3-position Substituent Contains -cooc- Group Patents (Class 514/195)
  • Patent number: 10233197
    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: Grant
    Filed: July 16, 2012
    Date of Patent: March 19, 2019
    Assignee: TECHFIELDS PHARMA CO., LTD.
    Inventor: Chongxi Yu
  • Patent number: 9999859
    Abstract: With the subject invention, a method is provided for preparing a filter membrane including the steps of dispersing a liquid which is generally hydrophobic into the pores of a porous membrane, and applying a solution containing lipids onto at least a first surface of the porous membrane containing the liquid. Advantageously, the subject invention allows for filter membranes to be prepared which can be stored for periods of time without degradation in performance. The subject invention may have applicability in various contexts, but is well-suited for preparing filter membranes for permeability screening, particularly Parallel Artificial Membrane Permeability Assay (PAMPA).
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: June 19, 2018
    Assignee: Corning Incorporated
    Inventors: Xiaoxi (Kevin) Chen, Charles L. Crespi
  • Patent number: 9452977
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: September 27, 2016
    Assignees: KYORIN PHARMACEUTICAL CO., LTD., TEIJIN PHARMA LIMITED
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Patent number: 9120808
    Abstract: The present invention relates to compounds of formula I and to compounds of formula II wherein the substituents have various meanings. These compounds are useful as beta lactamase inhibitors.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: September 1, 2015
    Assignee: NABRIVA THERAPEUTICS AG
    Inventor: Atchyuta Rama Chandra Murty Bulusu
  • Patent number: 9012442
    Abstract: The invention describes a composition for combating beta-lactamase-mediated antibiotic resistance using beta-lactamase inhibitor useful for injection, capable of pharmaceutical application. The invention relates to pharmaceutical composition containing ceftriaxone (normally as ceftriaxone sodium) and sulbactam (normally as sulbactam sodium). Such compositions are found to be useful for intramuscular or intravenous administration as antibiotics for hospitalized patients with serious infections. Specifically, this invention relates to a pharmaceutical composition further including an aminocarboxylic acid chelating agent, for example, ethylenediaminetetraacetic acid (EDTA), or a pharmaceutically acceptable salt thereof. The pharmaceutical compositions of this invention have been found normally to enhance resistance to particulate formation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use.
    Type: Grant
    Filed: September 25, 2012
    Date of Patent: April 21, 2015
    Assignee: Venus Remedies Limited
    Inventor: Manu Chaudhary
  • Publication number: 20150105337
    Abstract: The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.
    Type: Application
    Filed: October 16, 2014
    Publication date: April 16, 2015
    Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Elizabeth Marie Nolan, Tengfei Zheng, Phoom Chairatana
  • Patent number: 8957058
    Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: October 3, 2011
    Date of Patent: February 17, 2015
    Assignee: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Berthon
  • Publication number: 20140378415
    Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8901293
    Abstract: New monobactam antibiotics compounds which contain an 3-amino-azetidin-2-one ring and are active against gram-negative bacteria, wherein the compounds include the compound 2-(2-amino-thiazol-4-yl)-2-[(Z)-(1H,4H-1,5-dihydroxy-4-oxo-pyridin-2-yl)methoxyimino]-N-[3(S)-1-oxysulfonyl-2,2-dimethyl-4-oxo-azetidin-3-yl]acetamide.
    Type: Grant
    Filed: December 7, 2006
    Date of Patent: December 2, 2014
    Assignee: Basilea Pharmaceutica AG
    Inventors: Eric Desarbre, Bérangére Gaucher, Malcolm G. P. Page, Patrick Roussel
  • Publication number: 20140206636
    Abstract: Disclosed is a method of treating small intestinal bacterial overgrowth (SIBO) or a SIBO-caused condition in a human subject. SIBO-caused conditions include irritable bowel syndrome, fibromyalgia, chronic pelvic pain syndrome, chronic fatigue syndrome, depression, impaired mentation, impaired memory, halitosis, tinnitus, sugar craving, autism, attention deficit/hyperactivity disorder, drug sensitivity, an autoimmune disease, and Crohn's disease. Also disclosed are a method of screening for the abnormally likely presence of SIBO in a human subject and a method of detecting SIBO in a human subject. A method of determining the relative severity of SIBO or a SIBO-caused condition in a human subject, in whom small intestinal bacterial overgrowth (SIBO) has been detected, is also disclosed.
    Type: Application
    Filed: September 12, 2013
    Publication date: July 24, 2014
    Applicant: CEDARS-SINAI MEDICAL CENTER
    Inventors: Henry C. Lin, Mark Pimentel
  • Publication number: 20140206633
    Abstract: The present invention relates to processes for the preparation of compounds of formula IB wherein A1, A2, A3, A4, L, Y1, Y2, R1, R2, R3, R4 and R5 are as defined in the claims, comprising reacting a compound of formula (II) wherein Y1, Y2, L, A1, A2, R1, R2, R3, R4 and R5 are as defined for the compound of formula (I); with hydroxylamine in the presence of water, a base and a chiral phase transfer catalyst, which chiral phase transfer catalyst is a quinine derivative. The invention also relates to compounds of formula IB and enantiomerically enriched mixtures comprising compounds of formula IB.
    Type: Application
    Filed: February 3, 2011
    Publication date: July 24, 2014
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Nicholas Phillip Mulholland, Edouard Godineau, Jérôme Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Revol
  • Publication number: 20140206606
    Abstract: The present invention provides compounds of formula (I), wherein G1 is oxygen; R1 is hydrogen; R2 is group P (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y1 is C—R6, CH or nitrogen; Y2 and Y3 are independently CH or nitrogen; wherein no more than two of Y1, Y2 and Y3 are nitrogen and wherein Y2 and Y3 are not both nitrogen; R5 is hydrogen, halogen, cyano, nitro, NH2, C1-C2alkyl, C1-C2haloalkyl, C3-C5cycloalkyl, C3-C5halocycloalkyl, C1-C2alkoxy, C1-C2haloalkoxy; R6 together with R5 forms a —CH?CH—CH?CH— bridge; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 24, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140194376
    Abstract: The present invention provides compounds of formula (I) wherein G1 is oxygen; R1 is hydrogen; R2 is group (P) L is a bond, methylene or ethylene; one of A1 and A2 is S, SO or SO2 and the other is —C(R4)R4—; R3 is hydrogen or methyl; each R4 is independently hydrogen or methyl; Y2 and Y3 are independently CH or nitrogen, wherein Y2 and Y3 are not both nitrogen; X2 is C—X6 or nitrogen; X1, X3 and X6 are independently hydrogen, halogen or trihalomethyl, wherein at least two of X1, X3 and X6 are not hydrogen; X4 is trifluoromethyl, difluoromethyl or chlorodifluoromethyl. The invention also provides intermediates useful for the preparation of compounds of formula (I), as well as methods of controlling insects, acarines, nematodes or molluscs using the compounds of formula (I).
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Thomas Pitterna, Myriem El Qacemi
  • Publication number: 20140128358
    Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: October 3, 2011
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Berthon
  • Publication number: 20140107056
    Abstract: The present invention provides compounds of formula (I): wherein A1, A2, A3 and A4 are independently of one another C—H, C—R5, or nitrogen; B1—B2—B3—B4 is —CH2—C?N—CH2—, —CH2—N—CH2—CH2—, —CH2—C?CH-0- or —CH?C—CH2-0-; G1 is oxygen or sulfur; L is a single bond or C1-C8alkylene; R1 is hydrogen, C1-C8alkyl, C1-C8alkylcarbonyl-, C1-C8alkoxy, C2-C8alkenyl, C2-C8alkynyl, C1-C8alkoxy-C1-C8alkyl, aryl or aryl substituted by one to three R6, or R1 is heterocyclyl or heterocyclyl substituted by one to three R6 or C1-C8alkoxycarbonyl-; R2 is hydrogen, C1-C8haloalkyl or C1-C8alkyl; R3 is C1-C8haloalkyl; R4 is aryl or aryl substituted by one to three R6, or R4 is heterocyclyl or heterocyclyl substituted by one to three R6; Y1 is CR7R8, C?O or C?S; Y2, Y3 and Y4 are independently CR7R8, C=0, C?S, N—R9, O, S, SO or SO2; wherein at least two adjacent ring atoms in the ring formed by Y1, Y2, Y3 and Y4 are heteroatoms; each R7 and R8 is independently hydrogen, halogen, C1-C8alkyl, or C1-C8haloalkyl; and R5, R6, R7, R8 and R9 a
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
  • Publication number: 20140107057
    Abstract: The present invention provides a combination product comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is a further therapeutic agent; wherein the combination product is for use in a method of therapeutic treatment.
    Type: Application
    Filed: May 30, 2012
    Publication date: April 17, 2014
    Applicant: Syngenta Participations AG
    Inventors: Jerome Yves Cassayre, Myriem El Qacemi
  • Publication number: 20140057888
    Abstract: Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as ?-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ?-lactamases. These compounds restore/potentiate the activities of ?-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ?-lactamases.
    Type: Application
    Filed: November 25, 2011
    Publication date: February 27, 2014
    Inventors: Senthilkumar Udayampalayam Palanisamy, Maneesh Paul-Satyaseela, Shridhar Narayanan, Gopalan Balasubramanian, Aravind Appu, Senthilnathan Manickam, Hariharam Periasamy
  • Patent number: 8557800
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Grant
    Filed: October 19, 2011
    Date of Patent: October 15, 2013
    Assignee: Apogee Biotechnology Corporation
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Publication number: 20130084343
    Abstract: Methods of sepsis in a sample from a patient are provided. Methods of detecting changes in expression of one or more RNAs associated with sepsis are also provided. Compositions and kits are also provided.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 4, 2013
    Applicant: CEPHEID
    Inventors: David Vilanova, Olivier Delfour
  • Publication number: 20130059795
    Abstract: This invention describes a novel composition of matter describing a complex comprising leaf protein and a lipophilic substance(s), along with the method of producing it. Delivery of lipid-soluble materials into the body is challenging because they are generally highly insoluble in water and very subject to oxidative degradation. The inventors have found that leaf protein—the water-soluble proteins derived from plant leaves—can efficiently form a complex with lipophilic materials. This leaf protein—lipid-soluble material complex is an effective carrier of lipophilic substances. As such, the leaf protein—lipid-soluble material complex disclosed herein can be used for the delivery of lipophilic vitamins, fatty acids, caretenoids, lipophilic drugs, and other lipophilic materials. This complex can be used to deliver lipophiles in foods, nutritional and dietary supplements, topical compositions and in pharmaceutical products.
    Type: Application
    Filed: March 7, 2011
    Publication date: March 7, 2013
    Inventors: Yangming Martin Lo, Ansu Elizabeth Cherian, Neil Allen Belson
  • Publication number: 20130023512
    Abstract: The invention describes a composition for combating beta-lactamase-mediated antibiotic resistance using beta-lactamase inhibitor useful for injection, capable of pharmaceutical application. The invention relates to pharmaceutical composition containing ceftriaxone (normally as ceftriaxone sodium) and sulbactam (normally as sulbactam sodium). Such compositions are found to be useful for intramuscular or intravenous administration as antibiotics for hospitalized patients with serious infections. Specifically, this invention relates to a pharmaceutical composition further including an aminocarboxylic acid chelating agent, for example, ethylenediaminetetraacetic acid (EDTA), or a pharmaceutically acceptable salt thereof. The pharmaceutical compositions of this invention have been found normally to enhance resistance to particulate formation in solutions to be administered parenterally. The invention also gives details of the dosage forms stored in sealed containers to be reconstituted before use.
    Type: Application
    Filed: September 25, 2012
    Publication date: January 24, 2013
    Applicant: Venus Remedies Limited
    Inventor: Venus Remedies Limited
  • Publication number: 20130004577
    Abstract: A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.
    Type: Application
    Filed: September 7, 2012
    Publication date: January 3, 2013
    Applicant: NIPPON SHINYAKU
    Inventors: Hironobu KATO, Hirokazu SAKAMOTO
  • Publication number: 20120052124
    Abstract: The present invention provides for silk fibroin-based compositions comprising one or more antibiotic agents for prevention or treatment of microbial contamination, methods of making antibiotic-containing silk scaffold, methods of stabilizing antibiotics in silk scaffolds, and methods for preventing or treating microbial contamination using the antibiotic-containing compositions. Various methods may be used to embed the antibiotic(s) into the silk fibroin-based compositions. The antibiotic-containing compositions of the invention are particular useful for stabilizing antibiotics, preventing bacterial infections, and for medical implants, tissue engineering, drug delivery systems, or other pharmaceutical or medical applications.
    Type: Application
    Filed: March 4, 2010
    Publication date: March 1, 2012
    Applicant: TRUSTEES OF TUFTS COLLEGE
    Inventors: David L. Kaplan, Bruce Panilaitis, Eleanor M. Pritchard, Fiorenzo Omenetto, Jordan Axelrad
  • Publication number: 20110294760
    Abstract: The invention generally relates to compositions and methods for preventing sternal wound infections, such as mediastinitis. In certain embodiments, the invention provides an antimicrobial composition including at least one bioresorbable polymer, such as a tyrosine-derived polyesteramide, and at least one antimicrobial agent, in which the composition is adapted to be topically applied to an esophageal perforation in a subject or a median sternotomy incision site in the subject, and in which the at least one antimicrobial agent is present in an amount effective to inhibit development of mediastinitis in the subject.
    Type: Application
    Filed: June 1, 2010
    Publication date: December 1, 2011
    Applicant: TyRx Pharma, Inc.
    Inventors: Raman Bahulekar, Arikha Moses, Satish Pulapura, William C. McJames, II, Fatima Buevich
  • Patent number: 8063248
    Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.
    Type: Grant
    Filed: December 23, 2007
    Date of Patent: November 22, 2011
    Assignee: Apogee Biotechnology Corporation
    Inventors: Charles D. Smith, Kevin J. French, Yan Zhuang
  • Publication number: 20110269689
    Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC 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: December 4, 2009
    Publication date: November 3, 2011
    Inventor: Chongxi Yu
  • Publication number: 20110207687
    Abstract: This invention relates to a fulvic acid and antibiotic combination for use in the treatment of various diseases and conditions. The invention further relates to the use of the combination for the treatment of various diseases and conditions, including bacterial infection. In particular, the bacteria are antibiotic resistant bacteria.
    Type: Application
    Filed: June 4, 2009
    Publication date: August 25, 2011
    Applicant: PFEISMITH S.A. (PTY) LTD
    Inventors: Antonio Celestino Fernandes, Elizabeth Medlen, Stephen Leivers
  • Patent number: 7795244
    Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: September 14, 2010
    Assignee: Pfizer Inc.
    Inventors: Katherine Elizabeth Brighty, Anthony Marfat, Dale M. McLeod, John P. O'Donnell
  • Patent number: 7795243
    Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: September 14, 2010
    Assignee: Pfizer, Inc.
    Inventors: Katherine E. Brighty, Anthony Marfat, Dale G. McLeod, John P. O'Donnell
  • 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: 7687488
    Abstract: Novel 2-substituted methyl penam derivatives include the formula (I), their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their solvates, their pharmaceutically acceptable salts, and pharmaceutical compositions containing them; wherein A=C or N; Het is a three- to seven-membered heterocyclic ring; R1 represents carboxylate anion, or —COOR4 where R4 represents hydrogen, carboxylic acid protecting group or a pharmaceutically acceptable salt; R2 and R3 may be same or different and independently represent hydrogen, halogen, amino, alkyl, protected amino, optionally substituted alkyl, alkenyl, alkynyl and the like; R represents substituted or unsubstituted alkyl, alkenyl, aryl, aralkyl, cycloalkyl, heterocyclyl or heterocyclylalkyl.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: March 30, 2010
    Assignee: Orchid Chemicals & Pharmaceuticals Ltd.
    Inventors: Senthilkumar Udayampalayam Palanisamy, Andrew Gnanaprakasam, Panchapakesan Ganapathy, Mukut Gohain, Venkatasubramanian Hariharan, Sriram Rajagopal, Maneesh Paul-Satyaseela, Shakti Singh Solanki, Sathishkumar Devarajan
  • 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: 20100048528
    Abstract: This invention discloses and claims methods for inhibiting bacterial ?-lactamases and treating bacterial infections by inhibiting bacterial ?-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a ?-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a ?-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.
    Type: Application
    Filed: November 2, 2009
    Publication date: February 25, 2010
    Applicant: Novexel
    Inventors: Jozsef Aszodi, Claude Fromentin, Maxime Lampilas, David Alan Rowlands
  • Publication number: 20100009954
    Abstract: Inhibitors of the enzyme beta-lactamase are provided. 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: Application
    Filed: May 11, 2009
    Publication date: January 14, 2010
    Inventors: John D. Buynak, Anjaneyulu Sheri, Sundar Ram Reddy Pagadala
  • 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: 20090075966
    Abstract: The present application describes deuterium-enriched tazobactam, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 11, 2008
    Publication date: March 19, 2009
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • Publication number: 20090075965
    Abstract: The present application describes deuterium-enriched amoxicilin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: September 5, 2008
    Publication date: March 19, 2009
    Applicant: Protia, LLC
    Inventor: Anthony W. Czarnik
  • 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
  • Publication number: 20080193428
    Abstract: The present invention relates to the use of benzoic acid and/or its sodium salt in combination with saccharide(s) as active components in the manufacture of a vaginal composition for modulating vaginal flora and vaginal acidity, thereby maintaining the pH value of vaginal secretion within a range from 3.5 to 4.5; and the present invention further relates to a vaginal composition and a method for modulating and maintaining normal vaginal flora and vaginal acidity.
    Type: Application
    Filed: April 27, 2006
    Publication date: August 14, 2008
    Applicants: Shenzhen Phlora Biotechnology Limited, HK Phlora Health Science & Technology Ltd.
    Inventors: Ruyun Zhou, Zhongming Zeng
  • Publication number: 20080125408
    Abstract: The invention relates to prodrugs of sulopenem of formula (I): wherein R1 is —(C2-C8)alkyl, or a solvate or hydrate thereof. The invention also relates to the preparation, formulation, and use of the prodrugs of sulopenem to treat a disorder such as an infection in a patient in need thereof.
    Type: Application
    Filed: November 13, 2007
    Publication date: May 29, 2008
    Inventors: Katherine Elizabeth Brighty, Anthony Marfat, Dale Gordon McLeod, John P. O'Donnell, Stephen R. Anderson
  • 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
  • Patent number: 7091197
    Abstract: Prodrugs of 6-?-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed are pharmaceutical compositions comprising a prodrug of the present invention or a solvate thereof, an optional beta-lactam antibiotic and a pharmaceutically acceptable excipient. Further disclosed is a method for increasing the therapeutic effectiveness of a beta-lactam antibiotic in a mammal by administering an effective amount of a beta-lactam antibiotic and an effectiveness-increasing amount of a prodrug of the present invention, or a solvate thereof. Additionally disclosed is a method for treating a bacterial infection in a mammal by administering a therapeutically effective amount of a pharmaceutical composition of the present invention to a mammal in need thereof.
    Type: Grant
    Filed: August 25, 2003
    Date of Patent: August 15, 2006
    Assignee: Pfizer Inc.
    Inventors: Anthony Marfat, Dale G. McLeod
  • Publication number: 20040077622
    Abstract: The present invention provides a compound of formula 1, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: May 1, 2003
    Publication date: April 22, 2004
    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
  • Publication number: 20040043978
    Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
    Type: Application
    Filed: May 1, 2003
    Publication date: March 4, 2004
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
  • 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: 6495539
    Abstract: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond tha
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: December 17, 2002
    Assignee: Washington University
    Inventors: Scott J. Hultgren, Fredrik Almqvist, Gabriel Soto
  • 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: 6337339
    Abstract: Methods and compositions are disclosed utilizing the optically pure (S)-isomer of lomefloxacin to treat bacterial infection. In particular, this compound is a potent drug for the treatment of Mycobacteria infection.
    Type: Grant
    Filed: February 28, 2001
    Date of Patent: January 8, 2002
    Assignee: Sepracor Inc.
    Inventors: James W. Young, A. K. Gunnar Aberg
  • Patent number: 6271222
    Abstract: The present invention relates to penem antibacterial agents in which the releaseable liphophilic aromatic side-chain, tethered to the carbapenem nucleus via a methylene linker, necessary for anti-MRSA activity replaces the non-releaseable liphophilic side-chains found in 2-aryl and 2-benzothiazolylthio carbapenem compounds. The compound is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: April 23, 1999
    Date of Patent: August 7, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Frank P. Dininno