3-position Substituent Contains Pyridine Ring Patents (Class 514/203)
  • Patent number: 10308666
    Abstract: This disclosure provides methods of making certain 7-aminocephem derivatives useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: June 4, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • Patent number: 10059680
    Abstract: Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according to methods described herein. The methods provide products having desirable purity.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: August 28, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • Patent number: 9789097
    Abstract: Pharmaceutical compositions comprising imipenem or a pharmaceutically acceptable derivative, and a compound of Formula (I) or a stereoisomer or a pharmaceutically acceptable derivative thereof are disclosed.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: October 17, 2017
    Assignee: WOCKHARDT LIMITED
    Inventors: Sachin Bhagwat, Mahesh Vithalbhai Patel
  • Patent number: 9434728
    Abstract: Compound of Formula (I), its preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: September 6, 2016
    Assignee: WOCKHARDT LIMITED
    Inventors: Prasad Keshav Deshpande, Shivaji Sampatrao Pawar, Satish Bhawsar, Ravindra Dattatraya Yeole, Sachin Bhagwat, Mahesh Vithalbhai Patel
  • Patent number: 9359353
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: July 18, 2015
    Date of Patent: June 7, 2016
    Assignee: WOCKHARDT LIMITED
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Patent number: 9284314
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: March 15, 2016
    Assignee: Forest Laboratories Holdings Ltd.
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew Phillips, Mahendra G. Dedhiya
  • Patent number: 9045477
    Abstract: The present invention relates to azole bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 2, 2015
    Assignee: Epizyme, Inc.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Publication number: 20150141394
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 21, 2015
    Applicant: Wockhardt Ltd.
    Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 8969334
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: May 4, 2014
    Date of Patent: March 3, 2015
    Assignee: Wockhardt Ltd.
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Patent number: 8969570
    Abstract: Aryl substituted diazabicyclooctanes (DBO) compounds that inhibit ?-lactamases of class A, class C or class D and potentiate ?-lactam antibiotics are disclosed. In particular, this disclosure provides DBO compounds that, when used in the disclosed Synergy MIC Assay with a ?-lactam antibiotic at a fixed concentration have an MIC of 8 ?g/mL or less against one or more isogenic ?-lactamase expressing bacterial strains.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: March 3, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Robert Busch, Roland E. Dolle, Chester A. Metcalf, III
  • Patent number: 8962843
    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: Grant
    Filed: March 29, 2013
    Date of Patent: February 24, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8962844
    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: Grant
    Filed: March 29, 2013
    Date of Patent: February 24, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Dongpeng Wan
  • Patent number: 8940897
    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: Grant
    Filed: March 29, 2013
    Date of Patent: January 27, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Publication number: 20150025053
    Abstract: The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Application
    Filed: July 17, 2014
    Publication date: January 22, 2015
    Applicant: CUBIST PHARMACEUTICALS, INC.
    Inventors: Yong He, Yu Gui Gu, Ning Yin
  • Publication number: 20150018312
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: May 4, 2014
    Publication date: January 15, 2015
    Applicant: WOCKHARDT LTD.
    Inventors: Vijaykumar Jagdishwar PATIL, Ravikumar TADIPARTHI, Satish BIRAJDAR, Sachin BHAGWAT
  • Publication number: 20150017099
    Abstract: The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and/or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 15, 2015
    Inventors: Noam A. Cohen, Robert J. Lee, Danielle R. Reed
  • Patent number: 8933232
    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: Grant
    Filed: March 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Patent number: 8933233
    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: Grant
    Filed: March 29, 2013
    Date of Patent: January 13, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III
  • Publication number: 20150011524
    Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.
    Type: Application
    Filed: September 19, 2014
    Publication date: January 8, 2015
    Inventors: Larry SUTTON, Sophia YU
  • Patent number: 8927724
    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: Grant
    Filed: March 29, 2013
    Date of Patent: January 6, 2015
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch, Dongpeng Wan, Jon Christian Baber
  • Patent number: 8916709
    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: Grant
    Filed: March 29, 2013
    Date of Patent: December 23, 2014
    Assignee: Cubist Pharmaceuticals, Inc.
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Jon Christian Baber
  • Patent number: 8883772
    Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Compounds of the invention include those of formula: and pharmacologically acceptable salts thereof where variables Z, Y, M, y, n, R, R4, R5, R1 and R2 are as defined in the specification. M most generally represents a chemical moiety which is in conjugation with the nitrogen of the core beta-lactam ring system of the compound, such that one or more reactive species, e.g., electrophilic or nucleophilic sites are generated on modification of M which is initiated by cleavage of the beta-lactam ring. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition.
    Type: Grant
    Filed: October 9, 2008
    Date of Patent: November 11, 2014
    Assignee: Sopharmia, Inc.
    Inventors: Larry Sutton, Sophia Yu
  • Patent number: 8883773
    Abstract: A compound of the formula: wherein X is —N?, —CH?, or the like; W is —CH2— or the like; U is —S— or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; Q is a single bond or the like; R3 is hydrogen or the like; Ring A is a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; G is —C(?O)— or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: November 11, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Yamawaki, Hideki Sugimoto, Masayuki Sano
  • Publication number: 20140256697
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.
    Type: Application
    Filed: October 3, 2012
    Publication date: September 11, 2014
    Inventors: Kenji Yamawaki, Masayuki Sano, Jun Sato
  • Publication number: 20140249126
    Abstract: The present invention relates to cephalosporin antibacterial compounds of Formula (I): or corresponding pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods for bacterial infections, especially those caused by gram-negative bacteria.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Inventors: Xiangmin Liao, Neil David Pearson, Israil Pendrak, Masayuki Sano
  • Patent number: 8809314
    Abstract: The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: August 19, 2014
    Assignee: Cubist Pharmacueticals, Inc.
    Inventors: Yong He, Yu Gui Gu, Ning Yin, Dong Zou, Andre Lee Pearson
  • 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
  • Patent number: 8754102
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: June 17, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20140135296
    Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.
    Type: Application
    Filed: May 10, 2012
    Publication date: May 15, 2014
    Inventors: Vojo Deretic, Eliseo Castillo, Steven Bradfute, Larry A. Sklar
  • Publication number: 20140088068
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: August 24, 2012
    Publication date: March 27, 2014
    Inventors: Sachin Bhagwat, Prasad Keshav Deshpande, Satish Bhawsar, Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Shivaji Sampatrao Pawar, Sunil Bhaginath Jadhav, Sanjay Kisan Dabhade, Vikas Vitthalrao Deshmukh, Bharat Dond, Satish Birajdar, Mohammad Usman Shaikh, Deepak Dekhane, Piyush Ambalal Patel
  • 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: 20140088070
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infections are disclosed.
    Type: Application
    Filed: September 11, 2012
    Publication date: March 27, 2014
    Inventors: Vijaykumar Jagdishwar Patil, Ravikumar Tadiparthi, Satish Birajdar, Sachin Bhagwat
  • Publication number: 20130289012
    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: October 31, 2013
    Inventors: Yu Gui Gu, Yong He, Ning Yin, Dylan C. Alexander, Jason B. Cross, Chester A. Metcalf, III, Robert Busch
  • Publication number: 20130281425
    Abstract: Disclosed is a method of making particles of a drug wherein use is made of diafiltration. The diafiltration can be with anti-solvent, in which case a precipitate is obtained of particles as such. The diafiltration can also be with a pharmaceutically acceptable suspension medium. In that case several process steps of isolating, drying, transporting of particles can be avoided, because the suspension resulting from the synthesis of the particles is directly turned into a final drug product formulation.
    Type: Application
    Filed: January 11, 2012
    Publication date: October 24, 2013
    Applicant: Intervet International B.V.
    Inventors: Hans Peter Niedermann, Heiko Bothe
  • Publication number: 20130178455
    Abstract: The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 11, 2013
    Applicant: LEGOCHEM BIOSCIENCES, INC
    Inventor: Legochem Biosciences, Inc.
  • Publication number: 20130172309
    Abstract: Compositions and methods for the rapid and sensitive detection of a carbapenemase in a sample are provided. The compositions include novel primer and probe compositions for use in detecting the presence of this enzyme in a sample, particularly using PCR methods. These primers and probe sets can be used in amplification methods (such as PCR, particularly quantitative PCR) and packaged into kits for use in amplification methods for the purpose of detecting carbapenemase in a test sample, particularly a patient sample, particularly a direct sample. Thus, in one embodiment, the present invention provides for novel oligonucleotide primers set forth in SEQ ID NOs:1, 2, 4, 5, 7, 8, 14, 15, 17, 18, and 20, and the novel oligonucleotide probe sequences set forth in SEQ ID NOs:3, 6, 9, 16, and 19. These sequences can be used in a method of detecting carbapenemase in a sample.
    Type: Application
    Filed: December 3, 2012
    Publication date: July 4, 2013
    Applicant: BECTON, DICKINSON AND COMPANY
    Inventor: Becton, Dickinson and Company
  • Publication number: 20130164337
    Abstract: There is proposed herein a process for production of composite antimicrobial preparations for parenteral administration, featuring a higher therapeutic efficiency in case of grave infection and inflammatory diseases. The proposed compositions include active agents being betalactam antibiotics and finely dispersed nanostructured silica dioxide with a weight ratio from 10:1 to 75:1 respectively. The silica dioxide particles are antibiotic molecules delivery agents into the phagocytes, which allows increasing the antimicrobial preparations concentration at inflammation areas and considerably decrease microorganisms antibiotic resistance. The mentioned production process includes mixing betalactam antibiotic with finely dispersed nanostructured silica dioxide.
    Type: Application
    Filed: May 11, 2011
    Publication date: June 27, 2013
    Inventors: Viktor Lvovich Limonov, Konstantin Valentinoyich Gaidul, Aleksandr Valerevich Dushkin
  • Publication number: 20130156816
    Abstract: The invention features compositions, methods, and kits for the administration of an oxidatively transformed carotenoid, or a fractionated component thereof, for use in aquaculture.
    Type: Application
    Filed: February 18, 2011
    Publication date: June 20, 2013
    Applicant: Chemaphor Inc.
    Inventors: Larry Arthur Stobbs, James Gary Nickerson, Clayton Paul Dick
  • Publication number: 20130131032
    Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.
    Type: Application
    Filed: January 25, 2013
    Publication date: May 23, 2013
    Applicant: Revaax Pharmaceuticals, LLC
    Inventor: Revaax Pharmaceuticals, LLC
  • Publication number: 20130079319
    Abstract: A compound of the formula: wherein X is —N?, —CH?, or the like; W is —CH2— or the like; U is —S— or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; Q is a single bond or the like; R3 is hydrogen or the like; Ring A is a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; G is —C(?O)— or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: April 4, 2011
    Publication date: March 28, 2013
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Kenji Yamawaki, Hideki Sugimoto, Masayuki Sano
  • Publication number: 20130065818
    Abstract: The present invention discloses ophthalmic and otic compositions of facially amphiphilic antimicrobial polymers and oligomers and their uses, including their use in methods for treating and preventing ophthalmic infections and otic infections in humans and animals.
    Type: Application
    Filed: October 26, 2012
    Publication date: March 14, 2013
    Applicant: POLYMEDIX
    Inventor: PolyMedix
  • Publication number: 20130059774
    Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.
    Type: Application
    Filed: April 1, 2010
    Publication date: March 7, 2013
    Inventors: Mahesh Vithalbhai Patel, Sachin Subhash Bhagwat, Mohammad Alam Jafri
  • Publication number: 20130060208
    Abstract: The present invention relates to wound care products, devices and methods incorporating acetic acid for the treatment of bacterial infections, in particular bacterial biofilm infections. In particular it relates to a wound care product comprising acetic acid, wherein the product comprises at least one further antibacterial compound; a delivery system comprising a container connected to a means of delivery which is connected to a pad, wherein said container comprises a composition comprising acetic acid and said pad comprises a self-adhesive material; a kit comprising a dressing and an adhesive membrane, wherein the dressing comprises a composition comprising acetic acid; a method of treating a wound comprising a) applying acetic acid to the wound and b) applying a negative pressure to the wound.
    Type: Application
    Filed: December 21, 2010
    Publication date: March 7, 2013
    Applicants: RIGSHOSPITALET, COPENHAGEN UNIVERSITY HOSPITAL, BISPEBJERG HOSPITAL, DANMARKS TEKNISKE UNIVERSITET
    Inventors: Michael Christian Givskov, Thomas Bjarnsholt, Klaus Kirketerp-Møller
  • Publication number: 20120264727
    Abstract: The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
    Type: Application
    Filed: May 8, 2012
    Publication date: October 18, 2012
    Applicant: Legochem Biosciences, Inc.
    Inventors: Young Lag CHO, Hye Jin HEO, Kyu Man OH, Hyang Sook LEE, Chul Soon PARK, Sang Eun CHAE, Joung Yul YUN, Hyun Jin KWON, Young Jae YANG, Dae Hyuck KANG, Yong Zu KIM, Sung Ho WOO, Tae Kyo PARK
  • Publication number: 20120214781
    Abstract: The present invention relates to an antibacterial food composition comprising a Propolis extract and a Vaccinium macrocarpon cranberry extract.
    Type: Application
    Filed: April 1, 2010
    Publication date: August 23, 2012
    Inventor: Loïc Renard
  • Patent number: 8247400
    Abstract: The present invention relates to new cephem compounds useful for the treatment of bacterial infections of formula I: The invention also relates to methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and to methods of treatment using the compounds. The new cephem compounds are stable, exhibit good solubility, and are particularly well suited for, e.g., parenteral administration for the treatment of bacterial infections.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: August 21, 2012
    Inventors: Mahendra G. Dedhiya, Brahma N. Singh
  • 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: 20120122832
    Abstract: Disclosed is a process for the production of particles of a cefquinome acid addition salt, preferably cefquinome sulfate particles, by precipitation of cefquinome acid addition salt, preferably the sulfate, from a cefquinome betaine solution, wherein acid, preferably sulfuric acid, is added to the betaine solution. According to the invention the acid, preferably sulfuric acid, is added quickly in a single shot, in a molar excess of 40% to less than 100%. As a result, particles are formed that comprise agglomerates of microscale primary crystalline particles. This enables providing particles of cefquinome acid addition salt, preferably cefquinome sulfate, in particle sizes commensurate with micronized material, but with improved stability.
    Type: Application
    Filed: July 19, 2010
    Publication date: May 17, 2012
    Inventors: Hans Peter Niedermann, Heiko Bothe
  • Publication number: 20120071457
    Abstract: A new metallo-?-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of ?-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-?-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of ?-lactam antibiotics against metallo-?-lactamase producing bacteria by combining the compound of the general formula (I) with ?-lactam antibiotics.
    Type: Application
    Filed: November 29, 2011
    Publication date: March 22, 2012
    Inventors: Ken Chikauchi, Mizuyo Ida, Takao Abe, Yukiko Hiraiwa, Akihiro Morinaka, Toshiaki Kudo