Nitrogen Atoms Occupy 1 And 3- Positions Patents (Class 514/86)
  • Patent number: 10307433
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: June 4, 2019
    Assignee: SRX Cardio, LLC
    Inventors: Thomas E. Barta, Jonathan W. Bourne, Kyle D. Monroe, Michael M. Muehlemann
  • Patent number: 10034892
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: July 31, 2018
    Assignee: SRX CARDIO, LLC
    Inventors: Thomas E. Barta, Jonathan W. Bourne, Kyle D. Monroe, Michael M. Muehlemann
  • Patent number: 9950994
    Abstract: Methods and compositions for pest control, and more particularly for control of ants, e.g., of the subfamily Myrmicinae, using tyramides.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: April 24, 2018
    Assignees: VMI Foundation, The United States of America, as represented by the secretary of agriculture
    Inventor: Tappey H. Jones
  • Patent number: 9924718
    Abstract: Control and repellency of biting flies, house flies, ticks, ants, fleas, biting midges, cockroaches, spiders and stink bugs is obtained by contact of the insects with at least one of the compounds of the structure (I).
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: March 27, 2018
    Assignee: Bedoukian Research, Inc.
    Inventor: Robert H. Bedoukian
  • Patent number: 9781936
    Abstract: Embodiments of the present disclosure, in one aspect, relate to compositions including a copper/silica nanocomposite and a polymer, methods of making a composition, methods of using a composition, and the like.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: October 10, 2017
    Assignee: UNIVERSITY OF CENTRAL FLORIDA RESEARCH FOUNDATION, INC.
    Inventors: Swadeshmukul Santra, Mikaeel Young
  • Patent number: 9743661
    Abstract: The present invention relates to a method of pre-rinsing laundry and treating other surfaces employing a composition that can kill bedbug eggs. The composition includes a fatty alcohol and an alcohol ethoxylate.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: August 29, 2017
    Assignee: Ecolab USA Inc.
    Inventors: Kim R. Smith, Erik C. Olson, Yvonne M. Killeen, Victor F. Man, Joelle F. Olson, Erin F. Loosbrock
  • Patent number: 9670196
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: June 6, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas A. Miller, Alessia Petrocchi, Eric T. Romeo, Dilrukshi Vitharana, Solomon D. Kattar, Alan B. Northrup, Michael D. Altman, Neville J. Anthony
  • Patent number: 9657324
    Abstract: The present invention is directed to methods of treating a subject, wherein a biological sample taken from the subject comprises an antibody against a small protein encoded by an intermediate stage transcript of HHV-6 (SITH-1), and the antibody against SITH-1 being present in an amount sufficient to be detected in the biological sample which is at least diluted 10-fold or more by an immunological detection method. Such treatment methods are used for the following: a) treating or preventing mood disorders; b) suppressing an elevation of the level of SITH-1 within cells in the subject's brain, reducing the number of cells in the brain that carry the protein SITH-1, and/or reducing the total amount of SITH-1 in the brain; c) suppressing an elevation of the level of a calcium modulating cyclophilin ligand (CAML) protein within cells in the subject's brain; or d) suppressing an elevation of the level of calcium ions within cells in the subject's brain.
    Type: Grant
    Filed: October 5, 2009
    Date of Patent: May 23, 2017
    Assignees: VIRUS IKAGAKU KENKYUSHO INC., JAPAN TOBACCO INC.
    Inventors: Kazuhiro Kondo, Nobuyuki Kobayashi
  • Patent number: 9624210
    Abstract: The invention provides certain amino-pyrimidine-containing compounds. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: April 18, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventor: Michelle R. Machacek
  • Patent number: 9611283
    Abstract: The invention features a method for treating patients who have an ALK-driven cancer, which is, or has become, refractory to one or more of crizotinib, CH5424802 and ASP3026, or which bears an ALK mutation identified herein, by administering a compound of formula (I) to the patient. The invention also features methods, kits, and compositions for characterizing ALK-driven cancers to determine whether they express an ALK mutant.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: April 4, 2017
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: Sen Zhang, William C. Shakespeare, Victor M. Rivera
  • Patent number: 9504686
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: November 29, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
  • Patent number: 9328075
    Abstract: In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: May 5, 2012
    Date of Patent: May 3, 2016
    Assignee: St. Jude Children's Research Hospital
    Inventors: Thomas R. Webb, Vincent A. Boyd
  • Patent number: 9327013
    Abstract: An activity enhancer for an anticancer agent includes, as an active ingredient, a D-form amino acid residue-containing FNIII14 polypeptide, the D-form amino acid residue-containing FNIII14 being a polypeptide FNIII14 represented by SEQ ID NO: 1 in which at least one of amino acid residues at positions 1 to 13 is a D-form amino acid residue. An anticancer composition includes the activity enhancer for an anticancer agent and an anticancer agent.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: May 3, 2016
    Assignees: TOKYO UNIVERSITY OF SCIENCE FOUNDATION, SAGA UNIVERSITY, NATIONAL UNIVERSITY CORPORATION KAGAWA UNIVERSITY
    Inventors: Fumio Fukai, Hiroaki Kodama, Takuya Matsunaga
  • Patent number: 9156829
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein L, X, Ra, Rb, R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 19, 2015
    Date of Patent: October 13, 2015
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Charlotte Fieldhouse, Angela Glen, Stephanie Maine, Tatsuhiko Fujimoto, John Stephen Robinson
  • Patent number: 9150519
    Abstract: The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: October 6, 2015
    Assignee: MERCK SERONO SA
    Inventors: Agnes Bombrun, Matthias Schwarz, Stefano Crosignani, David Covini, Delphine Marin
  • Patent number: 9125408
    Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an aryl carbamate as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an aryl carbamate compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or a plant defense activator.
    Type: Grant
    Filed: February 27, 2013
    Date of Patent: September 8, 2015
    Assignee: North Carolina State University
    Inventors: Christian Melander, Steven A. Rogers
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Patent number: 9034851
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: September 19, 2012
    Date of Patent: May 19, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
  • 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: 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
  • Patent number: 9023834
    Abstract: This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: May 5, 2015
    Assignee: TaiGen Biotechnology Co., Ltd.
    Inventors: Chi-Feng Yen, Judy Yuan, Chi-Hsin Richard King
  • Publication number: 20150119365
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: December 29, 2014
    Publication date: April 30, 2015
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Publication number: 20150098928
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Application
    Filed: January 6, 2014
    Publication date: April 9, 2015
    Applicant: E.I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Patent number: 8999958
    Abstract: Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: April 7, 2015
    Assignee: Johnson Matthey Public Limited Company
    Inventors: George Scott Wilson, Angela Barkley, Jurjus Jurayj
  • Patent number: 8993578
    Abstract: The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the therapies comprise administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection. For example, the therapies comprise administering to a subject an effective amounts of therapeutic agent 1, therapeutic agent 2 (or therapeutic agent 3), and an inhibitor of cytochrome P450 (e.g., ritonavir).
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: March 31, 2015
    Assignee: AbbVie Inc.
    Inventors: Barry M. Bernstein, Rajeev M. Menon, Amit Khatri, Sven Mensing, Sandeep Dutta, Daniel E. Cohen, Scott C. Brun, Walid M. Awni, Emily O. Dumas, Cheri E. Klein, Thomas J. Podsadecki
  • Publication number: 20150087619
    Abstract: The present application provides methods and compositions for treatment or reducing risk of dsDNA virus infection in post-hematopoietic cell transplant (HCT or HSCT) patients. This application also provides methods and composition for reducing the incidence of BK virus associated hematuria and/or renal impairment. The invention also relates to a method of lowering BK viral load in post-hematopoietic cell transplant (HCT or HSCT) patients with HDP-CDV (HDP-CDV) or compound of Formula II, or a pharmaceutically acceptable salt thereof, thereby delaying onset of or reducing risk of end organ disease in these patients.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: George R. Painter, JR., Ernest Randall Lanier, Dorothy Margolskee, Gwendolyn Powell Painter, Roy Ware
  • Publication number: 20150087509
    Abstract: The present invention relates to substituted pyrazole-containing compounds of formula (I), and the stereoisomers and salts thereof, wherein the substituents are as defined in the description. The present invention further relates to a method for combating or controlling invertebrate pests, to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound according to the present invention, to a method for treating or protecting an animal from infestation or infection by parasites, to a process for the preparation of a composition for treating infested or infected animals and/or for protecting animals against infestation or infection by parasites, and to a compound according to the invention for use as a medicament.
    Type: Application
    Filed: April 29, 2013
    Publication date: March 26, 2015
    Inventors: Karsten Körber, Florian Kaiser, Gemma Veitch, Wolfgang Von Deyn, Nina Gertrud Bandur, Joachim Dickhaut, Arun Narine, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Publication number: 20150079036
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
    Inventor: Chung K. Chu
  • Publication number: 20150080344
    Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
    Type: Application
    Filed: September 29, 2014
    Publication date: March 19, 2015
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20150065466
    Abstract: The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group.
    Type: Application
    Filed: April 18, 2013
    Publication date: March 5, 2015
    Inventor: Yongcheng Song
  • Publication number: 20150056193
    Abstract: The present disclosure provides methods of that include detecting in a biological sample from a patient having or suspected of having cancer the presence of a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and detecting in the biological sample the presence of a mutant EGFR polypeptide or a polynucleotide encoding the same. In some aspects, the disclosure provides methods of treating a patient for cancer that include determining that a biological sample from a tumor in the patient includes a polypeptide having ROS1 kinase activity or a polynucleotide encoding the same and a mutant EGFR polypeptide or a polynucleotide encoding the same and administering to the patient a therapeutically effective amount of a ROS1 inhibitor and an EGFR inhibitor, thereby treating the patient for cancer.
    Type: Application
    Filed: April 18, 2013
    Publication date: February 26, 2015
    Applicant: CELL SIGNALING TECHNOLOGY, INC.
    Inventors: Katherine Eleanor Crosby, Victoria McGuinness Rimkunas, Matthew Ren Silver, Herbert Haack
  • Publication number: 20150030541
    Abstract: The present invention provides phosphonate conjugates and methods of preparing the phosphonate conjugates so as to allow, for example, improved methods and compounds for modifying the surface of a nanoparticle to increase in vivo circulation times and targeted delivery performance.
    Type: Application
    Filed: October 14, 2014
    Publication date: January 29, 2015
    Inventor: Thomas E. Rogers
  • Patent number: 8940927
    Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
    Type: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8937055
    Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: January 20, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
  • Patent number: 8927525
    Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of CK1, CK1?1, CK1?2, CK1?3, CK2, Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, the AKT pathway, and/or the mTOR pathway.
    Type: Grant
    Filed: October 24, 2012
    Date of Patent: January 6, 2015
    Assignee: Jasco Pharmaceuticals, LLC
    Inventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Stephane A. Dumas, Yvonne L. Flanders
  • Publication number: 20140364397
    Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 11, 2014
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20140349972
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Application
    Filed: September 19, 2012
    Publication date: November 27, 2014
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
  • Patent number: 8889159
    Abstract: Disclosed herein are a composition and unit dosage form for the treatment of hepatitis C virus (HCV) infection comprising GS-7977 and at least one pharmaceutically acceptable excipient, as well as methods for making said composition and unit dosage form. Also disclosed herein is a method of treating a subject, preferably a human, infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of GS-7977 and an effective amount of ribavirin. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of GS-7977 and an effective amount of ribavirin. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: November 18, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Darryl G. Cleary, Charles J. Reynolds, Miriam Michelle Berrey, Robert G. Hindes, William T. Symonds, Adrian S. Ray, Hongmei Mo, Christy M. Hebner, Reza Oliyai, Vahid Zia, Dimitrios Stefanidis, Rowchanak Pakdaman, Melissa Jean Casteel
  • Patent number: 8889658
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: November 18, 2014
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Publication number: 20140336155
    Abstract: The invention relates to novel active substance combinations consisting of heterocyclic trifluorobutenylen of formula (1), wherein X is halogen and n is 0, 1 or 2, and of known insecticide substances. Said novel active substance combinations are suitable for fighting harmful pests like insects and nematodes.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 13, 2014
    Inventors: Wolfram ANDERSCH, Anton KRAUS, Koichi ISHIKAWA
  • Patent number: 8883765
    Abstract: Artemisinin-derived monomers and artemisinin dimers are shown to exhibit in-vitro anti-cytomegalovirus (CMV) activity. Artemisinin dimers effectively inhibited CMV replication in human foreskin fibroblasts and human embryonic lung fibroblasts with no cytotoxicity at concentrations required for complete CMV inhibition. Artemisinin dimers were found to be potent and non-cytotoxic inhibitors of CMV replication, which indicates their use as therapeutic agents for the treatment of CMV infection in humans.
    Type: Grant
    Filed: December 8, 2010
    Date of Patent: November 11, 2014
    Assignee: The John Hopkins University
    Inventors: Ravit Arav-Boger, Gary Posner
  • Publication number: 20140328778
    Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative represented by Formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the therapeutic and/or prophylactic treatment of, inter alia, dermatitis.
    Type: Application
    Filed: July 17, 2014
    Publication date: November 6, 2014
    Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
  • Patent number: 8871746
    Abstract: Methods, compounds, and pharmaceutical compositions for treating arenavirus infections are disclosed. Methods for preparing the compounds and pharmaceutical compositions are also disclosed. The novel compounds and compositions are used for treatment of arenavirus infections, which include but are not limited to the following viruses: Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: October 28, 2014
    Assignee: Kineta Four, LLC
    Inventors: Dongcheng Dai, Sean M. Amberg, Tove Bolken, Dennis E. Hruby
  • Publication number: 20140303092
    Abstract: The present application provides methods and compositions for treatment or prevention of dsDNA virus infection in post-hematopoietic cell transplant (HCT or HSCT) patients.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Applicant: CHIMERIX, INC
    Inventors: George R. Painter, Ernest Randall Lanier, Merrick R. Almond, Dorothy Margolskee, Gwendolyn Powell Painter
  • Patent number: 8846643
    Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: September 30, 2014
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20140288025
    Abstract: The invention relates to fatty acid antiviral conjugates; compositions comprising an effective amount of a fatty acid antiviral conjugate; and methods for treating or preventing a viral infection comprising the administration of an effective amount of a fatty acid antiviral conjugate.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 25, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. MILNE, Michael R. JIROUSEK, Chi B. VU, Allison WENSLEY, Amal TING
  • Publication number: 20140274959
    Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Regents of the University of California, a California corporation
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20140243290
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Patent number: 8816082
    Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: August 26, 2014
    Assignee: The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Youla S. Tsantrizos, Joris Wim De Schutter, Yih-Shyan Lin
  • Publication number: 20140235583
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Application
    Filed: September 19, 2012
    Publication date: August 21, 2014
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua