6-position Substituent Contains Carbocyclic Ring Patents (Class 514/197)
  • Patent number: 9327053
    Abstract: A composition suitable for bone replacement is provided. The composition is a nanocomposite matrix, resembling both the structure and the properties of natural bone, including morphology, composition and mechanical characteristics. The nanocomposite is preferably porous and comprises: (1) micro or nano scale cellulose crystals or fibers; (2) hydroxyapatite nanoparticles; (3) Poly L-Lactide Acid or poly glycolic acid; and (4) a coupling agent, for example a surfactant, preferably an anionic surfactant such as sodium dodecyl sulfate. The composition is useful as an artificial bone replacement or bone graft, is preferably biomimetic, and can be suitable for use, for example, in trabecular bone substitution and osteoanagenesis applications. A method of fabrication of the nanocomposite is also provided.
    Type: Grant
    Filed: April 13, 2015
    Date of Patent: May 3, 2016
    Inventor: Samin Eftekhari
  • Patent number: 9226892
    Abstract: Novel drug carriers capable of targeted and/or pH dependent release of biologically active agents into selected pH environments including the gastrointestinal (GI), ophthalmic, urinary, or reproductive tracts. Unexpectedly, carriers including free fatty acids (FFA) are able to deliver biologically active agents to various pH environments. Such targeted delivery is tailorable and useful for active agents that are: (a) injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) acid labile, (c) impermeable/insoluble compounds in GI fluids, (d) susceptible to first pass metabolism, and/or (e) cause stomach irritation, upset, or dyspepsia.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: January 5, 2016
    Assignee: PLX PHARMA INC.
    Inventors: Upendra K. Marathi, Susann Edler Childress, Shaun L. Gammill, Robert W. Strozier
  • Publication number: 20150080361
    Abstract: The present invention relates to veterinary compositions in a form of an orally deliverable tablet, and more particularly to a controlled-release composition that provides sufficiently long duration to permit once daily administration.
    Type: Application
    Filed: August 6, 2014
    Publication date: March 19, 2015
    Inventors: Sunil Thomas Kumar Narishetty, Jeffrey Ellis Price, Sreenath Repakula
  • Publication number: 20150072957
    Abstract: This disclosure provides compositions containing solid forms of tazobactam arginine, and methods of manufacturing and using these compositions.
    Type: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Applicant: Calixa Therapeutics, Inc.
    Inventors: Jan-Ji Lai, Jian-Qiao Gu, Pradip M. Pathare, Valdas Jurkauskas, Joseph Terracciano, Nicole Miller Damour
  • Publication number: 20150044283
    Abstract: Single oral solid dosage form comprising an immediate release first dosage composition having at least two antibiotic agents and a delayed release second dosage composition having a proton pump inhibitor are provided herein. The single oral solid dosage form according to some aspects of the invention can be used for the treatment of disorders associated with infection by H. pylori or the prevention of recurrence of disorders associated with infection by H. pylori.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Reza Fathi, Gilead Raday, Guy Goldberg, Patrick Gosselin
  • Publication number: 20140356433
    Abstract: The present invention provides a pharmaceutical carrier and a drug structure using the carrier. The drug of the present invention comprises particular contents of chitosan, a negatively charged polymer, sodium tripolyphosphate, and an active ingredient, which combine with each other via electrostatic attraction. The drug structure has better release property and longer retention time; therefore overcomes the current drawbacks of the conventional treatment.
    Type: Application
    Filed: November 22, 2013
    Publication date: December 4, 2014
    Inventor: MING-JIUM SHIEH
  • Publication number: 20140286876
    Abstract: The present invention, as described above and as further defined by the claims, provides methods of administering an active agent via adhesion of a film to a mucous membrane in the oral cavity of a mammal, as well as and ODF formed therefore. An active agent may be ingested as the ODF dissolves resulting in systemic treatment of the mammal. In additional embodiments, an ODF may provide topical administration of an active agent.
    Type: Application
    Filed: March 28, 2014
    Publication date: September 25, 2014
    Inventor: Andrew L. Skigen
  • Publication number: 20140274925
    Abstract: Disclosed herein are compositions and methods for diagnosing, treating, and monitoring Lyme disease.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chenggang Jin, Gottfried H. Kellermann
  • Publication number: 20140212490
    Abstract: A pharmaceutical tablet comprising an immediate release portion containing an active ingredient and a delayed release portion, wherein the delayed release portion comprises an enteric-coated layer and within the enteric-coated layer there is at least one member selected from the group consisting of enteric-coated microparticle dosage forms containing an active ingredient and enteric-coated mini-tablet dosage forms containing an active ingredient, is disclosed.
    Type: Application
    Filed: March 28, 2014
    Publication date: July 31, 2014
    Applicant: SHIONOGI INC.
    Inventors: Bruce Cao, Sandra E. Wassink, Donald J. Treacy, JR., Beth A. Burnside, Colin E. Rowlings, John A. Bonck
  • Patent number: 8790695
    Abstract: A medicinal carrier is provided. The medicinal carrier comprises a first component, which is a biocompatible polymer with an amino group (—NH2); a saccharide; and a second component which is a biocompatible material. The saccharide grafts to the first component via the amino group (—NH2) of the first component, and the first component bonds to the second component via an ionic bond. The medicinal carrier can protect the medicine from gastric acid and swell or decompose to release the medicine under a specific pH condition, thus, showing a good applicability.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: July 29, 2014
    Assignee: China Medical University
    Inventor: Yu-Hsin Lin
  • Patent number: 8778924
    Abstract: An amoxicillin product comprising: at least one modified release component(s), wherein the at least one modified release component(s) comprises at least amoxicillin and a pharmaceutically acceptable carrier; and wherein when administered to a patient or subject in the fed state said amoxicillin product exhibits a pharmacokinetic profile for amoxicillin in the plasma characterized as follows: (1) the ratio of the portion of the AUC as measured from 2 hours post-administration to 5 hours post-administration to the portion of the AUC as measured from administration to 2 hours post-administration is at least 2.0:1; and (2) the ratio of the portion of the AUC as measured from 5 hours post-administration to 12 hours post-administration to the portion of the AUC as measured from administration to 2 hours post-administration is at least 1.1:1.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: July 15, 2014
    Assignee: Shionogi Inc.
    Inventors: Henry H. Flanner, Sanna Tolle-Sander, Donald Treacy, Beth A. Burnside, Susan P. Clausen
  • Patent number: 8754053
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 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: February 17, 2011
    Date of Patent: June 17, 2014
    Assignee: Syngenta Crop Protection LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Publication number: 20140128336
    Abstract: The present invention concerns products, such as compositions or medical devices, comprising one or more compounds of the Formula I, containing one or more free sulphhydryl groups, where R1 is hydrogen or an acetyl group, and R2 is a sulphhydryl group or a C1-C5 straight chained or branched hydrocarbon chain, optionally containing one or more heteroatoms selected from O, N and S, further containing one or more free sulphhydryl groups, for use in connection with Helicobacter pylori infections or other related infections, either as such or as combinations with antibiotics, whereby the compound(s) and optionally, when present, the antibiotic(s), are mixed with one or more pharmaceutically acceptable carriers providing sustained local release in the stomach or elsewhere in the upper aerodigestive tract.
    Type: Application
    Filed: April 18, 2012
    Publication date: May 8, 2014
    Applicant: BIOHIT OYJ
    Inventors: Matti Härkönen, Tuuli Marvola, Mikko Salaspuro, Osmo Suovaniemi
  • Publication number: 20140099371
    Abstract: A medicinal carrier is provided. The medicinal carrier comprises a first component, which is a biocompatible polymer with an amino group (—NH2); a saccharide; and a second component which is a biocompatible material. The saccharide grafts to the first component via the amino group (—NH2) of the first component, and the first component bonds to the second component via an ionic bond. The medicinal carrier can protect the medicine from gastric acid and swell or decompose to release the medicine under a specific pH condition, thus, showing a good applicability.
    Type: Application
    Filed: November 27, 2012
    Publication date: April 10, 2014
    Applicant: CHINA MEDICAL UNIVERSITY
    Inventor: Yu-Hsin LIN
  • Publication number: 20140080775
    Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject at least one compound selected from the group consisting of those set forth in Table 1, Table 2, Table 3, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.
    Type: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicants: UNIVERSITY OF WASHINGTON, The General Hospital Corporation, MASSACHUSETTS INSTITUTE OF TECHNOLOGY
    Inventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
  • Publication number: 20140073591
    Abstract: Multidrug resistance reversers of the d-tetrandrine family are used in conjunction with penicillins and other principle drugs used to treat MRSA.
    Type: Application
    Filed: September 12, 2013
    Publication date: March 13, 2014
    Applicant: CBA Pharma, Inc.
    Inventors: Wayne Michael Putnam, Beth D. Gudeman
  • Publication number: 20140018323
    Abstract: A composition which comprises a biologically active agent and a polymer that exhibits a reverse thermal gelation at a physiological temperature, in a carrier, and in which the active agent is in an undissolved form is disclosed herein. Further disclosed herein are methods utilizing the compositions for treating subjects, including non-human subjects, as well as kits for preparing and using a composition. The composition is preferably a sustained release formulation, and is particularly useful for treating animals, where single-dose treatment is desired.
    Type: Application
    Filed: March 28, 2012
    Publication date: January 16, 2014
    Inventors: Michael Friedman, Amnon Hoffman, Eran Lavy
  • Publication number: 20130338130
    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: August 19, 2013
    Publication date: December 19, 2013
    Applicant: Biogenic Innovations, LLC
    Inventors: Rodney Benjamin, Anthony L. Keller, Jeffrey Varelman
  • Publication number: 20130281424
    Abstract: An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against P. aeruginosa. The conjugates appear to be assimilated by an induced bacterial iron transport process as their activities were inversely related to iron concentration. The easily synthesized tris-catecolate siderophores can be used with a variety of drugs as conjugates to target antibiotic-resistant Gram-negative bacteria.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Applicant: University of Notre Dame Du Lac
    Inventors: Marvin J. MILLER, Cheng JI, Patricia A. MILLER
  • Publication number: 20130281359
    Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; and R1 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Inventors: Samarendra N. MAITI, Dai Nguyen, Jehangir Khan, Rong Ling
  • Patent number: 8546373
    Abstract: Embodiments of the invention relate generally to formulations comprising methylsulfonylmethane (MSM) and one or more therapeutic agents, and uses of such formulations to treat, inhibit and/or sensitize infectious diseases. In several embodiments, such formulations are effective to treat, inhibit and/or sensitize drug-resistant bacterial microorganisms, for example, methicillin-resistant Staphylococcus aureus (MRSA).
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: October 1, 2013
    Assignee: Biogenic Innovations, LLC
    Inventors: Rodney L. Benjamin, Anthony L. Keller, Jeffrey Varelman
  • Publication number: 20130224258
    Abstract: Compositions and methods, including novel homogeneous microparticulate suspensions, are described for treating natural and artificial surfaces that contain bacterial biofilm, including unexpected synergy or enhancing effects between bismuth-thiol (BT) compounds and certain antibiotics, to provide formulations including antiseptic formulations. 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 certain gram-positive bacterial infections, and distinct preferential efficacies of certain such compositions for treating certain gram-negative bacterial infections.
    Type: Application
    Filed: February 12, 2013
    Publication date: August 29, 2013
    Applicant: MICROBION CORPORATION
    Inventor: Microbion Corporation
  • Publication number: 20130225412
    Abstract: The various embodiments herein provide a nano silicon carrier as a drug delivery mechanism. The nano silicon carrier comprises a diatom frustules loaded with a drug molecule to be released at the target site. The diatom frustules are of Hannaea arcus and Navicula inflexa species of diatom. The pore size of the diatom frustules is 1 to 100 nm. The diatom frustules are comb-like in structure. The diatom frustules are in the form of powdered diatomaceous earth. The drug delivery mechanism described in the embodiments herein is a controlled release mechanism. The nano silicon carrier described in the embodiments herein is also used for delivery of pesticides and herbicides in plants. The nano silicon carrier described in the embodiments herein is also used in hormone waste water treatment.
    Type: Application
    Filed: February 28, 2012
    Publication date: August 29, 2013
    Inventors: Soroush Sardari Lodriche, Saeed Soltani, Roghieh Mirzazadeh
  • Publication number: 20130216609
    Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
    Type: Application
    Filed: March 21, 2013
    Publication date: August 22, 2013
    Applicants: The Regents of the University of California, Otonomy, Inc.
    Inventors: Otonomy, Inc., The Regents of the University of California
  • Publication number: 20130210705
    Abstract: It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide (“AMP”) and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 15, 2013
    Applicant: METALLOPHARM LLC
    Inventor: Metallopharm LLC
  • Publication number: 20130184230
    Abstract: This invention relates to the use of 4-methyl-8-phenoxy-1-(2-phenylethyl)-2,3-dihydro-1H-pyrrolo[3,2-c]quinoline or a pharmaceutically acceptable derivative thereof in combination with another antimicrobial agent selected from the group consisting of a beta-lactam antimicrobial agent, mupirocin and chlorhexidine or a pharmaceutically acceptable derivative thereof, for the prevention and/or treatment of microbial infections.
    Type: Application
    Filed: August 5, 2011
    Publication date: July 18, 2013
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Yanmin Hu, Anthony R.M. Coates
  • Publication number: 20130172298
    Abstract: The present invention provides compositions, methods of manufacture, process and uses for diagnosing, preventing, inhibiting, and treating the development and proliferation of diseases and disorders associated with Okadaella gastrococcus (Og) bacterial infection in a patient.
    Type: Application
    Filed: December 23, 2010
    Publication date: July 4, 2013
    Inventor: Takayuki Okada
  • 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: 20130136697
    Abstract: The invention discloses injectable hydrogels which are in the form of crosslinked nano beads or particle in the size range 5 nm to 10 ?m, comprising PAMAM dendrimer with asymmetrical peripheral end groups such that one of the terminal groups is involved in formation of hydrogel and the other in involved in the conjugation of drugs or imaging agents and their methods of preparation. The said gel is formed by reaction of the PAMAM dendrimer with asymmetrical end groups with other polymer wherein the other polymer is selected from the group of linear, branched, hyperbranched or star shaped polymers with functionalized terminal groups. The PAMAM dendrimer with asymmetrical terminal groups consists of a Generation 2 and above PAMAM dendrimer with symmetrical end groups modified using the amino acids or their modified forms.
    Type: Application
    Filed: March 31, 2011
    Publication date: May 30, 2013
    Applicants: NATIONAL INSTITUTES OF HEALTH, WAYNE STATE UNIVERSITY
    Inventors: Rangaramanujam M. Kannan, Sujatha Kannan, Roberto Romero, Raghavendra Navath, Anupa Menjoge
  • Publication number: 20130131033
    Abstract: The present invention relates to a pharmaceutical composition comprising ciprofloxacin or salts of thereof and amoxycillin or salts of thereof and other pharmaceutical excipients. The present invention provides more reliable effect against all bacteria, including the most commonly causative streptococci, responsible for especially respiratory tract infections. The invention makes up for the weakness of ciprofloxacin against streptococci.
    Type: Application
    Filed: January 6, 2011
    Publication date: May 23, 2013
    Applicant: TOYOCHEM LABORATORIES
    Inventor: Mayank Jasvantbhai Shah
  • Publication number: 20130116210
    Abstract: Disclosed herein are compositions and methods for the treatment of otic diseases or conditions with antimicrobial agent compositions and formulations administered locally to an individual afflicted with an otic disease or condition, through direct application of these compositions and formulations onto or via perfusion into the targeted auris structure(s).
    Type: Application
    Filed: October 4, 2012
    Publication date: May 9, 2013
    Applicants: OTONOMY, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: The Regents of the University of California, Otonomy, Inc.
  • Patent number: 8415339
    Abstract: Pharmaceutical compositions containing a carbapenem of the structural formula I and epicillin are strongly bactericidal against MRSA and MRSE. Equivalently, compositions of conventional carbapenem antibiotics and epicillin are highly synergistic in eradicating said bacteria.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: April 9, 2013
    Inventor: Hans Rudolf Pfaendler
  • Publication number: 20130053336
    Abstract: The invention relates to a method for treating infections of bacteria of the Chlamydiaceae family using a ?-lactam. The invention also relates to a method for treating diseases caused by an infection of bacteria of the Chlamydiaceae family using a ?-lactam.
    Type: Application
    Filed: January 13, 2011
    Publication date: February 28, 2013
    Inventors: Philippe Verbeke, Maud Dumoux, Colette Kanellopoulos
  • Publication number: 20130018029
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: July 16, 2012
    Publication date: January 17, 2013
    Inventor: Chongxi YU
  • Publication number: 20120329760
    Abstract: Methods of identifying a subject having a urinary tract infection using RNase 7 are described. The methods include providing a test sample of urine from the subject, determining the level of RNase 7 in the test sample, and then comparing the level of RNase 7 in the test sample to the level of RNase 7 in a control. A higher level of RNase 7 in the test sample indicates that the subject has an acute urinary tract infection, whereas a lower level of RNase 7 in the test sample indicates that the subject only has a chronic urinary tract infection.
    Type: Application
    Filed: April 19, 2012
    Publication date: December 27, 2012
    Applicant: NATIONWIDE CHILDREN'S HOSPITAL, INC.
    Inventors: David Hains, Andrew Lawrence Schwaderer, John David Spenser
  • Publication number: 20120321706
    Abstract: Disclosed is a multi-layered gastroretentive dosage form for the controlled release of a poorly soluble drug or diagnostic in the stomach and gastrointestinal tract of a patient, folded into a capsule which disintegrates rapidly and the said multi-layered dosage form unfolds rapidly upon contact with the gastric juice. The mechanisms of the gastric retention are not dependent on and do not influence the materials and methods used in controlling the release of the said poorly soluble drug.
    Type: Application
    Filed: October 19, 2010
    Publication date: December 20, 2012
    Applicant: INTEC PHARMA LTD.
    Inventors: Suher Masri, Eytan Moor, David Kirmayer, Elena Kluev, Giora Carni, Nadav Navon
  • Publication number: 20120322782
    Abstract: The present invention relates to veterinary compositions in a form of an orally deliverable tablet, and more particularly to a controlled-release composition that provides sufficiently long duration to permit once daily administration.
    Type: Application
    Filed: February 15, 2011
    Publication date: December 20, 2012
    Inventors: Sunil Thomas Kumar Narishetty, Jeffrey Ellis Price, Sreenath Repakula
  • Publication number: 20120316124
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 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: February 17, 2011
    Publication date: December 13, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Publication number: 20120289471
    Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
    Type: Application
    Filed: April 18, 2012
    Publication date: November 15, 2012
    Applicant: SIGNATURE R&D HOLDINGS, LLC
    Inventor: V. Ravi Chandran
  • Patent number: 8299052
    Abstract: A process for treating a bacterial infection with an antibiotic, comprising: administering to a patient with a bacterial infection a product that includes a modified release dosage form containing an antibiotic, said product being administered once-a-day in a dosage and for a number of days that provides a Total T>MIC sufficient to achieve at least the minimum amount of bacterial eradication for treatment of said bacterial infection.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: October 30, 2012
    Assignee: Shionogi Inc.
    Inventors: Henry H. Flanner, Robert Guttendorf, Donald Treacy, Susan P. Clausen, Beth A. Burnside
  • Publication number: 20120264726
    Abstract: Embodiments of the invention relate generally to formulations comprising methylsulfonylmethane (MSM) and one or more therapeutic agents, and uses of such formulations to treat, inhibit and/or sensitize infectious diseases. In several embodiments, such formulations are effective to treat, inhibit and/or sensitize drug-resistant bacterial microorganisms, for example, methicillin-resistant Staphylococcus aureus (MRSA).
    Type: Application
    Filed: April 27, 2012
    Publication date: October 18, 2012
    Inventors: Rodney L. Benjamin, Anthony L. Keller, Jeffrey Varelman
  • Publication number: 20120231995
    Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.
    Type: Application
    Filed: May 17, 2012
    Publication date: September 13, 2012
    Applicant: HELPERBY THERAPEUTICS LIMITED
    Inventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
  • Publication number: 20120213825
    Abstract: An antibiotic product is comprised of at least three dosages forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours after the initial release of antibiotic. In one embodiment, there is a delayed release dosage form, as well as two or more delayed sustained release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.
    Type: Application
    Filed: October 18, 2011
    Publication date: August 23, 2012
    Inventors: Beth A. Burnside, Henry H. Flanner, Colin Rowlings
  • Patent number: 8232322
    Abstract: Anhydride polymers that release active or activatable agent(s) have pre-selected properties such as molecular weight, flexibility, hardness, adhesiveness, and other valuable properties. The polymers are suitable for use in compositions, formulations, coatings, devices, and the like that benefit from the controlled release of an agent(s) over a period of time. The polymers are prepared by a process involving various alternative and sequential steps that allow the design a priori of products with specific characteristics. The polymers are suitable as delivery systems, either by themselves, as compositions, formulations or devices.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 31, 2012
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Anthony East, Alan Letton, Suseela Kanamathareddy, Bryant J. Pudil, Stephen Goodrich, Michael B. Hicks, Yun Choe
  • Publication number: 20120157373
    Abstract: Antimicrobial compounds, such as silanol or alcohol, include a protecting or leaving group that can protect the compound from degradation during the process of preparing a medical device containing the compound or reduce the volatility of the compound relative to its counterpart without the leaving group. Nearly any hydrolysable leaving group may be employed. The leaving group may be an agent that may serve a therapeutic function in addition to protecting or retaining the antimicrobial agents.
    Type: Application
    Filed: February 29, 2012
    Publication date: June 21, 2012
    Applicant: MEDTRONIC, INC.
    Inventors: Paul Hsien-Fu Wu, Catherine E. Taylor, Linnus Cheruiyot, Jianwei Li, Terese A. Bartlett, Matt Bergan
  • Publication number: 20120157371
    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 HPCs/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 HPCs/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: December 12, 2011
    Publication date: June 21, 2012
    Inventors: Chongxi YU, Lina Xu, Yuhua Chen, Binbing Yan, Shiqian Tu
  • Publication number: 20120157397
    Abstract: The present invention provides markers and methods for determining whether a subject, particularly a human subject, has or is at risk of developing, a disease such as cardiovascular disease, diabetes mellitus, insulin resistance, metabolic syndrome, NAFLD (Nonalcoholic Fatty Liver Disease) or NASH (Nonalcoholic Steatohepatitis) (e.g., within the ensuing year, two years, and/or three years). The present application also relates to the use of such markers and methods for monitoring the status of such diseases in a subject or the effects of therapeutic agents on subjects with such diseases.
    Type: Application
    Filed: November 28, 2011
    Publication date: June 21, 2012
    Inventors: Stanley L. Hazen, Zeneng Wang, Bruce S. Levison
  • Publication number: 20120141574
    Abstract: A palatable, edible soft chewable medication vehicle for delivery of a pharmaceutically acceptable active ingredient, such as a drug, to an animal or human subject. The edible soft chews contain only food grade or better inactive ingredients, and preferably do not contain ingredients of animal origin. Processes for manufacturing the edible soft chews do not require the use of heat or the addition of water during mixing of active and inactive ingredients, provide stable concentrations of the active ingredient, and produce chews of consistent weight and texture.
    Type: Application
    Filed: February 14, 2012
    Publication date: June 7, 2012
    Inventors: Neil E. Paulsen, Roland Johnson, Michael Coffee
  • Publication number: 20120134955
    Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.
    Type: Application
    Filed: February 18, 2010
    Publication date: May 31, 2012
    Inventors: Yasuhiro Goto, Kenji Niyama, Satoshi Sunami, Keiji Takahashi
  • Publication number: 20120115835
    Abstract: The peptidoglycan layer is a vital component of the bacterial cell wall, which comprises 4?3 and 3?3 transpeptide cross-linkages, the formation of which are catalyzed by D,D- and L,D-transpeptidases, respectively. Methods for the treatment of bacterial infections with agents that inhibit L,D-transpeptidases, either alone or in combination with D,D-transpeptidase inhibitors, are provided herein. Also provided are methods for the treatment of chronic stage tuberculosis with agents that inhibit enzyme with L,D-transpeptidase activity.
    Type: Application
    Filed: October 27, 2011
    Publication date: May 10, 2012
    Applicants: CENTRE DE RECHERCHE DES CORDELIERS, THE JOHNS HOPKINS UNIVERSITY
    Inventors: Gyanu Lamichhane, William R. Bishai, Radhika Gupta, Marie Lavollay, Jean-Luc Mainardi, Michel Arthur