relates to novel ?-lactam compounds, their preparation and use. In particular, this invention relates to novel ?-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 12, 2015
    Applicant: AiCuris GmbH & Co. KG
    Inventors: Burkhard Klenke, Irith Wiegand, Guido Schiffer, Heike Broetz-Oesterhelt, Samarendra N. Maiti, Jehangir Khan, Andhe Reddy, Zhixiang Yang, Mostafa Hena, Guofeng Jia, Ou Ligong, Hong Liang, Judy Yip, Chuanjun Gao, Sabiha Tajammul, Rahim Mohammad, Ganguli Biswajeet
  • Publication number: 20140315876
    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 12, 2014
    Publication date: October 23, 2014
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Publication number: 20140221330
    Abstract: An objective of the present invention is to provide a novel NDM (New Delhi metallo-?-lactamase) inhibitor that functions as a drug for restoring the antibacterial activity of ?-lactam antibiotics that have been inactivated as a result of decomposition by NDM.
    Type: Application
    Filed: July 26, 2012
    Publication date: August 7, 2014
    Inventors: Akihiro Morinaka, Kazunori Maebashi, Takashi Ida, Muneo Hikida, Mototsugu Yamada, Takao Abe
  • Patent number: 8673934
    Abstract: The invention refers to agents for the preventive therapy after acute stroke, in particular having the aim to prevent infections after stroke. The agents inventively employed in pharmaceutical preparations are anti-infective agents and/or immunomodulating agents, e.g. cytokines and/or inhibitors of the SNS.
    Type: Grant
    Filed: March 5, 2003
    Date of Patent: March 18, 2014
    Inventors: Andreas Meisel, Konstantin Prass, Christian Meisel, Elke Halle, Ulrich Dirnagl, Hans Dieter Volk
  • Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • 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.
  • Publication number: 20130303504
    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: November 14, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130296290
    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: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130296292
    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: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130296291
    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: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130296293
    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: November 7, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130274238
    Abstract: 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: Application
    Filed: June 12, 2013
    Publication date: October 17, 2013
    Inventors: Eric Desarbre, Malcolm G.P. Page
  • 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: 20130196900
    Abstract: The present invention provides compounds and compositions that enhance the innate immune system. The present invention comprises methods of preventing, treating or ameliorating an infectious disease comprising administering said compounds to a subject. The invention also comprises methods of formulation and administration of said compounds.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 1, 2013
    Applicant: MONTANA STATE UNIVERSITY
    Inventor: MONTANA STATE UNIVERSITY
  • Publication number: 20130178456
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130171210
    Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating acute wounds, chronic wounds and/or a wound or epithelial tissue surface that contains bacterial biofilm, including unexpected synergy between bismuth-thiol (BT) compounds and certain antibiotics, to provide topical formulations including antiseptic formulations, for management and promotion of wound healing and in particular infected wounds. Previously unpredicted antibacterial properties and anti-biofilm properties of disclosed BT compounds and BT compound-plus-antibiotic combinations are also described, including preferential efficacies of certain such compositions for treating gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating gram-negative bacterial infections.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 4, 2013
    Applicant: MICROBION CORPORATION
    Inventor: MICROBION CORPORATION
  • Publication number: 20130172313
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
    Type: Application
    Filed: December 13, 2012
    Publication date: July 4, 2013
    Applicant: FOB SYNTHESIS, INC.
    Inventor: FOB Synthesis, Inc.
  • Publication number: 20130065878
    Abstract: Provided herein are cell-free systems for generating carbapenems, e.g., a compound of the Formula (I): or salts thereof; wherein , R1, R2, R3, R4, R5, and R6 are defined herein. Also provided are pharmaceutical compositions comprising a compound generated by the inventive cell-free system, and use of these compounds and compositions for the treatment of bacterial infections.
    Type: Application
    Filed: September 7, 2012
    Publication date: March 14, 2013
    Inventors: William Jeremy Blake, Daniel Klein-Marcuschamer
  • 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
  • Patent number: 8329685
    Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: December 11, 2012
    Assignee: North West University
    Inventor: Petrus Johannes Meyer
  • Patent number: 8258127
    Abstract: A method for treating individuals affected with latent tuberculosis comprising a step of administering an effective amount of one or more carbapenem compounds to the said individuals.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: September 4, 2012
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Luc Mainardi, Michel Arthur, Laurent Gutmann, Marie Lavollay
  • Patent number: 8232268
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: July 31, 2012
    Assignee: FOB Synthesis, Inc.
    Inventors: Woo-Baeg Choi, Ewa Kowalik
  • Publication number: 20120149672
    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: February 17, 2012
    Publication date: June 14, 2012
    Inventors: Rodney Benjamin, Jeffrey Varelman, Anthony Keller
  • Patent number: 8183233
    Abstract: Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about ?50° C. to about ?10° C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (?50 to ?10° C.), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: May 22, 2012
    Assignees: Baxter International Inc., Baxter Healthcare S.A.
    Inventors: James E. Kipp, Joseph Chung Tak Wong, Lakshmy Nair, Reagan Miller, Barrett E. Rabinow
  • Patent number: 8173633
    Abstract: Disclosed is a protein kinase C enhancer characterized by containing a benzothiophene alkyl ether derivative represented by the general formula below or a salt thereof. (In the formula, R1 and R2 may be the same or different and represent one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkenyl group, an amino group, a heterocyclic group, an optionally protected amino group, a hydroxyl group, a carboxyl group, an oxo group and the like; R3 represents an alkylamino group, an amino group, a hydroxyl group or the like; and m and n may be the same or different and represent an integer of 1-6.) This protein kinase C enhancer is useful for treatment or prevention of various diseases associated with protein kinase C.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Tetsuo Fukushima, Akiko Takagi, Nobuo Terashima
  • Publication number: 20110287083
    Abstract: Bioabsorbable compositions of A) blends of bioabsorbable homopolymers and/or copolymers containing glycolide and lactide and B) salts of fatty acids and/or fatty acid esters are described. Processes for making the compositions and surgical articles made totally or in part therefrom, including suture coatings, are also described.
    Type: Application
    Filed: July 21, 2011
    Publication date: November 24, 2011
    Applicant: Tyco Healthcare Group LP
    Inventor: Ahmad R. Hadba
  • Publication number: 20110274651
    Abstract: Compositions and methods for treating or preventing infectious diseases, and inhibiting the ability of microbes to travel within mammalian cells, and inhibiting microbial replication, are disclosed. The compositions include various noscapine analogs, which are capable of blocking the movement of viruses and other microbes within mammalian and other cells by inhibiting the cytoplasmic transport mechanisms within the cells. The compositions described herein include an effective amount of the noscapine analogues described herein, along with a pharmaceutically acceptable carrier or excipient. The compositions can also include one or more additional antimicrobial compounds.
    Type: Application
    Filed: September 4, 2009
    Publication date: November 10, 2011
    Applicant: Emory University
    Inventors: Cory Acuff, Daniel Kalman
  • Publication number: 20110251169
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: April 5, 2011
    Publication date: October 13, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Publication number: 20110182869
    Abstract: This invention relates to products comprising antibiotics or probiotics and the use thereof for the treatment of gut motility disorders such as irritable bowel syndrome (IBS).
    Type: Application
    Filed: July 14, 2009
    Publication date: July 28, 2011
    Inventors: Jan Knol, Kaouther Ben Amor, Richèle Deodata Wind
  • Publication number: 20110166119
    Abstract: A pharmaceutical composition comprising carbapenem and Aztreonam each in the dosage range of about 0.25 g to 0.75 g and pharmaceutically acceptable excipients for the prevention and treatment of infections caused by Pseudomonas aeruginosa, Acinetobacter baumannii, Klebsiella pneumoniae or MRSA (Methicillin Resistant Staphylococcus aureus).
    Type: Application
    Filed: December 1, 2009
    Publication date: July 7, 2011
    Applicant: Glade Organics Private Limited
    Inventor: Kalyanasundaram Kasiviswanathan
  • 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: 20110028407
    Abstract: The present invention provides compounds and compositions that enhance the innate immune system. The present invention comprises methods of preventing, treating or ameliorating an infectious disease comprising administering said compounds to a subject. The invention also comprises methods of formulation and administration of said compounds.
    Type: Application
    Filed: February 8, 2008
    Publication date: February 3, 2011
    Inventors: Mark A. Jutila, Kirk J. Lubick
  • Publication number: 20100256082
    Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.
    Type: Application
    Filed: June 12, 2007
    Publication date: October 7, 2010
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventor: Robert J. Schotzinger
  • Publication number: 20100160284
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.
    Type: Application
    Filed: February 15, 2010
    Publication date: June 24, 2010
    Applicant: FOB Synthesis, Inc.,
    Inventors: Woo-Baeg Choi, Ewa Kowalk
  • Publication number: 20100152101
    Abstract: The present invention relates to the use of a Compound of formula I preferably 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or a pharmaceutically acceptable salt thereof for the preparation of a medicament for use in the treatment of biofilm formation, e.g. of P. aeruginosa, e.g. in cystic fibrosis patients.
    Type: Application
    Filed: May 21, 2008
    Publication date: June 17, 2010
    Applicant: Novartis AG
    Inventor: David Reid
  • Publication number: 20100075945
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.
    Type: Application
    Filed: November 6, 2009
    Publication date: March 25, 2010
    Inventors: Woo-Baeg Choi, David S. Menaldino, Deog-II Kim, Martin Bouygues, Michael W. Hager
  • Patent number: 7683049
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions, wherein the compounds are generally of the Formulae The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: March 23, 2010
    Assignee: FOB Synthesis, Inc.
    Inventors: Woo-Baeg Choi, Ewa Kowalik
  • Publication number: 20100063023
    Abstract: Provided is a ?-lactamase antibiotic and a compound of formula I, a process of producing the compound, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: September 9, 2009
    Publication date: March 11, 2010
    Applicant: Wyeth
    Inventors: Tarek Suhayl Mansour, Aranapakam Mudumbai Venkatesan
  • Publication number: 20100056478
    Abstract: A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a ?-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another ?-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI).
    Type: Application
    Filed: December 7, 2006
    Publication date: March 4, 2010
    Inventors: Eric Desarbre, Bérangère Gaucher, Malcolm G.P. Page, Patrick Roussel
  • Publication number: 20100040548
    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: June 10, 2009
    Publication date: February 18, 2010
    Inventor: Chongxi Yu
  • Publication number: 20100022504
    Abstract: A method for treating individuals affected with latent tuberculosis comprising a step of administering an effective amount of one or more carbapenem compounds to the said individuals.
    Type: Application
    Filed: July 28, 2008
    Publication date: January 28, 2010
    Applicant: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)
    Inventors: JEAN-LUC MAINARDI, MICHEL ARTHUR, LAURENT GUTMANN, MARIE LAVOLLAY
  • Publication number: 20100016208
    Abstract: Photoactivatable antimicrobial compounds and methods for the use thereof in the treatment of infections are provided.
    Type: Application
    Filed: November 15, 2006
    Publication date: January 21, 2010
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Tayyaba Hasan, Gerald J. Nau
  • Patent number: 7632828
    Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions, wherein the compounds are generally of the Formulae The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ÿ-methyl carbapenems which are useful as antibacterial agents.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: December 15, 2009
    Assignee: FOB Synthesis, Inc.
    Inventors: Woo-Baeg Choi, David S. Menaldino, Deog-Il Kim, Martin Bouygues, Michael W. Hager
  • Publication number: 20090286764
    Abstract: Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about ?50° C. to about ?10° C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (?50 to ?10° C.), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject.
    Type: Application
    Filed: May 8, 2009
    Publication date: November 19, 2009
    Applicants: Baxter International Inc., Baxter Healthcare S.A.
    Inventors: JAMES E. KIPP, JOSEPH CHUNG TAK WONG, LAKSHMY NAIR, REAGAN MILLER, BARRETT E. RABINOW
  • Publication number: 20090029964
    Abstract: An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R0 represents hydrogen atom or the like; R1 represents C1-C3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH2(CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH2—, —NRaCH2— (wherein Ra represents hydrogen atom, optionally substituted C1-C4 alkyl group or the like) or the like.
    Type: Application
    Filed: March 23, 2006
    Publication date: January 29, 2009
    Inventors: Makoto Sunagawa, Akira Sasaki, Takashi Tsukimura