2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
  • Publication number: 20140213540
    Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
    Type: Application
    Filed: March 20, 2014
    Publication date: July 31, 2014
    Applicants: IDENIX PHARMACEUTICALS, INC., L'UNIVERSITE MONTPELLIER II, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITA DEGLI STUDI DI CAGLIARI
    Inventors: Richard STORER, Gilles GOSSELIN, Jean-Pierre SOMMADOSSI, Paolo LACOLLA
  • Patent number: 8791089
    Abstract: The invention provides a method for supporting operational activities in daily living by providing a combination of (a) long-chain polyunsaturated fatty acids, particularly DHA and/or EPA, and (b) nucleosides or nucleotides, particularly uridine or its equivalent. The operational activities comprise eating; walking; toileting; bathing; grooming; dressing; use of communication equipment; making conversations; keeping appointments; use of household appliances; cleaning dishes; preparation of meal or drink; writing; reading; independent housekeeping; transportation and shopping.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: July 29, 2014
    Assignee: N.V. Nutricia
    Inventors: Martine Groenendijk, Mattheus Cornelis de Wilde, Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Publication number: 20140206635
    Abstract: A metal-salen complex compound, which exhibits excellent noninvasiveness and can be efficiently transferred to an affected site, a local anesthetic containing this metal-salen complex compound, and an antineoplastic drug containing this metal-salen complex compound are provided. Regarding the metal-salen complex compound, a metal atom part in each of two molecules of a metal-salen complex or a derivative of the metal-salen complex is dimerized via water, and the metal-salen complex compound is mixed with a base to produce an ointment.
    Type: Application
    Filed: May 10, 2012
    Publication date: July 24, 2014
    Applicants: IHI CORPORATION
    Inventors: Yoshihiro Ishikawa, Haruki Eguchi
  • Publication number: 20140205567
    Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 24, 2014
    Applicant: AB Pharma Ltd.
    Inventor: Zheng-yun James Zhan
  • Publication number: 20140206640
    Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140206639
    Abstract: The present invention provides pharmaceutical compositions comprising a dihydro base described herein (e.g., compound DHdC). The dihydro base may show multiple tautomerism and may increase mutation of an RNA and/or DNA of a virus or cancer cell. The dihydro base may be used to reduce DNA methylation (e.g., in a cancer cell). The present invention also provides kits including the inventive pharmaceutical compositions and methods of treating a viral infection (e.g., influenza, HIV infection, or hepatitis C) or cancer using the pharmaceutical compositions or kits.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 24, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: John M. Essigmann, Deyu Li, Katherine J. Silvestre
  • Publication number: 20140200516
    Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II; aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: ABBOTT LABORATORIES
    Inventor: Harry A. DUGGER, III
  • Publication number: 20140199265
    Abstract: The present disclosure relates to nutritional compositions comprising a neurologic component, wherein, the neurologic component may promote brain and nervous system development and further provide neurological protection and repair. The neurologic component may include phosphatidylethanolamine, sphingomyelin, cytidine diphosphate-choline, ceramide, uridine, at least one ganglioside, and mixtures thereof. The disclosure further relates to methods of promoting brain and nervous system health by providing said nutritional compositions to target subjects, which includes pediatric subjects.
    Type: Application
    Filed: January 11, 2013
    Publication date: July 17, 2014
    Applicant: Mead Johnson Nutrition Company
    Inventors: Chenzhong Kuang, Yan Xiao, Eduard Poels, Zeina Jouni, Dirk Hondmann
  • Publication number: 20140187510
    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 a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.
    Type: Application
    Filed: July 11, 2013
    Publication date: July 3, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATION
    Inventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
  • Patent number: 8765712
    Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventor: Peter Mayser
  • Patent number: 8765713
    Abstract: A marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker, wherein the marker for determining sensitivity to an anti-cancer agent is a protein or a fragment, where in the protein or a fragment thereof exhibits a peak at m/z of 5,300 to 5,400, a peak at m/z of 6,130 to 6,230, a peak at m/z of 7,000 to 7,080 a peak at m/z of 7,840 to 7,920, a peak at m/z of 8,920 to 9,000, a peak at m/z of 12,440 to 12,560, a peak at m/z of 17,100 to 17,270, a peak at m/z of 18,290 to 18,470, a peak at m/z of 24,660 to 24,750, a peak at m/z of 35,980 to 36,290, a peak at m/z of 8,650 to 8,750, a peak at m/z of 9,100 to 9,200, a peak at m/z of 11,760 to 11,890, the peaks being determined by means of a mass spectrometer.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: July 1, 2014
    Assignees: Keio University, Kabushiki Kaisha Yakult Honsha
    Inventors: Yusuke Tanigawara, Sayo Suzuki, Yusuke Ikoma, Akito Nishimuta, Tetsuya Suzuki, Shinji Sugimoto
  • Publication number: 20140179627
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
  • Publication number: 20140178337
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Patent number: 8759319
    Abstract: The invention pertains to the use of a lipid fraction for the support of brain function. The lipid fraction comprises the medium-chain fatty acids at least 4 g hexanoic acid and/or at least 5 g octanoic acid, at least 1 g eicosapentaenoic acid, and in addition more than 0.4 g ?-linolenic acid per 100 g fatty acids of the lipid fraction.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: June 24, 2014
    Assignee: N.V. Nutricia
    Inventors: Robert Johan Joseph Hageman, Eline Marleen Van Der Beek, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Publication number: 20140170157
    Abstract: Methods of treatment for Crohn's disease and multiple sclerosis are disclosed. Also disclosed are methods for repositioning a pharmaceutical by selecting at least one target gene, gene product, or loci associated with the treatment of at least one first disease, trait, or phenotype by the pharmaceutical, identifying at least one second disease, trait, or phenotype associated with the least one target gene, gene product, or loci using genome-wide associated studies, and selecting at least one identified second disease, trait and/or phenotype based on step for treatment with the pharmaceutical.
    Type: Application
    Filed: June 15, 2012
    Publication date: June 19, 2014
    Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
    Inventors: Pankaj Agarwal, Lon R. Cardon, Vincent Eugene Mooser, Philippe Sanseau
  • Publication number: 20140170112
    Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.
    Type: Application
    Filed: March 8, 2012
    Publication date: June 19, 2014
    Applicant: VICUS THERAPEUTICS, LLC
    Inventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
  • Publication number: 20140154211
    Abstract: The present invention relates to 2?-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Substituted Nucleoside Derivative, and methods of using the 2?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: June 5, 2014
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Vishal Verma, Frank Bennett, Angela Kereles, Ashok Arasappan, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Patent number: 8735372
    Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: May 27, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20140128339
    Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 8, 2014
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
  • Publication number: 20140128338
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 8, 2014
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
  • Patent number: 8716346
    Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: May 6, 2014
    Assignee: Case Western Reserve University
    Inventors: Stanton Gerson, Lili Liu
  • Publication number: 20140107062
    Abstract: The present invention provides compositions and methods for treating or preventing diseases associated with vascular and non-vascular body passageways, the method comprising the step of delivering to a body passageway a therapeutic agent delivered locally through a polymer matrix from an implanted stent or other structure.
    Type: Application
    Filed: December 18, 2013
    Publication date: April 17, 2014
    Applicant: ARAVASC INC.
    Inventor: Narmada Shenoy
  • Publication number: 20140100188
    Abstract: The present disclosure relates to an immune signature of tumor infiltrating leukocytes. In particular, the disclosure provides methods and kits for determining the immune signature of tumor infiltrating leukocytes for use in assessing risk of cancer recurrence and long term survival, and for developing a treatment regimen for a cancer patient.
    Type: Application
    Filed: October 2, 2013
    Publication date: April 10, 2014
    Applicants: University College Dublin, The Regents of the University of California
    Inventors: Lisa M. COUSSENS, David G. DENARDO, Donal J. BRENNAN
  • Patent number: 8691789
    Abstract: A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [123I]-IaraU is disclosed. Commercial available uridine is used as the raw material for the synthesis of the precursor. A radioactive iodine-123 is marked on an alkaline group of uridine to obtain [123I]-IaraU, which is distinguishable from [18F]-FLT marking 18F on a glycosyl group to obtain a novel tumor radiation probe. The marking procedures include mixing the marker precursor with Na [123I] solution, acetic acid and hydrogen peroxide solution, and the solution of chloroform and sodium hydroxide. The sonication time increases from 1 minute to 10 minutes, so that [123I]-IaraU has radiologically chemical purity of higher than 98% and radiological specific activity of not less than 0.196 GBq/umole, and the yield can increase from 8% to 40%. Its radioactive specific activity, yield and purity reach to the degree for the use in biological experiments, while reducing production cost.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: April 8, 2014
    Assignee: Institute of Nuclear Energy Research, Atomic Energy Council
    Inventors: Jenn-Tzong Chen, Ho-Lien Huang, Jia-Rong Chen, Chung-Shan Yu, Wen-Chin Su, Ching-Shiuann Yang, Wuu-Jyh Lin
  • Patent number: 8691788
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: April 8, 2014
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, Universite Montpellier II
    Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Publication number: 20140080784
    Abstract: The present invention relates to a pharmaceutical or dietary composition comprising deoxyuridine and a pharmaceutically or dietetically suitable carrier. Another aspect of the present invention relates to a method of supplementing the dietary needs of a subject. This method includes administering to the subject a dietary supplementing effective amount of deoxyuridine. Yet another aspect of the present invention relates to a method of treating cancer in a subject. This method includes selecting a subject having cancer and administering to the selected subject a therapeutically effective amount of uridine, thereby treating the cancer in the selected subject.
    Type: Application
    Filed: April 25, 2012
    Publication date: March 20, 2014
    Applicant: CORNELL UNIVERSITY
    Inventors: Patrick J. Stover, Martha S. Field
  • Publication number: 20140080769
    Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Applicants: The Chancellor, Masters and Scholars of the University of Oxford, The Government of the United States of America, as represented by the Secretary, Department of Healt
    Inventors: Frances Mary Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
  • Patent number: 8664181
    Abstract: A prodrug comprising at least two different pharmaceutically and/or diagnostically active compounds independently bound by cleavable linkers and a protein-binding moiety which is capable of binding to carrier a molecule is described.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: March 4, 2014
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: Felix Kratz, Irmgard Merfort
  • Publication number: 20140057863
    Abstract: The disclosed invention is a composition for and a method of treating a Flaviviridae (including BVDV and HCV), Orthomyxoviridae (including Influenza A and B) or Paramyxoviridae (including RSV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans, using a nucleoside of general formula (I)-(XXIII) or its pharmaceutically acceptable salt or prodrug. This invention also provides an effective process to quantify the viral load, and in particular BVDV, HCV or West Nile Virus load, in a host, using real-time polymerase chain reaction (“RT-PCR”). Additionally, the invention discloses probe molecules that can fluoresce proportionally to the amount of virus present in a sample.
    Type: Application
    Filed: June 3, 2013
    Publication date: February 27, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Lieven Stuyver, Kyoichi Watanabe
  • Patent number: 8658619
    Abstract: Provided are methods of treating subclinical sun damage and of inducing a chemocytotoxic response in skin. Methods of treating subclinical sun damage include the steps of: topically administering to skin of a patient a composition comprising a chemocytotoxic agent in an amount effective to induce erythema, scaling, crusting, or combinations thereof and resolve at least a portion of the subclinical sun damage, where the skin has a condition of no clinical sign of sun damage and the patient was not previously treated for actinic keratosis or nonmelanoma skin cancer. The chemocytotoxic agent can comprise a fluorinated pyrimidine antimetabolite such as 5-fluorouracil (FU), 5-fluorouridine (FUR), 5-fluorouridine-5?-monophosphate (FUMP), 5-fluorodeoxyuridine (FUdR), 5-fluorodeoxyuridine-5?-monophosphate (FdUMP), or combinations thereof.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: February 25, 2014
    Inventor: Robert K. Ilowite
  • Patent number: 8658618
    Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU generated from a prodrug is in substantial excess of DPD inhibitor in the patient.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: February 25, 2014
    Assignee: Adherex Technologies, Inc.
    Inventor: Thomas Spector
  • Publication number: 20140045915
    Abstract: Disclosed herein are methods for assaying a biological sample from a subject by analyzing components of microvesicle fractions in aid of risk, diagnosis, prognosis or monitoring of or directing treatment of the subject for, a disease or other medical condition in the subject. Also disclosed are methods of treatment and identifying biomarkers using a microvesicle fraction of a subject. Kits, pharmaceutical compositions, and profiles related to the methods are also disclosed.
    Type: Application
    Filed: August 31, 2011
    Publication date: February 13, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Johan Karl Olov Skog, Leonora Balaj, Mikkel Noerholm, Xandra O. Breakefield
  • Patent number: 8648054
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: April 12, 2013
    Date of Patent: February 11, 2014
    Assignee: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Publication number: 20140023642
    Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones thereof, represented by the Formula (I) wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.
    Type: Application
    Filed: March 31, 2012
    Publication date: January 23, 2014
    Applicant: Impact Therapeutics, Inc.
    Inventors: Sui Xiong Cai, Ye Edward Tian, Haijun Dong, Qingbing Xu, Lizhen Wu, Lijun Liu, Yangzhen Jiang, Qingli Bao, Guoxiang Wang, Feng Yin, Chengyun Gu, Xiuhua Hu, Xiaozhu Wang, Sishun Kang, Shengzhi Chen
  • Publication number: 20140005136
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 2, 2014
    Applicant: Ardea Biosciences, Inc.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Patent number: 8618075
    Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: December 31, 2013
    Assignee: Eisai Inc.
    Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
  • Patent number: 8609677
    Abstract: This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration.
    Type: Grant
    Filed: March 31, 2013
    Date of Patent: December 17, 2013
    Assignee: Yagna Limited
    Inventor: Giuseppe Trigiante
  • Patent number: 8609066
    Abstract: The present invention relates to methods for determining whether blood flow is restricted in a blood vessel of an individual suspected of compromised blood flow in the vessel, the method comprising the steps of delivering UTP, a derivative thereof, or a salt thereof to the vessel, assessing blood flow quantitatively in the vessel by obtaining a value that correlates to blood flow in said vessel, comparing the obtained value with a reference value, and determining whether the individual has compromised blood flow based on the results of the comparison. The invention also provides for methods of diagnosing atherosclerotic and ischemic heart diseases using UTP, a derivative thereof, or a salt thereof, as well as methods for inducing maximal hyperemia for diagnostic purposes.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: December 17, 2013
    Inventor: Jaya Brigitte Rosenmeier
  • Patent number: 8609623
    Abstract: Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: December 17, 2013
    Assignee: ALT Solutions Inc.
    Inventor: Igor E. Bondarev
  • Patent number: 8609628
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Grant
    Filed: January 23, 2012
    Date of Patent: December 17, 2013
    Assignee: University of North Carolina at Wilmington
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Publication number: 20130330297
    Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.
    Type: Application
    Filed: August 2, 2013
    Publication date: December 12, 2013
    Applicants: Idenix Pharmaceuticals, Inc., L'Universite Montpellier II (UMII), Centre National De La Recherche Scientifique (CNRS), Universita degli Studi di Cagliari
    Inventors: Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi, Paolo LaColla
  • Patent number: 8604000
    Abstract: The present invention relates to the use of a taste masking agent selected from the group of cellulose; starch; xanthan gum; gellan gum; alginate; galactomannans such as fenugreek, guar gum, tara gum, locust bean gum, and cassia gum; gum karaya; gum tragacanth; carrageenan; and mixture thereof, for improving one or more of mouth feel, taste, aftertaste and smell of a liquid aqueous nutritional composition comprising a nucleotide and/or a nucleoside. It also relates to a nutritional composition comprising an unsavory nucleotide and/or a nucleoside component, having improved sensory characteristics such as improved mouth feel, taste, aftertaste and smell. In particular, it relates to a composition comprising said un-savory nucleotide and/or a nucleoside component, in particular comprising an uridine-containing nucleotide and/or a nucleoside in combination with an unsavory edible oil, such as a fish oil.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: December 10, 2013
    Assignee: N.V. Nutricia
    Inventors: Esther Jacqueline de Kort, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Publication number: 20130324491
    Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
    Type: Application
    Filed: March 22, 2013
    Publication date: December 5, 2013
    Applicants: Idenix Pharmaceuticals, Inc., L'Universite Montpellier II, Centre National de la Recherche Scientifique
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
  • Publication number: 20130315863
    Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Application
    Filed: July 31, 2013
    Publication date: November 28, 2013
    Applicants: Universita' degli Studi di Cagliari, Idenix Pharmaceuticals, Inc.
    Inventors: Jean-Pierre SOMMADOSSI, Paolo LaColla
  • Publication number: 20130315862
    Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Application
    Filed: July 29, 2013
    Publication date: November 28, 2013
    Applicants: Universita' degli Studi di Cagliari, Idenix Pharmaceuticals, Inc.
    Inventors: Jean-Pierre Sommadossi, Paolo LaColla
  • Publication number: 20130310335
    Abstract: The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar.
    Type: Application
    Filed: July 26, 2013
    Publication date: November 21, 2013
    Applicant: BioAlliance Pharma, S.A.
    Inventors: Jean-Marc AIACHE, Dominique COSTANTINI, Christine CHAUMONT
  • Publication number: 20130310336
    Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Application
    Filed: November 13, 2012
    Publication date: November 21, 2013
    Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.
    Inventors: Jean-Pierre SOMMADOSSI, Paolo LACOLLA
  • Publication number: 20130303479
    Abstract: ASPECTS OF EMBODIMENTS RELATE TO methods of treating human immunodeficiency virus (HIV) infection. Further aspects of embodiments also relate to constellations of compositions for treating HIV infection. Still additional aspects of embodiments relate to a many methods of making compositions useful in the treatment of HIV infection.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 14, 2013
    Inventors: Todd William Hawley, Yuntao Wu, Jia Guo
  • Publication number: 20130303473
    Abstract: The invention provides pharmaceutical compositions based on liquid vehicles whose density is substantially higher than that of aqueous physiological fluids. The compositions are useful as medicines in ophthalmology, in particular for the treatment of conditions affecting the posterior segment of an eye. They may be administered topically into the eye or in a minimally invasive manner by periocular injection. Preferred liquid carriers are selected from semifluorinated alkanes.
    Type: Application
    Filed: November 10, 2011
    Publication date: November 14, 2013
    Applicant: NOVALIQ GmbH
    Inventor: Clive G. Wilson
  • Patent number: 8580765
    Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: November 12, 2013
    Assignee: Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du, Peiyuan Wang, Dhanapalan Nagarathnam