2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
  • Patent number: 10214553
    Abstract: The present disclosure encompasses solid state forms of Sofosbuvir, processes for their production, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: February 26, 2019
    Assignees: TEVA PHARMACEUTICALS INTERNATIONAL GMBH, RATIOPHARM GMBH
    Inventors: Wolfgang Albrecht, Judith Aronhime, Brijnath P. Chaurasia, Jens Geier, Richard Guserle, Julia Hrakovsky, Claudia Lauer, Ramkaran Prajapati, Vinod K. Kansal, Pavan V. Kumar, Hans-Juergen Mika, Siva Rama Krishna Muppalla, Marina Ratkaj, Roman Safonov, Dirk Schenk, Naveen C. Srivastav, Ralph Stefan, Ashish Tripathi
  • Patent number: 10175256
    Abstract: The invention relates to compositions and methods for utilizing lysophosphatidylcholine scaffolds. The compositions and methods can be used for LPC-mediated delivery of fatty acids and other molecules; to screen and identify fatty acid formulations for parenteral nutrition; and for live animal organ imaging, among other uses. The invention also provides compositions and methods for utilizing mutations and polymorphisms in human Mfsd2a as markers for neurological deficits.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: January 8, 2019
    Assignee: NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: David Lawrence Silver, Nam Long Nguyen, Robert Zahler
  • Patent number: 10130708
    Abstract: 2:1 cocrystals of amino acids and Li+ salts crystallize from hot water to afford water stable cationic networks based upon tetrahedral lithium cations: bilayered square grids, a lithium zeolitic metal-organic material (LiZMOM) and several lithium diamondoid metal-organic materials (LiDMOMs). The compositions may be used as a pharmaceutical for the treatment of suicidality and other disorders that require lithium to penetrate the blood brain barrier and exert therapeutic effects in the CNS. Advantageously, the novel cocrystal forms described herein may be used to lower the oral dose required to achieve therapeutic concentrations of lithium in the brain, thus reducing the peripheral toxicity and potentially broadening the therapeutic index in comparison to conventional lithium forms.
    Type: Grant
    Filed: March 26, 2012
    Date of Patent: November 20, 2018
    Assignee: University of South Florida
    Inventors: Michael John Zaworotko, Roland D. Shytle, Tien Teng Ong, Ryan N. Cantwell, Tranhha Nguyen, Adam John Smith, Padmini Kavuru
  • Patent number: 10030044
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver cancer such as hepatocellular carcinoma, cholangiocarcinoma, or biliary tract cancer. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-cancer agents. In certain embodiments, the compounds are nucleoside analogs of Formula I: (I); or a pharmaceutically acceptable salt thereof, wherein Base, Z1, Z2, Z3, Z4, V, W, X, Ar, R1 and R2 are as described herein.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: July 24, 2018
    Assignee: IDENIX PHARMACEUTICALS LLC
    Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy
  • Patent number: 10022378
    Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
    Type: Grant
    Filed: May 15, 2017
    Date of Patent: July 17, 2018
    Assignee: EMORY UNIVERSITY
    Inventors: Christina Gavegnano, Raymond F. Schinazi
  • Patent number: 9913854
    Abstract: Provided herein are methods for inducing cell death in a gram positive bacterium and methods for reducing the proliferation of a gram positive bacterium that include contacting a gram positive bacterium with a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are methods of treating a subject having a gram positive bacterial infection that include administering to a subject having a gram positive bacterial infection a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are compositions containing a dye (e.g., an azo dye) and a TarO inhibitor, and kits containing at least one of these compositions.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: March 13, 2018
    Assignee: Massachusetts Eye & Ear Infirmary
    Inventors: Michael S. Gilmore, Takashi Suzuki
  • Patent number: 9878984
    Abstract: The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation.
    Type: Grant
    Filed: September 8, 2014
    Date of Patent: January 30, 2018
    Assignee: NORTHWESTERN UNIVERSITY
    Inventors: Sui Huang, John Norton, Daniel Appella, Mark Witschi
  • Patent number: 9693553
    Abstract: Storage stable polyhydroxylated aromatic ether adducts of polyalkylene oxide are described. Reactive compositions are formed by combining an ether adduct with an aldehyde, optionally further adding a phenolic-aldehyde prepolymer. The reactive compositions are cured by removing water, by acidification, or both. The cured compositions sorb solvated compounds from environments containing water. The cured compositions are also useful for pre-loading with compounds that are subsequently released at a controlled rate into environments containing water.
    Type: Grant
    Filed: April 21, 2016
    Date of Patent: July 4, 2017
    Assignee: Eco Verde Technologies, Inc.
    Inventor: Curtis Elliott
  • Patent number: 9662332
    Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: May 30, 2017
    Assignee: EMORY UNIVERSITY
    Inventors: Christina Gavegnano, Raymond F. Schinazi
  • Patent number: 9346848
    Abstract: Disclosed herein are 4?-azido-substituted nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of 4?-azido-substituted nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a 4?-azido-substituted nucleoside, a nucleotide and/or an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: May 24, 2016
    Assignee: Alios BioPharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Patent number: 9333216
    Abstract: The present invention relates to the new indications of chronic obstructive pulmonary disease (COPD) and idiophathic lung fibrosis (IPF) for uridine and uridine analogues.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: May 10, 2016
    Assignee: Universitaetsklinikum Freiburg
    Inventors: Marco Idzko, Stephan Sorichter
  • Patent number: 9296776
    Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.
    Type: Grant
    Filed: July 9, 2008
    Date of Patent: March 29, 2016
    Assignees: Eastern Virginia Medical School, Board of Governors for Higher Education, State of Rhode Island and Providence Plantations
    Inventors: Gustavo F. Doncel, Keykavous Parang, Hitesh Kumar Agarwal
  • Patent number: 9265787
    Abstract: Methods for treating tumors comprising cells expressing the vitamin D receptor are provided, and comprise inhibiting the expression or the biologic activity of the vitamin D receptor in the tumor cells, and/or inhibiting the expression or the biologic activity of a constituent of the vitamin D receptor signaling pathway in the tumor cells, and administering to the tumor cells an effective amount of gemcitabine.
    Type: Grant
    Filed: December 26, 2013
    Date of Patent: February 23, 2016
    Assignee: Institute for Cancer Research
    Inventors: Timothy J. Yen, Vikram Bhattacharjee
  • Patent number: 9249173
    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: March 4, 2014
    Date of Patent: February 2, 2016
    Assignee: Idenix Pharmaceuticals, LLC
    Inventors: Jean-Pierre Sommadossi, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
  • Patent number: 9206217
    Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
    Type: Grant
    Filed: January 2, 2013
    Date of Patent: December 8, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
  • Patent number: 9181549
    Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: November 10, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Patent number: 9181550
    Abstract: Provided herein are oligomeric compounds with conjugate groups targeting apoplipoprotein (a) [apo(a)]. In certain embodiments, the apo(a) targeting oligomeric compounds are conjugated to N-Acetylgalactosamine. Also disclosed herein are conjugated oligomeric compounds targeting apo(a) for use in decreasing apo(a) to treat, prevent, or ameliorate diseases, disorders or conditions related to apo(a) and/or Lp(a). Certain diseases, disorders or conditions related to apo(a) and/or Lp(a) include inflammatory, cardiovascular and/or metabolic diseases, disorders or conditions. The conjugated oligomeric compounds disclosed herein can be used to treat such diseases, disorders or conditions in an individual in need thereof.
    Type: Grant
    Filed: December 31, 2014
    Date of Patent: November 10, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze, Mark J. Graham
  • Patent number: 9173391
    Abstract: The present invention relates to crystalline complexes of 4-hydroxy benzoic acid and selected pesticides. It also relates to agriculturally useful compositions of the complexes.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: November 3, 2015
    Assignee: BASF SE
    Inventors: Heidi Emilia Saxell, Rafel Israels, Ansgar Schaefer, Matthias Bratz, Hans Wolfgang Hoeffken, Ingo Brode, Elisa Nauha, Maija Nissinen
  • Patent number: 9163239
    Abstract: Provided herein are oligomeric compounds with conjugate groups targeting apoplipoprotein C-III (ApoCIII). In certain embodiments, the ApoCIII targeting oligomeric compounds are conjugated to N-Acetylgalactosamine. Also disclosed herein are conjugated oligomeric compounds targeting ApoCIII for use in decreasing ApoCIII to treat, prevent, or ameliorate diseases, disorders or conditions related to ApoCIII. Certain diseases, disorders or conditions related to ApoCIII include inflammatory, cardiovascular and/or metabolic diseases, disorders or conditions. The conjugated oligomeric compounds disclosed herein can be used to treat such diseases, disorders or conditions in an individual in need thereof.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: October 20, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze, Mark J. Graham
  • Patent number: 9145558
    Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: September 29, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Patent number: 9127276
    Abstract: Provided herein are oligomeric compounds with conjugate groups. In certain embodiments, the oligomeric compounds are conjugated to N-Acetylgalactosamine.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: September 8, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Punit P. Seth, Eric E. Swayze
  • Patent number: 9089574
    Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: July 28, 2015
    Assignee: EMORY UNIVERSITY
    Inventors: Christina Gavegnano, Raymond F. Schinazi
  • Patent number: 9040502
    Abstract: A method for treating an individual infected with XDR-TB, the method including administering to the individual an anti-XDR-TB drug which comprises a compound having a structure expressed by Structural Formula (1) below:
    Type: Grant
    Filed: March 30, 2011
    Date of Patent: May 26, 2015
    Assignees: Microbial Chemistry Research Foundation, Infectious Disease Research Institute
    Inventors: Yoshiaki Takahashi, Masayuki Igarashi, Masaji Okada
  • Patent number: 9040501
    Abstract: Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: May 26, 2015
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Sergel Belyakov, Bridget Duvall, Dana Ferraris, Gregory Hamilton, Mark Vaal
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 9029346
    Abstract: Methods and compounds are disclosed for irreversibly inhibiting a DNA repair enzyme that possesses lyase activity.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: May 12, 2015
    Assignee: The Johns Hopkins University
    Inventors: Marc M. Greenberg, Dumitru Arian, Theodore L. Deweese, Mohammad Hedayati
  • Patent number: 9029413
    Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: May 12, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
  • Publication number: 20150126437
    Abstract: The disclosure provides compounds useful as insect repellents, compositions comprising such repellents, and methods of repelling an arthropod using such compounds and compositions. The disclosure further provides insect traps and method for identifying ligands and cognates for biological molecules.
    Type: Application
    Filed: October 17, 2012
    Publication date: May 7, 2015
    Applicant: The Regents of the University of California
    Inventors: Anandasankar Ray, Sean Michael Boyle
  • Patent number: 9012427
    Abstract: Disclosed herein are pharmaceutical compositions that can include a thionucleotide analog for use in combination therapy with other agents. Also disclosed herein are methods of treating diseases and/or conditions with a pharmaceutical composition that can include a thionucleotide analog in combination therapy with other agents.
    Type: Grant
    Filed: March 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Alios BioPharma, Inc.
    Inventors: Lawrence M Blatt, Leonid Beigelman, Hua Tan, Julian Alexander Symons, David Bernard Smith, Min Jiang, Tara Lynn Kieffer, Cornelis Arie Rijnbrand
  • Patent number: 9012428
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 21, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20150105341
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150105342
    Abstract: The present invention relates to a method for determining the likelihood of disease outcome of a patient diagnosed with microsatellite stable, stage II colorectal cancer. More in particular, the present invention relates to a method for determining the prognosis of a patient diagnosed with microsatellite stable, stage II colorectal cancer wherein the CpG island methylation status of the promoter of the CHFR gene is determined and wherein methylation of the promoter is indicative of a poor prognosis.
    Type: Application
    Filed: April 25, 2013
    Publication date: April 16, 2015
    Applicant: Universiteit Maastricht
    Inventors: Manon van Engeland, Adriaan Pieter de Bruïne, James Herman
  • Publication number: 20150104511
    Abstract: The present invention relates to a pharmaceutical antiretroviral composition comprising lamivudine, festinavir and nevirapine, to a process for preparing such a composition and to the use of such a composition for the treatment and/or prophylaxis of diseases caused by retroviruses, especially acquired immune deficiency syndrome or an HIV infection.
    Type: Application
    Filed: March 5, 2013
    Publication date: April 16, 2015
    Inventors: Geena Malhotra, Shrinivas Madhukar Purandare
  • Patent number: 9006208
    Abstract: An agent for treatment of dry eye comprising a combination of a P2Y2 receptor agonist at a therapeutically effective concentration and hyaluronic acid or a salt thereof at a therapeutically effective concentration, which agent has a dosage form of an ophthalmic agent, can promote the secretion of tear remarkably and can improve corneal epithelial disorders remarkably, and is therefore expected to be a novel agent for treatment of dry eye.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: April 14, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Yuko Shichijo, Atsuyoshi Dota, Takashi Nagano, Masatsugu Nakamura, Asuka Sakamoto
  • Patent number: 9006209
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 14, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20150087614
    Abstract: Provided herein are methods for inducing cell death in a gram positive bacterium and methods for reducing the proliferation of a gram positive bacterium that include contacting a gram positive bacterium with a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are methods of treating a subject having a gram positive bacterial infection that include administering to a subject having a gram positive bacterial infection a dye (e.g., an azo dye) and a TarO inhibitor. Also provided are compositions containing a dye (e.g., an azo dye) and a TarO inhibitor, and kits containing at least one of these compositions.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 26, 2015
    Inventors: Michael S. Gilmore, Takashi Suzuki
  • Publication number: 20150051167
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 19, 2015
    Inventors: Guangyi Wang, David Bernard Smith, Leonid Beigelman, Jerome Deval, Marija Prhavc
  • Patent number: 8957046
    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: April 16, 2014
    Date of Patent: February 17, 2015
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20150044304
    Abstract: The invention relates to a composition comprising: (i) one or more of uridine and cytidine, or salts, phosphates, acyl derivatives or esters thereof; and (ii) a lipid fraction comprising at least one of docosahexaenoic acid (22:6; DHA), eicosapentaenoic acid (20:5; EPA) and docosapentaenoic acid (22:5; DPA), or esters thereof, for use in the improvement of the composite NTB score. The invention also provides an improved NTB method comprising an optimized set of individualized tests, in particular for a (prodromal or mild) Alzheimer's or dementia patient.
    Type: Application
    Filed: October 30, 2012
    Publication date: February 12, 2015
    Inventors: Martine Groenendijk, Anke Bongers, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Patent number: 8951988
    Abstract: The invention provides the Zidovudine-conjugated quinoline compound N-((1-(2-(hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kill hepatoma cells, especially hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm that the compound has an anti-hepatoma effect and can be used in preparation of anti-hepatoma drugs.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: February 10, 2015
    Assignee: Huazhong University of Science and Technology
    Inventor: Qibing Zhou
  • Patent number: 8951987
    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: November 25, 2013
    Date of Patent: February 10, 2015
    Assignee: Otsuka Pharmaceuticals Co., Ltd.
    Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
  • Patent number: 8951985
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 10, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Dominique Surleraux, Cyril B. Dousson, David Dukhan, Claire Pierra
  • Publication number: 20150038446
    Abstract: The present disclosure relates to compositions and methods for treating retinal damage and/or retinal degradation. More specifically, this disclosure relates to methods for treating degradation of the retinal pigment epithelium by administering compositions comprising a nucleoside and/or a nucleoside or nucleotide reverse transcriptase inhibitor.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 5, 2015
    Inventors: Jayakrishna Ambati, Benjamin Fowler
  • Publication number: 20150017124
    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: July 17, 2014
    Publication date: January 15, 2015
    Inventors: Richard STORER, Gilles GOSSELIN, Jean-Pierre SOMMADOSSI, Paolo LACOLLA
  • Publication number: 20150011497
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 8, 2015
    Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
  • Publication number: 20150010496
    Abstract: Disclosed herein are ?-galactosylceramide (?-GalCer) analogs and compositions thereof, methods of activating invariant Natural Killer T (iNKT) cells using said analogs, methods of treating diseases by activating iNKT cells using said analogs, and combination therapy of said analogs.
    Type: Application
    Filed: November 30, 2012
    Publication date: January 8, 2015
    Inventors: Vincenzo Cerundolo, Gurdyal S. Besra, Liam Cox
  • Publication number: 20150010509
    Abstract: Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection, tuberculosis and type 2 diabetes based upon the administration of CaFolate. In one embodiment is a method of treating cancer comprising administration of CaFolate. In another embodiment is a method of treatment inflammatory-based disease and disorders comprising administration of CaFolate.
    Type: Application
    Filed: January 29, 2013
    Publication date: January 8, 2015
    Applicant: SanRx Pharmaceuticals, Inc.
    Inventor: Phillip Moheno
  • Publication number: 20150011488
    Abstract: Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins are applied (A) directly to a genital wart in the form of a cream, ointment, paste or solution, (B) directly to the genital wart wherein such cream, ointment, paste or solution contains as an additional active ingredient a skin permeabilizing agent, (C) following electrosurgical resection or removal of the genital wart in such form of a cream, ointment, paste or solution, (D) following chemical resection or extirpation of the genital wart in such form, (E) following surgical resection or removal of the genital wart in such form, wherein said Epicatechins, Epicatechin Oligomers, or Thiolated Epicatechins both provide antiviral activity against multiple strains of human pappilomavirus (HPV) and promote healing following resection polymers contained in a vehicle. Disclosed are the compositions, therapeutical kits containing such composition, methods of treatment using such composition, and methods of enhancing the stability of such composition.
    Type: Application
    Filed: March 10, 2014
    Publication date: January 8, 2015
    Applicant: CACAO BIO-TECHNOLOGIES, LLC
    Inventors: Daniel PRESTON, Randall B. MURPHY
  • Publication number: 20150005251
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi