Purines (including Hydrogenated) (e.g., Adenine, Guanine, Etc.) Patents (Class 514/45)
  • Patent number: 8846635
    Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: September 30, 2014
    Assignee: Can-Fite Biopharma Ltd.
    Inventors: Pnina Fishman, Shira Cohen
  • Patent number: 8846637
    Abstract: Provided herein are 2?-amino and 2?-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.
    Type: Grant
    Filed: June 2, 2011
    Date of Patent: September 30, 2014
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Thazha P. Prakash, Eric E. Swayze
  • Publication number: 20140286903
    Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
  • Publication number: 20140288018
    Abstract: The present invention relates to methods for predicting the response to treatment with an agonist of TLR7, or an agonist of TLR8 or an anti-cancer agent for treating cancer, in particular non-small cell lung cancer comprising the step of detecting the expression of TLR7 or TLR8 in cancer cells of said patient.
    Type: Application
    Filed: March 27, 2014
    Publication date: September 25, 2014
    Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale )
    Inventors: Julien Cherfils, Herve Fridman, Isabelle Cremer
  • Patent number: 8840926
    Abstract: The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: September 23, 2014
    Assignee: Ultragenyx Pharmaceutical Inc.
    Inventors: Emil Kaskkis, Steven Jungles, He Zhao
  • Patent number: 8841275
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: September 23, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Michael Joseph Sofia
  • Publication number: 20140271876
    Abstract: The present invention relates to an ophthalmic formulation which comprises a fine particle of Compound A in an aqueous suspension and a manufacturing process thereof. More specifically, the present invention relates to a topically applied ophthalmic aqueous suspension which is obtainable by suspending fine particles of Compound A in an aqueous vehicle containing a surfactant and boric acid. The invention also provides processes for making the ophthalmic formulations and to methods of use thereof.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventors: William K. MCVICAR, Harun TAKRURI
  • Patent number: 8815827
    Abstract: Myeloid differentiating agents can be used in the treatment of myeloid disorders.
    Type: Grant
    Filed: June 12, 2008
    Date of Patent: August 26, 2014
    Assignee: Case Western Reserve University
    Inventor: David Wald
  • Publication number: 20140235563
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicants: Gilead Sciences, Inc., Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du
  • Patent number: 8809299
    Abstract: Described are methods and compositions for treating cancer that include a dopamine receptor (DR) antagonist such as thioridazine and a chemotherapeutic agent. Optionally, the chemotherapeutic agent is a DNA synthesis inhibitor such as cytarabine or a microtubule inhibitor such as paclitaxel or docetaxel. The methods and compositions are useful for the treatment of cancers such as acute myeloid leukemia.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: August 19, 2014
    Assignee: McMaster University
    Inventors: Mickie Bhatia, Eleftherios Sachlos
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • 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
  • Publication number: 20140213539
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Application
    Filed: August 19, 2013
    Publication date: July 31, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein, Robert Seemayer, Travis Lemons
  • Patent number: 8791081
    Abstract: A method of treating a neoplastic disease in a subject includes administering to neoplastic cells of the subject an MGMT inhibitor and at least one of an antimitotic agent or a DNA damaging agent.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: July 29, 2014
    Assignee: Case Western Reserve University
    Inventors: Lili Liu, Stanton Gerson
  • 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
  • Patent number: 8778906
    Abstract: A method is provided for treating individuals suffering from cancer characterized by tumor cells which are telomerase negative, do not have telomerase activity or have L1RT expression or alternative lengthening of telomeres. The method includes administering to an individual in need of treatment thereof, and having the aforementioned cancer, a therapeutically effective amount of a nucleoside analog selected from one or more of the group consisting of: 3?-azido-2?,3?-dideoxythymidine (AZT), 2?,3?-dideoxyinosine (ddI) and 2?,3?-didehydro-3?-deoxythymidine (d4T).
    Type: Grant
    Filed: February 22, 2008
    Date of Patent: July 15, 2014
    Assignee: ALT Solutions, Inc.
    Inventors: Igor E. Bondarev, John S. Bertram
  • Publication number: 20140194349
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: AbbVie Inc.
    Inventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
  • Patent number: 8765935
    Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.
    Type: Grant
    Filed: January 29, 2013
    Date of Patent: July 1, 2014
    Assignee: Regents of the University of Minnesota
    Inventor: Carston R. Wagner
  • Patent number: 8765710
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: July 1, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du
  • 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: 8759318
    Abstract: Phosphoramidate compounds derived from guanine bases having enhanced therapeutic potency are provided, and these compounds in particular have enhanced potency with respect to treatment of viral infections, such as hepatitis C virus. Pharmaceutical compositions, methods of preparing the compounds, and methods of using the compounds and compositions to treat viral infections are also provided.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: June 24, 2014
    Assignees: Inhibitex, Inc., University College Cardiff Consultants Limited
    Inventors: Stanley Chamberlain, Jeff Hutchins, Karolina Madela, Christopher McGuigan, John Vernachio, Mohamed Aljarah, Arnaud Gilles
  • Patent number: 8759510
    Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: June 24, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
  • Patent number: 8759315
    Abstract: A ribose-related compound is added to whole blood or packed red cells which have suboptimal function as measured by decreased levels of 2,3-DPG in order to rejuvenate the red blood cells to normal function as seen by raised levels of 2,3-DPG. Two representative ribose-related compounds are D-ribose and inosine.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: June 24, 2014
    Assignee: Viacell, LLC
    Inventors: John A St. Cyr, Daniel G Ericson, Clarence A Johnson
  • 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: 8742101
    Abstract: This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: June 3, 2014
    Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier II
    Inventors: Richard Storer, Gilles Gosselin, David Dukhan, Frederic Leroy
  • Publication number: 20140140955
    Abstract: This invention is directed to novel compounds of formula (I) having the structure (I) wherein U, V, W, Z, R1, X1, X2, and Y are defined herein. The compounds of formula (I) and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals mediated, at least in part, by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV).
    Type: Application
    Filed: December 29, 2011
    Publication date: May 22, 2014
    Applicants: UNIVERSITY COLLEGE OF CARDIFF CONSULTANTS LIMITED, INHIBITEX, INC.
    Inventors: Chris McGuigan, Karolina Madela, Claire Bourdin, John Vernachio, Stanley Chamberlain
  • Patent number: 8729047
    Abstract: The invention provides compositions for inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, comprising an effective amount of a redox-sensitive purine compound and an effective amount of a redox agent. The invention further provides methods of inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, by administering compositions of the invention. Methods of screening for compounds that inhibit a redox-sensitive GTPase protein, including compounds that target and inhibit Rho or Rab family GTPases, are further provided.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: May 20, 2014
    Assignee: Board of Regents, The University of Texas System
    Inventor: Jongyun Heo
  • Publication number: 20140128322
    Abstract: Disclosed is a method of promoting neuronal growth by administering IGFBPL-1, or an agent that increases or stabilizes IGFBPL-1 activity to a subject in need thereof, e.g., a subject in need of treating optic nerve degeneration.
    Type: Application
    Filed: February 28, 2012
    Publication date: May 8, 2014
    Inventors: Dong Feng Chen, Chenying Guo
  • Patent number: 8716253
    Abstract: The invention relates to the therapeutic use of oligonucleotides or oligonucleotide analogs as immunostimulatory agents in immunotherapy applications. The invention provides methods for enhancing the immune response caused by immunostimulatory oligonucleotide compounds.
    Type: Grant
    Filed: October 27, 2003
    Date of Patent: May 6, 2014
    Assignee: Idera Pharmaceuticals, Inc.
    Inventors: Ekambar R. Kandimalla, Qiuyan Zhao, Dong Yu, Sudhir Agrawal
  • Patent number: 8716263
    Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: May 6, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Byoung-Kwon Chun, Jinfa Du, Suguna Rachakonda, Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Wonsuk Chang, Hai-Ren Zhang, Dhanapalan Nagarathnam
  • Patent number: 8709996
    Abstract: The present invention provides a solid composition for oral administration comprising: (i) a drug compound; (ii) chitosan or a derivative thereof or a salt of chitosan or salt of a derivative of chitosan; and (iii) an organic acid. Preferably the drug compound is a polar molecule having a molecular weight of 1 KDa or less, a peptide, a protein or a polysaccharide. The compositions of the invention provide enhance absorption of the drug compound.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: April 29, 2014
    Assignee: Archimedes Development Limited
    Inventors: Michael Leane, Alan Smith, Lisbeth Illum
  • Patent number: 8680070
    Abstract: The invention provides methods and compositions for reducing or inhibiting bone resorption, osteoclast differentiation and stimulation and the loosening of medical prostheses by administering a compound or agent that modulates an adenosine receptor such as the adenosine A2A receptor, in particular, an agonist of an adenosine A2A receptor. The invention also extends to pharmaceutical compositions comprising such an agent that modulates an adenosine receptor such as an adenosine A2A agonist and to prosthetic devices containing such an agent that modulates an adenosine receptor such as an A2A agonist on one or more surfaces or within the prosthetic device such as, for example, suspended in the cement forming the prosthetic device.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: March 25, 2014
    Assignee: New York University
    Inventors: Bruce N. Cronstein, Aranzazu Mediero Munoz
  • 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
  • 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
  • Publication number: 20140045780
    Abstract: The present invention relates to compositions comprising spicamycin derivatives, methods of making such compositions, and their use in the treatment and/or prevention of pain, including neuropathic pain.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 13, 2014
    Applicant: DARA BioSciences, Inc.
    Inventors: Michael Radomsky, Mary Katherine Delmedico, Linda Jett
  • Patent number: 8637475
    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: Grant
    Filed: June 24, 2011
    Date of Patent: January 28, 2014
    Assignees: Idenix Pharmaceuticals, Inc., University of Cagliari, The Centre National de la Recherché Scientifique, L'Universite Montpelier II
    Inventors: Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
  • Patent number: 8637486
    Abstract: Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: January 28, 2014
    Assignee: Retrotope, Inc.
    Inventor: Mikhail S. Shchepinov
  • 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: 8609627
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: December 17, 2013
    Assignees: RFS Pharma, LLC, Emory University
    Inventors: Jong Hyun Cho, Steven J. Coats, Raymond F. Schinazi, Hongwang Zhang, Longhu Zhou
  • 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
  • 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
  • Publication number: 20130324461
    Abstract: The invention includes methods of treating, preventing, or limiting obesity or weight gain, or reducing or suppressing appetite, by the administration of A2A adenosine receptor pathway agonists. The A2AR pathway agonists may be administered in conjunction with a therapeutic agent having a side effect of weight gain, in order to prevent or limit that weight gain. In some instances, the A2AR pathway agonist is administered as a sleeping pill, and in other instances the A2AR pathway agonist is administered in a non-drowsy formulation.
    Type: Application
    Filed: August 26, 2011
    Publication date: December 5, 2013
    Inventors: Michail V. Sitkovsky, Akio Ohta
  • 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: 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
  • Patent number: 8592566
    Abstract: A novel immunostimulatory oligonucleotide by which an IFN-inducing activity is enhanced and an inflammatory cytokine-inducing activity is reduced, and a pharmaceutical containing the same, and an application thereof are provided.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: November 26, 2013
    Assignees: Toray Industries, Inc., Osaka University
    Inventors: Tomokatsu Iwamura, Hideki Narumi, Hajime Masumoto, Akihito Kaneda, Akiko Soneda, Shizuo Akira
  • Publication number: 20130309188
    Abstract: The present invention has an object to provide an external dermal agent with a sustainable anti-wrinkle action, which has both the action of enhancing the proliferation and differentiation of keratinocytes in the skin and the action of enhancing the collagen production in the skin, and which assists the maintenance and the improvement of tissue structures and physiological functions of the epidermis and the dermis, whereby providing a remarkable skin improvement effect. The present invention solves the above abject by providing an external dermal agent containing ?-D-glucopyranosyl-(1?3?)-adenosine and/or ?-D-glucopyranosyl-(1?5?)-adenosine as an effective ingredient(s).
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: HAYASHIBARA CO., LTD.
    Inventors: Tatsuya Ishihara, Shimpei Ushio, Rohko Yamamoto, Takanori Ohkura, Shigeharu Fukuda
  • Publication number: 20130310333
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Application
    Filed: December 5, 2011
    Publication date: November 21, 2013
    Applicant: EPIZYME, INC.
    Inventors: Richard Chesworth, Kevin Wayne Kuntz, Edward James Olhava, Michael A. Patane
  • Patent number: 8580763
    Abstract: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.
    Type: Grant
    Filed: April 17, 2008
    Date of Patent: November 12, 2013
    Assignees: Zhanggui Wu, Zhe Jiang Medicine Co., Ltd
    Inventors: Zhanggui Wu, Weidong Ye, Jianyong Yuan, Gang Chen
  • Patent number: 8580753
    Abstract: Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention of tumorigenic telomerase positive cells from having a chance to grow into a tumor and methods for promoting tumor regression (decrease in size of an established tumor) using acyclic nucleoside analogs has been disclosed.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: November 12, 2013
    Assignee: ALT Solutions Inc.
    Inventor: Igor E. Bondarev