2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
  • Publication number: 20120294869
    Abstract: The present invention relates to the compositions, formulations and methods of treating fatty liver disorders, such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH) and their sequelae by administration of uridine or a compound that modulates one or more uridine phosphorylases in a subject in need thereof.
    Type: Application
    Filed: May 15, 2012
    Publication date: November 22, 2012
    Applicant: Nevada Cancer Institute
    Inventors: Giuseppe Pizzorno, Amy Ziemba, Steve Brotman
  • Patent number: 8314064
    Abstract: The present invention provides methods of stimulating or enhancing production of a cellular membrane, improving a cognitive function or a neurological function, treating or ameliorating a decline in a cognitive function or a neurological function, increasing cytidine levels, or treating a neurological disorder in a subject, comprising administering a uridine, a uridine precursor, or a derivative or metabolite thereof to the subject. The invention also provides methods of improving neural function, comprising contacting the neuron with a uridine, a uridine precursor, or a derivative or metabolite thereof.
    Type: Grant
    Filed: October 26, 2004
    Date of Patent: November 20, 2012
    Assignee: Massachusetts Institute of Technology
    Inventors: Carol Watkins, Richard J. Wurtman
  • Publication number: 20120282218
    Abstract: New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.
    Type: Application
    Filed: December 7, 2010
    Publication date: November 8, 2012
    Applicant: University of Georgia Research Foundation Inc.
    Inventors: Vasu Nair, Maurice O. Okello, Abdumalik A. Nishonov, Sanjaykumar Mishra
  • Patent number: 8299038
    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: Grant
    Filed: July 16, 2009
    Date of Patent: October 30, 2012
    Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paulo LaColla
  • Patent number: 8293778
    Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
    Type: Grant
    Filed: February 20, 2010
    Date of Patent: October 23, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
  • Publication number: 20120263678
    Abstract: Provided are compounds of Formula I: nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 18, 2012
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Aesop Cho, Choung U. Kim, Thorsten A. Kirschberg, Michael R. Mish, Neil Squires
  • Publication number: 20120264707
    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: May 4, 2012
    Publication date: October 18, 2012
    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: 20120258929
    Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.
    Type: Application
    Filed: June 23, 2006
    Publication date: October 11, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
  • Patent number: 8283336
    Abstract: The invention pertains to a composition comprising (i) uridine in nucleobase, nucleoside and/or nucleotide form; (ii) docosahexaenoic acid (DHA) and/or eicosapentaenoic acid (EPA); and (iii) a tocopherol and/or an equivalent thereof, wherein said composition has: a) a weight of 200-3000 mg per unit dose; b) an energy content of less than 50 kcal per unit dose; and/or c) a volume between 0.1 and 10 ml per unit dose. The invention also pertains to the use of such composition in reducing abeta plaque burden and neurodegeneration, in the treatment of diseases related with imparted nerve functioning, in particular dementia, Alzheimer's disease and memory disorders.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: October 9, 2012
    Assignee: N. V. Nutricia
    Inventors: Martine Groenendijk, Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis, Erwin Peke Meijer
  • Patent number: 8283335
    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: June 20, 2008
    Date of Patent: October 9, 2012
    Assignee: N.V. Nutricia
    Inventors: Robert Johan Joseph Hageman, Eline Marleen van der Beek, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Publication number: 20120251495
    Abstract: Disclosed herein are methods for the treatment of cancer and inflammatory-based diseases and disorders, such as hepatitis B virus infection based upon the administration of calcium pterin. In one embodiment is a method of treating cancer comprising administration of dipterinyl calcium pentahydrate (DCP). In another embodiment is a method of treating hepatitis B virus infection comprising administration of dipterinyl calcium pentahydrate (DCP).
    Type: Application
    Filed: January 16, 2009
    Publication date: October 4, 2012
    Inventors: Phillip Moheno, Wolfgang Pfleiderer, Antonio DiPasquale, Arnold Rheingold, Dietmar Fuchs
  • Publication number: 20120237480
    Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
  • Patent number: 8268800
    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: October 16, 2008
    Date of Patent: September 18, 2012
    Assignee: Eisai Inc.
    Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
  • Patent number: 8268348
    Abstract: The present invention provides combination therapy methods of treating proliferative diseases (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include, for example, radiation, surgery, administration of chemotherapeutic agents, or combinations thereof. Also provided are methods of administering to an individual a drug taxane in a nanoparticle composition based on a metronomic dosing regime.
    Type: Grant
    Filed: September 8, 2011
    Date of Patent: September 18, 2012
    Assignee: Abraxis Bioscience, LLC
    Inventors: Neil P. Desai, Patrick Soon-Shiong
  • Publication number: 20120232029
    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: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Publication number: 20120232028
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Application
    Filed: May 21, 2012
    Publication date: September 13, 2012
    Applicant: Tobira Therapeutics, Inc.
    Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
  • Publication number: 20120225836
    Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.
    Type: Application
    Filed: March 7, 2012
    Publication date: September 6, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Joseph Desimone, Yogen Saunthararajah
  • Publication number: 20120225837
    Abstract: 1-(2-Fluoro-4-thio-?-D-arabinofuranosyl)-5-methyluracil exhibits an anti-EB virus activity, and is therefore effective as a prophylactic or therapeutic agent for a disease associated with an EB virus. Each of a plasmid capable of expressing EB virus-TK and a plasmid capable of expressing human-TK is introduced into a TK-defect cell, thereby producing two types of cells respectively having the plasmids introduced therein. By using the two types of cells, it is possible to screen a medicinal agent which has cytotoxicity against the cell having the plasmid capable of expressing EB virus-TK introduced therein but has no toxicity against the cell having the plasmid capable of expressing human-TK introduced therein. In this manner, it becomes possible to screen a medicinal agent which specifically exhibits an anti-EB virus activity.
    Type: Application
    Filed: April 16, 2012
    Publication date: September 6, 2012
    Applicants: Kyoto University, Yamasa Corporation
    Inventors: Eiichi KODAMA, Masao Matsuoka, Noriyuki Ashida
  • Publication number: 20120225838
    Abstract: There is provided an agent for potentiating the effects of an anti-tumor agent. An anti-tumor effect potentiator containing, as an active ingredient, a uracil compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents a C1-5 alkylene group and one of methylene groups constituting the alkylene group is optionally substituted with an oxygen atom; R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl) C1-6 alkyl group, a halogeno-C1-6 alkyl group or a saturated heterocyclic group.
    Type: Application
    Filed: November 29, 2010
    Publication date: September 6, 2012
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Patent number: 8258116
    Abstract: The present invention relates to therapeutic combinations comprising a protease inhibitor and a polymerase inhibitor for the treatment of HCV. The present invention also relates to therapeutic combinations comprising VX-950 and a polymerase inhibitor. Also within the scope of the invention are methods using the therapeutic combinations of the present invention for treating HCV infection or alleviating one or more symptoms thereof in a patient. The present invention also provides kits comprising the combinations of the present invention.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: September 4, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Ann Kwong, Nagraj Mani, Yi Zhou, Chao Lin
  • Patent number: 8247382
    Abstract: A method for increasing oxytocin release through direct action on the epidermal keratinocytes is provided. The method for increasing oxytocin release in the epidermis includes increasing the calcium ion concentration in the epidermal cells. In the method of the present invention, the increase of the calcium ion concentration in the epidermal cells may be achieved by physically stimulating the skin. The physical stimulation may be achieved by applying a heat stimulus and/or a massage. The increase of the calcium ion concentration in the epidermal cells may be achieved by stimulating the epidermal cells by at least one agent selected from the group consisting of ATP, UTP, 4 alpha-phorbol 12,13-didecanoate, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: August 21, 2012
    Assignee: Shiseido Company, Ltd.
    Inventors: Sumiko Denda, Mitsuhiro Denda, Kazuyuki Ikeyama
  • Patent number: 8242087
    Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.
    Type: Grant
    Filed: August 27, 2009
    Date of Patent: August 14, 2012
    Assignee: K.U.Leuven Research & Development
    Inventors: Olga Adelfinskaya, Piet Herdewijn
  • Patent number: 8236779
    Abstract: Compounds having the formula I wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: August 7, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Han Ma, Keshab Sarma, David Bernard Smith
  • Patent number: 8236756
    Abstract: The present invention provides a new prodrug technology and new prodrugs in order to increase the solubility, to modulate plasma protein binding or to enhance the biovailability of a drug. In the present invention the prodrugs are conjugates of a therapeutic compound and a peptide (eg tetrapeptide or hexapeptide) wherein the conjugate is cleavable by dipeptidyl-peptidases, more preferably by CD26, also known as DPPIV (dipeptidyl aminodipeptidase IV). The present invention furthermore provides a method of producing the prodrugs, to enhance brain and lymphatic delivery of drugs and/or to extend drug half-lives in plasma.
    Type: Grant
    Filed: May 10, 2004
    Date of Patent: August 7, 2012
    Assignees: Consejo Superior de Investigaciones Clentificas (CSIC), K.U. Leuven Research & Development
    Inventors: Jan Balzarini, Maria José Camarasa Ríus, Sonsoles Velázquez Díaz
  • Publication number: 20120198576
    Abstract: Embodiments of the invention are based upon the discovery that exposure of cleavage-stage embryos to a stress inducer, e.g. heat shock or chemical, renders the exposed embryos more sensitive to a secondary treatment with a stress inducer, e.g. heat shock or chemical inducer. Accordingly, the present invention is directed to methods for making embryos, embryonic cells arising from them, and animals and plants that are sensitized to stress, e.g. physiologic or chemical stressors. Methods of screening for inducers and inhibitors of stress using, as test model systems, embryonic cells, embryos, animals, and plants that are sensitized to stress are also disclosed.
    Type: Application
    Filed: July 1, 2010
    Publication date: August 2, 2012
    Applicant: BRANDEIS UNIVERSITY
    Inventors: Lawrence J. Wangh, Cristina Hartshorn, Yanwei Jia
  • Publication number: 20120165288
    Abstract: This invention relates to novel compounds that are azapeptides, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel azapeptide compounds that are derivatives of the HIV protease inhibitor atazanavir sulfate. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administering HIV protease inhibitors. The invention also relates to the use of one or more of the disclosed compounds as reagents in analytical studies involving atazanavir.
    Type: Application
    Filed: March 2, 2012
    Publication date: June 28, 2012
    Inventors: Scott L. Harbeson, Roger D. Tung
  • Patent number: 8207143
    Abstract: The present invention relates to the use of the compound according to formula (I), below for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states: Where X is H or F; R1 and R2 are independently H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (A) or (B) group; Where Nu is a radical of a biologically active compound such as an anticancer, antiviral or antihyperproliferative compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; each R8 is independently H, or a C1-C20 alkyl or ether group, preferably a C1-C12 alkyl group; k is 0-12, preferably, 0-2; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: January 11, 2011
    Date of Patent: June 26, 2012
    Assignee: Yale University
    Inventor: Yung-chi Cheng
  • Publication number: 20120142627
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2-amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.
    Type: Application
    Filed: November 29, 2011
    Publication date: June 7, 2012
    Applicants: Emory University, RFS Pharma, LLC
    Inventors: Raymond F. Schinazi, Steven J. Coats
  • Publication number: 20120142626
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: Pharmasset, Inc.
    Inventors: JINFA DU, Michael Joseph Sofia
  • Patent number: 8193165
    Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.
    Type: Grant
    Filed: August 17, 2009
    Date of Patent: June 5, 2012
    Assignee: Yale University
    Inventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
  • Publication number: 20120135950
    Abstract: Compositions and methods to treat lymphoma and cancer are disclosed. In particular, the method teaches treatment of lymphoma and cancer using anti-HERV-K(HML-2) therapies. Further taught are compositions and methods for characterizing patient samples to, for example, select or identify therapeutic options or assess the impact of therapies.
    Type: Application
    Filed: May 21, 2010
    Publication date: May 31, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Mark H. Kaplan, Rafael Contreras-Galindo, David Markovitz
  • Publication number: 20120135954
    Abstract: Described herein are compounds and methods that prevent the viral infection of cells. The compounds and methods described herein minimize viral resistance and maximize the number of targeted viruses. Additionally, the compounds and methods minimize the toxicity toward uninfected cells.
    Type: Application
    Filed: February 27, 2008
    Publication date: May 31, 2012
    Inventors: Luis M. Schang, Mireilli R. St. Vincent, Alexey V. Ustinov
  • Patent number: 8188222
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: May 29, 2012
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120129800
    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: Application
    Filed: January 14, 2010
    Publication date: May 24, 2012
    Applicant: Justus-Liebig-Universitat Giessen
    Inventor: Peter Mayser
  • Publication number: 20120114604
    Abstract: The present invention relates to co-administering a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The combination acts by interfering with the life cycle of the hepatitis C virus and is therefore useful as an antiviral therapy. As such, the combination may be used for treating or preventing Hepatitis C infections in patients. The invention also relates to compositions comprising the combination of inhibitors. The invention also relates to kits and pharmaceutical packs comprising a Hepatitis C virus NS3/4A protease inhibitor and a cytochrome P450 monooxygenase inhibitor. The invention also relates to processes for preparing these compositions, combinations, kits, and packs.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 10, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Tung, Gurudatt Chandorkar, Robert Perni
  • Publication number: 20120115807
    Abstract: Co-administration of alovudine and zidovudine at ratios considerably in excess of the prior art completely or substantially abolishes the mitochondrial toxicity of alovudine in mitochondrial DNA depletion experiments. The invention thus provides pharmaceutical compositions comprising alovudine and zidovudine in a molar ratio in the range 1:100 to 1:350 and methods for the treatment or prophylaxis of multiply resistant HIV comprising the simultaneous or consequential administration of alovudine and zidovudine in the characteristic molar ratio.
    Type: Application
    Filed: January 17, 2012
    Publication date: May 10, 2012
    Applicant: Medivir AB
    Inventors: Hong ZHANG, Bo Oberg
  • Patent number: 8173620
    Abstract: The disclosure encompasses caged compounds such as caged nucleoside phosphoesters (caged nucleotides). In an embodiment, the caged nucleotides include compounds corresponding to those described by formula (I) that may be activated by two-photon excitation, and methods of synthesis of such compounds. 8-Bromo-7-hydroxyquinoline-caged ATP was synthesized and examined for its photochemistry as a biologically useful, temporally and spatially controlled ATP-releasing reagent. The combination of two-photon excitation hydrolysis and activation of caged ATP enables methods for finely focusing ATP activation at the sub-cellular level or to a greater depth of activation, thereby providing improved resolution of ATP-dependent processes at the cellular level.
    Type: Grant
    Filed: August 20, 2009
    Date of Patent: May 8, 2012
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Timothy M. Dore, Yue Zhu, Khalilah G. Reddie, James D. Lauderdale
  • Publication number: 20120107276
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: December 28, 2011
    Publication date: May 3, 2012
    Applicant: Siga Technologies, Inc.
    Inventors: Dennis E. Hruby, Tove C. Bolken, Dongcheng Dai
  • Publication number: 20120093738
    Abstract: The present invention relates to taste-masked oral formulations of influenza antivirals. The taste-masked pharmaceutical formulations for oral administration comprise one or more influenza antivirals, at least one taste-masking agent and at least one pharmaceutically acceptable excipient. Further, the taste-masked influenza antiviral formulations of the present invention are provided in the form of dispersible tablets, effervescent tablets, orally disintegrating tablets, chewable tablets, bite-dispersion tablets or the like, wherein the bitter taste of influenza antivirals is masked thereby providing palatable formulations.
    Type: Application
    Filed: June 10, 2010
    Publication date: April 19, 2012
    Applicant: Rubicon Research Private Limited
    Inventors: Pratibha Sudhir Pilgaonkar, Maharukh Tehmasp Rustomjee, Anilkumar Surendrakumar Gandhi
  • Patent number: 8158607
    Abstract: The disclosure herein relates to a new Lamivudine polymorphic form, methods of making the same, and pharmaceutical formulations thereof. A (?) cis-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one in the form of monoclinic crystals has characteristic powder X-ray diffractogram, as disclosed herein, is disclosed along with a process for preparation of the same. A pharmaceutical composition in solid dosage unit form comprising a therapeutically effective amount of a new Lamivudine polymorphic form in combination with a pharmaceutically acceptable carrier is also disclosed along with a pharmaceutical composition useful for treating HIV infections in humans.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: April 17, 2012
    Assignee: Lupin Limited
    Inventors: Girij Pal Singh, Dhananjai Srivastava, Manmeet Brijkishore Saini, Pritesh Rameshbhai Upadhyay
  • Patent number: 8158606
    Abstract: It has been discovered that ?-L-2?-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. In addition, a method for preventing lamivudine resistant HBV (M552V) mutation from occurring in a naïve host is provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug. A method for preventing and/or suppressing the emergence of the HBV double mutant (L528M/M552V) in a host is also provided that includes administering a ?-L-2?-deoxynucleoside or its pharmaceutically acceptable salt, ester or prodrug.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: April 17, 2012
    Assignee: Novartis, AG
    Inventors: David Standring, Jean-Pierre Sommadossi, April Patty, Maria Seifer
  • Patent number: 8158605
    Abstract: The present invention is directed toward compounds of Formula (I) as follows: wherein, R is H, R5C(O); R1 is where the crossing dashed line illustrates the bond formed joining R1 to the molecule of Formula (I); R2 and R3 are independently OH or H, provided that R2 and R3 are not simultaneously OH; R4 is H or R5C(O), provided that R and R4 are not simultaneously H; and R5 is a C3-C26 alkenyl, or a pharmaceutical salt thereof. Methods of making and using these compounds are also disclosed.
    Type: Grant
    Filed: September 25, 2008
    Date of Patent: April 17, 2012
    Assignee: Mount Sinai School of Medicine
    Inventors: Lewis Silverman, James Holland
  • Publication number: 20120077772
    Abstract: The present invention relates to the oral solid pharmaceutical composition comprising lamivudine or a pharmaceutically acceptable salt thereof with isomalt as a filler. The present invention also relate to the combination of lamivudine and other Anti-HIV agents. Thus, for example, the present invention provides a stable tablet formulation comprising lamivudine, isomalt, crospovidone, calcium stearate and opadry white.
    Type: Application
    Filed: May 27, 2009
    Publication date: March 29, 2012
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Male Srinivas Reddy, Pothireddy Venkateswar Reddy, Muppidi Vanaja Kumari
  • Patent number: 8143234
    Abstract: The present invention provides methods of improving a cognitive function or a neurological function, treating or ameliorating a decline in a cognitive function or a neurological function, increasing cytidine levels, or treating a neurological disorder in a subject, comprising administering a uridine, a uridine precursor, or a derivative or metabolite thereof to the subject. The invention also provides methods of improving neural function, comprising contacting the neuron with a uridine, a uridine precursor, or a derivative or metabolite thereof.
    Type: Grant
    Filed: September 20, 2004
    Date of Patent: March 27, 2012
    Assignee: Massachusetts Institute of Technology
    Inventors: Richard J. Wurtman, Carol Watkins
  • Publication number: 20120070415
    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. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
    Type: Application
    Filed: September 19, 2011
    Publication date: March 22, 2012
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Publication number: 20120065145
    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: Application
    Filed: July 22, 2011
    Publication date: March 15, 2012
    Inventors: Stanton L. Gerson, Lili Liu
  • Publication number: 20120064127
    Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a) a lipid fraction comprising at least one of docosahexaenoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b) a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c) a mineral fraction comprising at least one of manganese and molybdenum, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.
    Type: Application
    Filed: November 11, 2011
    Publication date: March 15, 2012
    Applicant: N.V.NUTRICIA
    Inventor: Robert J.J. Hageman
  • Publication number: 20120065156
    Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
    Type: Application
    Filed: May 11, 2010
    Publication date: March 15, 2012
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20120040020
    Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.
    Type: Application
    Filed: October 27, 2011
    Publication date: February 16, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven John Durrant, David Kay, Michael O'Donnell, Ronald Marcellus Alphonsus Knegtel, Somhairle MacCormick, Joanne Pinder, Stephen Clinton Young, Haley Marie Binch, Thomas Cleveland, Lev Tyler Dewey Fanning, Dennis James Hurley, Pramod Joshi, Urvi Jagdishbhai Sheth, Alina Silina, Philip Michael Reaper, Anisa Nizarali Virani
  • Publication number: 20120034184
    Abstract: The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: October 17, 2011
    Publication date: February 9, 2012
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda